ID

DB00210|APRD00780||

名称

Adapalene

描述

Acne vulgaris is a multifactorial disorder of the pilosebaceous unit involving increased sebum production, inflammation, and hyperproliferation/hyperkeratinization of the follicular infundibulum. It is also associated with _Cutibacterium acnes_ (also known as _Propionibacterium acnes_). Adapalene is a third-generation topical retinoid used for the treatment of acne vulgaris.[A193518] Adapalene has similar efficacy but a superior safety profile compared to tretinoin.[A193521] [Tazarotene] is more efficacious than adapalene but is designated as pregnancy category X and hence is contraindicated in pregnant women.[A193518] Adapalene can also be combined with benzoyl peroxide (BPO), which possesses bactericidal properties[A193524], and either adapalene alone, or adapalene BPO combination products, are commonly used to treat mild-to-severe acne.[A193518] Differin®, produced by Galderma Labs, was first granted FDA approval on May 31st, 1996, as a 0.1% adapalene topical solution. Differin was later made available as 0.1% gel, cream, or lotion, or 0.3% gel products. On December 8th, 2008, Galderma Labs gained FDA approval for Epiduo®, a 0.1% adapalene, 2.5% BPO combination gel.[L12873]

cas号

106685-40-9

唯一标识码

1L4806J2QF

状态

solid

组

approved,

指示

Adapalene is indicated for the topical treatment of acne vulgaris in patients aged 12 and over.[L12873]

药效学

Adapalene is anticomedogenic, preventing the formation of new comedones and inflammatory lesions, and also acts to reduce inflammation by modulating the innate immune response.[A193512] Like other retinoid compounds, adapalene is chemically stable but photosensitive; use with sunscreen is recommended. Minor skin irritations, including erythema, scaling, dryness, and stinging/burning, have been reported.[L12873]

作用机制

Adapalene is used for the treatment/maintenance of mild-to-severe acne (acne vulgaris). Acne is a multifactorial condition, and evidence exists to support multiple mechanisms of action for adapalene. Adapalene binds to retinoic acid receptor (RAR)-beta and RAR-gamma; this complex subsequently binds to one of three retinoid X receptors (RXRs), which as a complex is capable of binding DNA to modulate transcriptional activity.[A193509] Although the full extent of transcriptional modulation is not described, retinoid activation is generally known to affect cellular proliferation and differentiation[A193527], and adapalene has been shown to inhibit HeLa cell proliferation and human keratinocyte differentiation.[A193515] These effects primarily account for adapalene's comedolytic and anticomedogenic properties. In addition, adapalene modulates the immune response by down-regulating toll-like receptor 2 (TLR-2) expression and inhibiting the transcription factor activator protein 1 (AP-1). TLR-2 recognizes _Cutibacterium acnes_ (formerly _Propionibacterium acnes_), the bacterium primarily associated with acne. TLR-2 activation causes nuclear translocation of AP-1 and downstream pro-inflammatory gene regulation. Therefore, adapalene has a general anti-inflammatory effect, which reduces inflammation-mediated acne symptoms.[A193512] When used with benzoyl peroxide, which possesses free radical-mediated bactericidal effects, the combination acts synergistically to reduced comedones and inflammatory lesions.[A193512]

毒性

Toxicity information regarding adapalene is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as redness, scaling, and skin discomfort. Symptomatic and supportive measures are recommended.[L12873] Adapalene has an acute oral LD₅₀ in S-D rats and CD-1 mice of over 5000 mg/kg. The LD₅₀ of 0.3% applied topically to Credo OF1 mice is over 10 ml/kg (30 mg/kg). No systemic or local toxicity was observed in rats treated topically with 6 mg/kg/day of 0.3% adapalene.[L12897]

代谢

Extensive information regarding adapalene metabolism in humans is unavailable, although it is known to accumulate in the liver and GI-tract. In human, mouse, rat, rabbit, and dog cultured hepatocytes, metabolism appears to affect the methoxybenzene moiety but remains incompletely characterized. The major products of metabolism are glucuronides. Approximately 25% of the drug is metabolized; the rest is excreted as parent drug.[L12897]

吸收

Adapalene is applied topically and absorbed through the skin. In one clinical study treating patients once per day with 2g of 0.3% gel applied to 2 mg/cm² of skin, 15 patients had detectable blood plasma adapalene levels (0.1 ng/ml) resulting in a mean C_max of 0.553 ± 0.466 ng/ml and a mean AUC of 8.37 ± 8.46 ng\*h/ml on day 10.[L12873]

半衰期

In one clinical study, after ten days of treatment with 2g of 0.3% cream or gel, the terminal half-life was between 7 and 51 hours, with a mean of 17.2 ± 10.2.[L12873]

分类

description:This compound belongs to the class of organic compounds known as retinoids. These are oxygenated derivatives of 3,7-dimethyl-1-(2,6,6-trimethylcyclohex-1-enyl)nona-1,3,5,7-tetraene and derivatives thereof.
direct-parent:Retinoids
kingdom:Organic compounds
superclass:Lipids and lipid-like molecules
class:Prenol lipids
subclass:Retinoids
alternative-parent:Alkyl aryl ethers
alternative-parent:Anisoles
alternative-parent:Carboxylic acids
alternative-parent:Hydrocarbon derivatives
alternative-parent:Methoxybenzenes
alternative-parent:Monocarboxylic acids and derivatives
alternative-parent:Naphthalenecarboxylic acids
alternative-parent:Organic oxides
alternative-parent:Phenoxy compounds
alternative-parent:Phenylnaphthalenes
substituent:2-naphthalenecarboxylic acid
substituent:2-naphthalenecarboxylic acid or derivatives
substituent:Adapalene
substituent:Alkyl aryl ether
substituent:Anisole
substituent:Aromatic homopolycyclic compound
substituent:Benzenoid
substituent:Carboxylic acid
substituent:Carboxylic acid derivative
substituent:Ether
substituent:Hydrocarbon derivative
substituent:Methoxybenzene
substituent:Monocarboxylic acid or derivatives
substituent:Monocyclic benzene moiety
substituent:Naphthalene
substituent:Organic oxide
substituent:Organic oxygen compound
substituent:Organooxygen compound
substituent:Phenol ether
substituent:Phenoxy compound
substituent:Phenylnaphthalene

消除途径

Adapalene is primarily excreted by the biliary route at about 30 ng/g of the topically applied amount. Approximately 75% of the drug remains unchanged.[A193509]

种类

Anti-Acne Preparations

Anti-Acne Preparations for Topical Use

Anti-Inflammatory Agents
D000893
Dermatologicals
D003879
Misc. Skin and Mucous Membrane Agents

Naphthalenes
D009281
Retinoids
D012176
Retinoids for Topical Use in Acne

盐类

蛋白质结合

清除

Adapalene is rapidly cleared from blood plasma, typically undetectable after 72 hours following topical application.[L12873]

同义词

language:english; code:; name;6-(3-(1-Adamantyl)-4-methoxyphenyl)-2-naphthoic acid
language:english; code:inn/usan; name;Adapalene
language:french; code:inn; name;Adapalène
language:spanish; code:inn; name;Adapaleno
language:latin; code:inn; name;Adapalenum

国际品牌

AdaferinDifferine

配送量

产品

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ema-product-code:
ema-ma-number:
started-marketing-on:2019-11-08
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:ANDA208108
generic:true
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Adapalene and Benzoyl Peroxide
labeller:Taro Pharmaceuticals U.S.A., Inc.
ndc-id:
ndc-product-code:51672-1384
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2018-10-17
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:ANDA209148
generic:true
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Adapalene and Benzoyl Peroxide Swab
labeller:Biomes Pharmaceuticals
ndc-id:
ndc-product-code:69150-001
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2020-12-01
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:
generic:false
over-the-counter:false
approved:false
country:US
source:FDA NDC
name:Adapalene Topical Solution
labeller:Marnel Pharmaceuticals, Inc.
ndc-id:
ndc-product-code:0682-0053
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2018-08-27
ended-marketing-on:
dosage-form:Swab
strength:1 mg/1mL
route:Topical
fda-application-number:ANDA204593
generic:true
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Adapalene Topical Solution
labeller:Allegis Holdings LLC
ndc-id:
ndc-product-code:71297-410
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2016-10-03
ended-marketing-on:
dosage-form:Solution
strength:1 mg/1mL
route:Topical
fda-application-number:ANDA203981
generic:true
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Adapalene Topical Solution
labeller:CALL INC (d.b.a Rochester Pharmaceuticals)
ndc-id:
ndc-product-code:49908-117
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2016-10-03
ended-marketing-on:2020-01-17
dosage-form:Solution
strength:1 mg/1mL
route:Topical
fda-application-number:ANDA203981
generic:true
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Clindap-T
labeller:Accumix Pharmaceuticals
ndc-id:
ndc-product-code:69167-1015
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2014-12-15
ended-marketing-on:2015-07-17
dosage-form:Kit
strength:
route:Topical
fda-application-number:
generic:false
over-the-counter:false
approved:false
country:US
source:FDA NDC
name:Differin
labeller:DPT Laboratories, Ltd.
ndc-id:
ndc-product-code:63094-5905
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:1998-01-28
ended-marketing-on:2006-01-31
dosage-form:Solution
strength:1 mg/1mL
route:Topical
fda-application-number:NDA020338
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Differin
labeller:Physicians Total Care, Inc.
ndc-id:
ndc-product-code:54868-5271
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2005-04-19
ended-marketing-on:
dosage-form:Cream
strength:1 mg/1g
route:Topical
fda-application-number:NDA020748
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Differin
labeller:Physicians Total Care, Inc.
ndc-id:
ndc-product-code:54868-6114
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2010-04-27
ended-marketing-on:
dosage-form:Lotion
strength:1 mg/1g
route:Topical
fda-application-number:NDA022502
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Differin
labeller:Physicians Total Care, Inc.
ndc-id:
ndc-product-code:54868-5958
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2008-10-24
ended-marketing-on:
dosage-form:Gel
strength:3 mg/1g
route:Topical
fda-application-number:NDA021753
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Differin
labeller:Physicians Total Care, Inc.
ndc-id:
ndc-product-code:54868-5030
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2004-07-07
ended-marketing-on:
dosage-form:Gel
strength:1 mg/1g
route:Topical
fda-application-number:NDA020380
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Differin
labeller:Galderma
ndc-id:
ndc-product-code:0299-5918
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2009-09-15
ended-marketing-on:
dosage-form:Gel
strength:3 mg/1g
route:Topical
fda-application-number:NDA021753
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Differin
labeller:Galderma
ndc-id:
ndc-product-code:0299-5912
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2010-03-31
ended-marketing-on:
dosage-form:Lotion
strength:0.1 g/100mL
route:Topical
fda-application-number:NDA022502
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Differin
labeller:Galderma
ndc-id:
ndc-product-code:0299-5915
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2009-11-24
ended-marketing-on:
dosage-form:Cream
strength:1 mg/1g
route:Topical
fda-application-number:NDA020748
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Differin
labeller:Galderma Laboratories, L.P.
ndc-id:
ndc-product-code:0299-4910
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2016-07-08
ended-marketing-on:
dosage-form:Gel
strength:1 mg/1g
route:Topical
fda-application-number:NDA020380
generic:false
over-the-counter:true
approved:true
country:US
source:FDA NDC
name:Differin
labeller:Galderma Laboratories, L.P.
ndc-id:
ndc-product-code:0299-5910
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:1996-05-31
ended-marketing-on:2019-07-08
dosage-form:Gel
strength:1 mg/1g
route:Topical
fda-application-number:NDA020380
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Differin
labeller:Galderma
ndc-id:
ndc-product-code:
dpd-id:02148749
ema-product-code:
ema-ma-number:
started-marketing-on:1996-12-31
ended-marketing-on:
dosage-form:Gel
strength:0.1 %
route:Topical
fda-application-number:
generic:false
over-the-counter:false
approved:true
country:Canada
source:DPD
name:Differin
labeller:Galderma
ndc-id:
ndc-product-code:
dpd-id:02231592
ema-product-code:
ema-ma-number:
started-marketing-on:1998-01-08
ended-marketing-on:
dosage-form:Cream
strength:0.1 %
route:Topical
fda-application-number:
generic:false
over-the-counter:false
approved:true
country:Canada
source:DPD
name:Differin
labeller:Galderma
ndc-id:
ndc-product-code:
dpd-id:02148757
ema-product-code:
ema-ma-number:
started-marketing-on:2001-08-08
ended-marketing-on:2003-07-08
dosage-form:Liquid
strength:0.1 %
route:Topical
fda-application-number:
generic:false
over-the-counter:false
approved:true
country:Canada
source:DPD
name:Differin
labeller:Galderma
ndc-id:
ndc-product-code:
dpd-id:02376660
ema-product-code:
ema-ma-number:
started-marketing-on:
ended-marketing-on:
dosage-form:Lotion
strength:0.1 %
route:Topical
fda-application-number:
generic:false
over-the-counter:false
approved:true
country:Canada
source:DPD
name:Differin Xp
labeller:Galderma
ndc-id:
ndc-product-code:
dpd-id:02274000
ema-product-code:
ema-ma-number:
started-marketing-on:2007-07-19
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:
generic:false
over-the-counter:false
approved:true
country:Canada
source:DPD
name:Epiduo
labeller:Physicians Total Care, Inc.
ndc-id:
ndc-product-code:54868-5991
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2009-02-24
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:NDA022320
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Epiduo
labeller:Galderma
ndc-id:
ndc-product-code:0299-5908
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2008-12-08
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:NDA022320
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Epiduo Forte
labeller:Galderma Laboratories, L.P.
ndc-id:
ndc-product-code:0299-5906
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2015-07-01
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:NDA207917
generic:false
over-the-counter:false
approved:true
country:US
source:FDA NDC
name:Nuvya
labeller:Accumix Pharmaceuticals
ndc-id:
ndc-product-code:69167-0485
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2014-12-15
ended-marketing-on:2015-07-17
dosage-form:Kit
strength:
route:Topical
fda-application-number:
generic:false
over-the-counter:false
approved:false
country:US
source:FDA NDC
name:Proactiv MD Adapalene Acne Treatment
labeller:The Proactiv Company, Llc
ndc-id:
ndc-product-code:11410-956
dpd-id:
ema-product-code:
ema-ma-number:
started-marketing-on:2017-03-27
ended-marketing-on:
dosage-form:Gel
strength:0.1 g/100g
route:Topical
fda-application-number:NDA020380
generic:true
over-the-counter:true
approved:true
country:US
source:FDA NDC
name:Sandoz Adapalene/benzoyl Peroxide
labeller:Sandoz Canada Incorporated
ndc-id:
ndc-product-code:
dpd-id:02489007
ema-product-code:
ema-ma-number:
started-marketing-on:2019-09-27
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:
generic:true
over-the-counter:false
approved:true
country:Canada
source:DPD
name:Tactupump
labeller:Galderma
ndc-id:
ndc-product-code:
dpd-id:02365871
ema-product-code:
ema-ma-number:
started-marketing-on:2011-05-13
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:
generic:false
over-the-counter:false
approved:true
country:Canada
source:DPD
name:Tactupump Forte
labeller:Galderma
ndc-id:
ndc-product-code:
dpd-id:02446235
ema-product-code:
ema-ma-number:
started-marketing-on:2016-01-04
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:
generic:false
over-the-counter:false
approved:true
country:Canada
source:DPD
name:Taro-adapalene/benzoyl Peroxide
labeller:Taro Pharmaceuticals, Inc.
ndc-id:
ndc-product-code:
dpd-id:02456923
ema-product-code:
ema-ma-number:
started-marketing-on:2019-10-01
ended-marketing-on:
dosage-form:Gel
strength:
route:Topical
fda-application-number:
generic:true
over-the-counter:false
approved:true
country:Canada
source:DPD

混合物

name:Differin
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Differin
ingredients:Adapalene
name:Differin
ingredients:Adapalene
name:Differin
ingredients:Adapalene
name:Differin
ingredients:Adapalene
name:Epiduo
ingredients:Adapalene + Benzoyl peroxide
name:Clindap-T
ingredients:Adapalene + Clindamycin
name:Nuvya
ingredients:Adapalene + Diclofenac + Tamoxifen
name:Adapalene
ingredients:Adapalene
name:Proactiv MD Adapalene Acne Treatment
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene and Benzoyl Peroxide
ingredients:Adapalene + Benzoyl peroxide
name:Adapalene
ingredients:Adapalene
name:ADAPALENE and BENZOYL PEROXIDE
ingredients:Adapalene + Benzoyl peroxide
name:Adapalene
ingredients:Adapalene
name:Differin
ingredients:Adapalene
name:Differin
ingredients:Adapalene
name:Epiduo
ingredients:Adapalene + Benzoyl peroxide
name:Differin
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene and Benzoyl Peroxide
ingredients:Adapalene + Benzoyl peroxide
name:Adapalene and Benzoyl Peroxide
ingredients:Adapalene + Benzoyl peroxide
name:Adapalene Topical Solution
ingredients:Adapalene
name:Adapalene 0.3% / Niacinamide 4%
ingredients:Adapalene + Nicotinamide
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene and Benzoyl Peroxide
ingredients:Adapalene + Benzoyl peroxide
name:Adapalene
ingredients:Adapalene
name:Adapalene Topical Solution
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene and Benzoyl Peroxide
ingredients:Adapalene + Benzoyl peroxide
name:Adapalene
ingredients:Adapalene
name:Epiduo Forte
ingredients:Adapalene + Benzoyl peroxide
name:Adapalene and Benzoyl Peroxide
ingredients:Adapalene + Benzoyl peroxide
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Differin
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene 0.3% / Benzoyl Peroxide 2.5% / Niacinamide 4%
ingredients:Adapalene + Benzoyl peroxide + Nicotinamide
name:Adapalene 0.1% / Benzoyl Peroxide 2.5% / Niacinamide 4%
ingredients:Adapalene + Benzoyl peroxide + Nicotinamide
name:Adapalene 0.3% / Benzoyl Peroxide 2.5% / Clindamycin 1%
ingredients:Adapalene + Benzoyl peroxide + Clindamycin
name:Adapalene 0.1% / Benzoyl Peroxide 2.5% / Clindamycin 1%
ingredients:Adapalene + Benzoyl peroxide + Clindamycin
name:Differin
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene Topical Solution
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene
ingredients:Adapalene
name:Adapalene and Benzoyl Peroxide Swab
ingredients:Adapalene + Benzoyl peroxide
name:Differin
ingredients:Adapalene
name:Differin
ingredients:Adapalene
name:Differin Xp
ingredients:Adapalene
name:Tactupump
ingredients:Adapalene + Benzoyl peroxide
name:Differin
ingredients:Adapalene
name:Differin
ingredients:Adapalene
name:Tactupump Forte
ingredients:Adapalene + Benzoyl peroxide
name:Sandoz Adapalene/benzoyl Peroxide
ingredients:Adapalene + Benzoyl peroxide
name:Taro-adapalene/benzoyl Peroxide
ingredients:Adapalene + Benzoyl peroxide

包装者

name:Ameri-Pac Inc.
url:http://www.ameri-pac.com
name:DPT Laboratories Ltd.
url:http://www.dptlabs.com
name:E. Fougera and Co.
url:http://www.fougera.com
name:Galderma Laboratories
url:http://www.galderma.com
name:Glenmark Generics Ltd.
url:http://www.glenmark-generics.com
name:Lake Erie Medical and Surgical Supply
url:
name:Physicians Total Care Inc.
url:http://www.physicianstotalcare.com
name:Teva Pharmaceutical Industries Ltd.
url:http://www.tevapharm.com

生产者

generic:是; url:; name;Nycomed us inc
generic:否; url:; name;Galderma laboratories lp
generic:是; url:; name;Glenmark generics inc usa
generic:是; url:; name;Pliva hrvatska doo
generic:否; url:; name;Galderma research and development inc
generic:否; url:; name;Galderma Laboratories

价格

Differin 0.1% cream
4.85(单位：USD）
g
Differin 0.3% Gel 45 gm Tube
219.65(单位：USD）
tube
Differin 0.1% Cream 45 gm Tube
227.13(单位：USD）
tube
Differin 0.1% Gel 45 gm Tube
227.13(单位：USD）
tube

受影响的生物体

Humans and other mammals

剂量

form:Gel
route:Topical
strength:0.1 g
form:Cream
route:Topical
strength:0.1 g/100g
form:Cream
route:Topical
strength:1 mg/1g
form:Gel
route:Topical
strength:1 mg/1g
form:Gel
route:Topical
strength:45 g/1g
form:Lotion
route:Topical
strength:.1 g/100mL
form:Swab
route:Topical
strength:1 mg/1mL
form:Cream
route:Topical
strength:1 MG/G
form:Gel
route:
strength:25 mg
form:Gel
route:Topical
strength:1 g
form:Kit
route:Topical
strength:
form:Gel
route:Cutaneous
strength:0.1 % w/w
form:Cream
route:Topical
strength:0.1 %
form:Cream
route:Topical
strength:100 mg/100g
form:Gel
route:Topical
strength:100 mg/100g
form:Gel
route:Topical
strength:3 mg/1g
form:Liquid
route:Topical
strength:0.1 %
form:Lotion
route:Topical
strength:0.1 %
form:Lotion
route:Topical
strength:0.1 g/100mL
form:Lotion
route:Topical
strength:1 mg/1g
form:Solution
route:Topical
strength:1 mg/1mL
form:Gel
route:Topical
strength:1 mg/g
form:Gel
route:Topical
strength:0.1 %
form:Cream
route:Cutaneous
strength:0.1 %
form:Gel
route:Topical
strength:
form:Gel
route:Topical
strength:
form:Gel
route:Topical
strength:0.3 %
form:Gel
route:Cutaneous
strength:0.1 %
form:Gel
route:Topical
strength:2.5 %
form:Gel
route:Topical
strength:0.3 g
form:Cream
route:
strength:0.1 % w/w
form:Gel
route:Topical
strength:0.1 MG/G
form:Solution
route:Topical
strength:0.1 g
form:Gel
route:Topical
strength:0.1 % W/W
form:Gel
route:
strength:1 mg
form:Gel
route:Topical
strength:0.1 g/100g
form:Cream
route:Topical
strength:0.1 g

atc代码

Retinoids for topical use in acne
ANTI-ACNE PREPARATIONS FOR TOPICAL USE
ANTI-ACNE PREPARATIONS
DERMATOLOGICALS
Retinoids for topical use in acne
ANTI-ACNE PREPARATIONS FOR TOPICAL USE
ANTI-ACNE PREPARATIONS
DERMATOLOGICALS

fda标签

//s3-us-west-2.amazonaws.com/drugbank/fda_labels/DB00210.pdf?1265922800

化学品安全技术说明书

//s3-us-west-2.amazonaws.com/drugbank/msds/DB00210.pdf?1265922740

专利

number:4717720
country:United States
approved:1988-01-05
expires:2010-05-31
pediatric-extension:否
number:8909305
country:United States
approved:2014-12-09
expires:2022-12-23
pediatric-extension:否
number:7579377
country:United States
approved:2009-08-25
expires:2025-02-23
pediatric-extension:否
number:7834060
country:United States
approved:2010-11-16
expires:2023-03-12
pediatric-extension:否
number:7868044
country:United States
approved:2011-01-11
expires:2023-03-12
pediatric-extension:否
number:8703820
country:United States
approved:2014-04-22
expires:2023-03-12
pediatric-extension:否
number:7838558
country:United States
approved:2010-11-23
expires:2023-03-12
pediatric-extension:否
number:7737181
country:United States
approved:2010-06-15
expires:2024-08-29
pediatric-extension:否
number:7964202
country:United States
approved:2011-06-21
expires:2024-09-01
pediatric-extension:否
number:8071644
country:United States
approved:2011-12-06
expires:2027-07-18
pediatric-extension:否
number:8080537
country:United States
approved:2011-12-20
expires:2027-07-18
pediatric-extension:否
number:8105618
country:United States
approved:2012-01-31
expires:2022-12-23
pediatric-extension:否
number:8129362
country:United States
approved:2012-03-06
expires:2027-07-18
pediatric-extension:否
number:8445543
country:United States
approved:2013-05-21
expires:2027-07-12
pediatric-extension:否
number:8809305
country:United States
approved:2014-08-19
expires:2022-12-23
pediatric-extension:否
number:8936800
country:United States
approved:2015-01-20
expires:2022-12-23
pediatric-extension:否
number:8241649
country:United States
approved:2012-08-14
expires:2022-12-23
pediatric-extension:否
number:7820186
country:United States
approved:2010-10-26
expires:2025-11-23
pediatric-extension:否
number:7998467
country:United States
approved:2011-08-16
expires:2028-05-31
pediatric-extension:否
number:8435502
country:United States
approved:2013-05-07
expires:2026-09-15
pediatric-extension:否
number:8709392
country:United States
approved:2014-04-29
expires:2026-09-15
pediatric-extension:否
number:8785420
country:United States
approved:2014-07-22
expires:2022-12-23
pediatric-extension:否
number:8729127
country:United States
approved:2014-05-20
expires:2023-03-12
pediatric-extension:否
number:9381179
country:United States
approved:2016-07-05
expires:2023-03-12
pediatric-extension:否
number:9387187
country:United States
approved:2016-07-12
expires:2023-03-12
pediatric-extension:否
number:9814690
country:United States
approved:2017-11-14
expires:2022-12-23
pediatric-extension:否

食物相互作用

药物相互作用

DB00936
The risk or severity of adverse effects can be increased when Salicylic acid is combined with Adapalene.
DB11085
The risk or severity of adverse effects can be increased when Resorcinol is combined with Adapalene.

序列

实验性质

Melting Point
300
http://datasheets.scbt.com/sds/aghs/en/sc-203803.pdf
Boiling Point
606.3
http://datasheets.scbt.com/sds/aghs/en/sc-203803.pdf
logP
6.917
http://www.chemspider.com/Chemical-Structure.54244.html?rid=2edd1b0e-994a-4cdc-870c-186c62dcad5a&page_num=0

外部标识符

resource：Drugs Product Database (DPD)
identifier：224
resource：ChEBI
identifier：31174
resource：PubChem Compound
identifier：60164
resource：PubChem Substance
identifier：46505019
resource：KEGG Drug
identifier：D01112
resource：ChemSpider
identifier：54244
resource：BindingDB
identifier：50048280
resource：PharmGKB
identifier：PA448047
resource：Therapeutic Targets Database
identifier：DAP000115
resource：Wikipedia
identifier：Adapalene
resource：ChEMBL
identifier：CHEMBL1265
resource：ZINC
identifier：ZINC000003784182
resource：RxCUI
identifier：60223

外部链接

RxList
http://www.rxlist.com/cgi/generic3/adapalene.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/dif1134.shtml
Drugs.com
http://www.drugs.com/cdi/adapalene-cream.html

路径

目标

id:BE0000206
name:Retinoic acid receptor beta
organism:Humans
action:agonist
Shroot B, Michel S: Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.
Pierard GE, Pierard-Franchimont C, Paquet P, Quatresooz P: Spotlight on adapalene. Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1565-75. doi: 10.1517/17425250903386269.
Ghyselinck NB, Duester G: Retinoic acid signaling pathways. Development. 2019 Jul 4;146(13). pii: 146/13/dev167502. doi: 10.1242/dev.167502.
Kim MJ, Ciletti N, Michel S, Reichert U, Rosenfield RL: The role of specific retinoid receptors in sebocyte growth and differentiation in culture. J Invest Dermatol. 2000 Feb;114(2):349-53.
known-action:yes
name:Retinoic acid receptor beta
general-function:Zinc ion binding
specific-function:Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence or presence of hormone ligand, acts mainly as an activator of gene expression due to weak binding to corepressors. In concert with RARG, required for skeletal growth, matrix homeostasis and growth plate function.
gene-name:RARB
locus:3p24
cellular-location:Nucleus
transmembrane-regions:
signal-regions:
theoretical-pi:7.86
molecular-weight:50488.63
chromosome-location:3
organism:Humans
external-identifiers:HUGO Gene Nomenclature Committee (HGNC)HGNC:9865GenAtlasRARBGenBank Gene DatabaseX07282GenBank Protein Database35883IUPHAR591Guide to Pharmacology591UniProtKBP10826UniProt AccessionRARB_HUMAN
synonyms:HAPHBV-activated proteinNR1B2Nuclear receptor subfamily 1 group B member 2RAR-betaRAR-epsilon
amino-acid-sequence:>lcl|BSEQ0000411|Retinoic acid receptor beta MTTSGHACPVPAVNGHMTHYPATPYPLLFPPVIGGLSLPPLHGLHGHPPPSGCSTPSPAT IETQSTSSEELVPSPPSPLPPPRVYKPCFVCQDKSSGYHYGVSACEGCKGFFRRSIQKNM IYTCHRDKNCVINKVTRNRCQYCRLQKCFEVGMSKESVRNDRNKKKKETSKQECTESYEM TAELDDLTEKIRKAHQETFPSLCQLGKYTTNSSADHRVRLDLGLWDKFSELATKCIIKIV EFAKRLPGFTGLTIADQITLLKAACLDILILRICTRYTPEQDTMTFSDGLTLNRTQMHNA GFGPLTDLVFTFANQLLPLEMDDTETGLLSAICLICGDRQDLEEPTKVDKLQEPLLEALK IYIRKRRPSKPHMFPKILMKITDLRSISAKGAERVITLKMEIPGSMPPLIQEMLENSEGH EPLTPSSSGNTAEHSPSISPSSVENSGVSQSPLVQ
gene-sequence:>lcl|BSEQ0010005|Retinoic acid receptor beta (RARB) ATGTTTGACTGTATGGATGTTCTGTCAGTGAGTCCTGGGCAAATCCTGGATTTCTACACT GCGAGTCCGTCTTCCTGCATGCTCCAGGAGAAAGCTCTCAAAGCATGCTTCAGTGGATTG ACCCAAACCGAATGGCAGCATCGGCACACTGCTCAATCAATTGAAACACAGAGCACCAGC TCTGAGGAACTCGTCCCAAGCCCCCCATCTCCACTTCCTCCCCCTCGAGTGTACAAACCC TGCTTCGTCTGCCAGGACAAATCATCAGGGTACCACTATGGGGTCAGCGCCTGTGAGGGA TGTAAGGGCTTTTTCCGCAGAAGTATTCAGAAGAATATGATTTACACTTGTCACCGAGAT AAGAACTGTGTTATTAATAAAGTCACCAGGAATCGATGCCAATACTGTCGACTCCAGAAG TGCTTTGAAGTGGGAATGTCCAAAGAATCTGTCAGGAATGACAGGAACAAGAAAAAGAAG GAGACTTCGAAGCAAGAATGCACAGAGAGCTATGAAATGACAGCTGAGTTGGACGATCTC ACAGAGAAGATCCGAAAAGCTCACCAGGAAACTTTCCCTTCACTCTGCCAGCTGGGTAAA TACACCACGAATTCCAGTGCTGACCATCGAGTCCGACTGGACCTGGGCCTCTGGGACAAA TTCAGTGAACTGGCCACCAAGTGCATTATTAAGATCGTGGAGTTTGCTAAACGTCTGCCT GGTTTCACTGGCTTGACCATCGCAGACCAAATTACCCTGCTGAAGGCCGCCTGCCTGGAC ATCCTGATTCTTAGAATTTGCACCAGGTATACCCCAGAACAAGACACCATGACTTTCTCA GACGGCCTTACCCTAAATCGAACTCAGATGCACAATGCTGGATTTGGTCCTCTGACTGAC CTTGTGTTCACCTTTGCCAACCAGCTCCTGCCTTTGGAAATGGATGACACAGAAACAGGC CTTCTCAGTGCCATCTGCTTAATCTGTGGAGACCGCCAGGACCTTGAGGAACCGACAAAA GTAGATAAGCTACAAGAACCATTGCTGGAAGCACTAAAAATTTATATCAGAAAAAGACGA CCCAGCAAGCCTCACATGTTTCCAAAGATCTTAATGAAAATCACAGATCTCCGTAGCATC AGTGCTAAAGGTGCAGAGCGTGTAATTACCTTGAAAATGGAAATTCCTGGATCAATGCCA CCTCTCATTCAAGAAATGCTGGAGAATTCTGAAGGACATGAACCCTTGACCCCAAGTTCA AGTGGGAACACAGCAGAGCACAGTCCTAGCATCTCACCCAGCTCAGTGGAAAACAGTGGG GTCAGTCAGTCACCACTCGTGCAATAA
pfams:PF00104Hormone_recepPF00105zf-C4
go-classifiers:componentcytoplasmcomponentnucleoplasmcomponentnucleusfunctionDNA bindingfunctiondrug bindingfunctionretinoic acid receptor activityfunctionsequence-specific DNA bindingfunctionsteroid hormone receptor activityfunctionzinc ion bindingprocessembryonic digestive tract developmentprocessgene expressionprocesspositive regulation of neuron differentiationprocessregulation of myelinationprocesssignal transductionprocesstranscription initiation from RNA polymerase II promoter
id:BE0000144
name:Retinoic acid receptor gamma
organism:Humans
action:agonist
Shroot B, Michel S: Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.
Pierard GE, Pierard-Franchimont C, Paquet P, Quatresooz P: Spotlight on adapalene. Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1565-75. doi: 10.1517/17425250903386269.
Ghyselinck NB, Duester G: Retinoic acid signaling pathways. Development. 2019 Jul 4;146(13). pii: 146/13/dev167502. doi: 10.1242/dev.167502.
Kim MJ, Ciletti N, Michel S, Reichert U, Rosenfield RL: The role of specific retinoid receptors in sebocyte growth and differentiation in culture. J Invest Dermatol. 2000 Feb;114(2):349-53.
known-action:yes
name:Retinoic acid receptor gamma
general-function:Zinc ion binding
specific-function:Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence of ligand, acts mainly as an activator of gene expression due to weak binding to corepressors. Required for limb bud development. In concert with RARA or RARB, required for skeletal growth, matrix homeostasis and growth plate function (By similarity).
gene-name:RARG
locus:12q13
cellular-location:Nucleus
transmembrane-regions:
signal-regions:
theoretical-pi:7.52
molecular-weight:50341.405
chromosome-location:12
organism:Humans
external-identifiers:HUGO Gene Nomenclature Committee (HGNC)HGNC:9866GenAtlasRARGGenBank Gene DatabaseM24857GenBank Protein Database306887IUPHAR592Guide to Pharmacology592UniProtKBP13631UniProt AccessionRARG_HUMAN
synonyms:NR1B3Nuclear receptor subfamily 1 group B member 3RAR-gamma
amino-acid-sequence:>lcl|BSEQ0000287|Retinoic acid receptor gamma MATNKERLFAAGALGPGSGYPGAGFPFAFPGALRGSPPFEMLSPSFRGLGQPDLPKEMAS LSVETQSTSSEEMVPSSPSPPPPPRVYKPCFVCNDKSSGYHYGVSSCEGCKGFFRRSIQK NMVYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKEAVRNDRNKKKKEVKEEGSPDSY ELSPQLEELITKVSKAHQETFPSLCQLGKYTTNSSADHRVQLDLGLWDKFSELATKCIIK IVEFAKRLPGFTGLSIADQITLLKAACLDILMLRICTRYTPEQDTMTFSDGLTLNRTQMH NAGFGPLTDLVFAFAGQLLPLEMDDTETGLLSAICLICGDRMDLEEPEKVDKLQEPLLEA LRLYARRRRPSQPYMFPRMLMKITDLRGISTKGAERAITLKMEIPGPMPPLIREMLENPE MFEDDSSQPGPHPNASSEDEVPGGQGKGGLKSPA
gene-sequence:>lcl|BSEQ0020450|Retinoic acid receptor gamma (RARG) ATGGCCACCAATAAGGAGCGACTCTTTGCGGCTGGTGCCCTGGGGCCTGGATCTGGCTAC CCAGGGGCAGGTTTCCCCTTCGCCTTCCCAGGGGCACTCAGGGGGTCTCCGCCTTTCGAG ATGCTGAGCCCTAGCTTCCGGGGCCTGGGCCAGCCTGACCTCCCCAAGGAGATGGCCTCT CTGTCGGTGGAGACACAGAGCACCAGCTCAGAGGAGATGGTGCCCAGCTCGCCCTCGCCC CCTCCGCCTCCTCGGGTCTACAAGCCATGCTTCGTGTGCAATGACAAGTCCTCTGGCTAC CACTATGGGGTCAGCTCTTGTGAAGGCTGCAAGGGCTTCTTTCGCCGAAGCATCCAGAAG AACATGGTGTACACGTGTCACCGCGACAAAAACTGTATCATCAACAAGGTGACCAGGAAT CGCTGCCAGTACTGCCGGCTACAGAAGTGCTTCGAAGTGGGCATGTCCAAGGAAGCTGTG CGAAATGACCGGAACAAGAAGAAGAAAGAGGTGAAGGAAGAAGGGTCACCTGACAGCTAT GAGCTGAGCCCTCAGTTAGAAGAGCTCATCACCAAGGTCAGCAAAGCCCATCAGGAGACT TTCCCCTCGCTCTGCCAGCTGGGCAAGTATACCACGAACTCCAGTGCAGACCACCGCGTG CAGCTGGATCTGGGGCTGTGGGACAAGTTCAGTGAGCTGGCTACCAAGTGCATCATCAAG ATCGTGGAGTTTGCCAAGCGGTTGCCTGGCTTTACAGGGCTCAGCATTGCTGACCAGATC ACTCTGCTCAAAGCTGCCTGCCTAGATATCCTGATGCTGCGTATCTGCACAAGGTACACC CCAGAGCAGGACACCATGACCTTCTCCGACGGGCTGACCCTGAACCGGACCCAGATGCAC AATGCCGGCTTCGGGCCCCTCACAGACCTTGTCTTTGCCTTTGCTGGGCAGCTCCTGCCC CTGGAGATGGATGACACCGAGACAGGGCTGCTCAGCGCCATCTGCCTCATCTGCGGAGAC CGCATGGACCTGGAGGAGCCCGAAAAAGTGGACAAGCTGCAGGAGCCACTGCTGGAAGCC CTGAGGCTGTACGCCCGGCGCCGGCGGCCCAGCCAGCCCTACATGTTCCCAAGGATGCTA ATGAAAATCACCGACCTCCGGGGCATCAGCACTAAGGGAGCTGAAAGGGCCATTACTCTG AAGATGGAGATTCCAGGCCCGATGCCTCCCTTAATCCGAGAGATGCTGGAGAACCCTGAA ATGTTTGAGGATGACTCCTCGCAGCCTGGTCCCCACCCCAATGCCTCTAGCGAGGATGAG GTTCCTGGGGGCCAGGGCAAAGGGGGCCTGAAGTCCCCAGCCTGA
pfams:PF00104Hormone_recepPF00105zf-C4
go-classifiers:componentintegral component of membranecomponentnuclear chromatincomponentnucleoplasmcomponentnucleuscomponenttranscription factor complexfunctionDNA bindingfunctionretinoic acid receptor activityfunctionretinoid X receptor bindingfunctionRNA polymerase II regulatory region sequence-specific DNA bindingfunctionsteroid hormone receptor activityfunctiontranscription factor activity, sequence-specific DNA bindingfunctionzinc ion bindingprocessanterior/posterior pattern specificationprocesscanonical Wnt signaling pathwayprocesscellular response to retinoic acidprocessembryonic camera-type eye developmentprocessembryonic eye morphogenesisprocessembryonic hindlimb morphogenesisprocessface developmentprocessgene expressionprocessglandular epithelial cell developmentprocessgrowth plate cartilage chondrocyte growthprocessHarderian gland developmentprocessmulticellular organism growthprocessnegative regulation of apoptotic processprocessnegative regulation of cell proliferationprocessnegative regulation of chondrocyte differentiationprocessnegative regulation of transcription from RNA polymerase II promoterprocessneural tube closureprocesspositive regulation of apoptotic processprocesspositive regulation of cell proliferationprocesspositive regulation of programmed cell deathprocesspositive regulation of transcription from RNA polymerase II promoterprocessprostate gland epithelium morphogenesisprocessregulation of cell sizeprocessregulation of myelinationprocessregulation of myeloid cell differentiationprocessresponse to retinoic acidprocessretinal pigment epithelium developmentprocessretinoic acid receptor signaling pathwayprocesstrachea cartilage developmentprocesstranscription initiation from RNA polymerase II promoter
id:BE0000078
name:Retinoic acid receptor RXR-beta
organism:Humans
action:agonist
Shroot B, Michel S: Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.
Pierard GE, Pierard-Franchimont C, Paquet P, Quatresooz P: Spotlight on adapalene. Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1565-75. doi: 10.1517/17425250903386269.
Ghyselinck NB, Duester G: Retinoic acid signaling pathways. Development. 2019 Jul 4;146(13). pii: 146/13/dev167502. doi: 10.1242/dev.167502.
Kim MJ, Ciletti N, Michel S, Reichert U, Rosenfield RL: The role of specific retinoid receptors in sebocyte growth and differentiation in culture. J Invest Dermatol. 2000 Feb;114(2):349-53.
known-action:yes
name:Retinoic acid receptor RXR-beta
general-function:Zinc ion binding
specific-function:Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5 (By similarity). Specifically binds 9-cis retinoic acid (9C-RA).
gene-name:RXRB
locus:6p21.3
cellular-location:Nucleus
transmembrane-regions:
signal-regions:
theoretical-pi:8.24
molecular-weight:56921.38
chromosome-location:6
organism:Humans
external-identifiers:HUGO Gene Nomenclature Committee (HGNC)HGNC:10478GenAtlasRXRBGenBank Gene DatabaseX63522GenBank Protein Database30448IUPHAR611Guide to Pharmacology611UniProtKBP28702UniProt AccessionRXRB_HUMAN
synonyms:NR2B2Nuclear receptor subfamily 2 group B member 2Retinoid X receptor beta
amino-acid-sequence:>lcl|BSEQ0000156|Retinoic acid receptor RXR-beta MSWAARPPFLPQRHAAGQCGPVGVRKEMHCGVASRWRRRRPWLDPAAAAAAAVAGGEQQT PEPEPGEAGRDGMGDSGRDSRSPDSSSPNPLPQGVPPPSPPGPPLPPSTAPSLGGSGAPP PPPMPPPPLGSPFPVISSSMGSPGLPPPAPPGFSGPVSSPQINSTVSLPGGGSGPPEDVK PPVLGVRGLHCPPPPGGPGAGKRLCAICGDRSSGKHYGVYSCEGCKGFFKRTIRKDLTYS CRDNKDCTVDKRQRNRCQYCRYQKCLATGMKREAVQEERQRGKDKDGDGEGAGGAPEEMP VDRILEAELAVEQKSDQGVEGPGGTGGSGSSPNDPVTNICQAADKQLFTLVEWAKRIPHF SSLPLDDQVILLRAGWNELLIASFSHRSIDVRDGILLATGLHVHRNSAHSAGVGAIFDRV LTELVSKMRDMRMDKTELGCLRAIILFNPDAKGLSNPSEVEVLREKVYASLETYCKQKYP EQQGRFAKLLLRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLEAPHQLA
gene-sequence:>lcl|BSEQ0016010|Retinoic acid receptor RXR-beta (RXRB) ATGTCTTGGGCCGCTCGCCCGCCCTTCCTCCCTCAGCGGCATGCCGCAGGGCAGTGTGGG CCGGTGGGGGTGCGAAAAGAAATGCATTGTGGGGTCGCGTCCCGGTGGCGGCGGCGACGG CCCTGGCTGGATCCCGCAGCGGCGGCGGCGGCGGCGGTGGCAGGCGGAGAACAACAAACC CCGGAGCCGGAGCCAGGGGAGGCTGGACGGGACGGGATGGGCGACAGCGGGCGGGACTCC CGAAGCCCAGACAGCTCCTCCCCAAATCCCCTTCCCCAGGGAGTCCCTCCCCCTTCTCCT CCTGGGCCACCCCTACCCCCTTCAACAGCTCCATCCCTTGGAGGCTCTGGGGCCCCACCC CCACCCCCGATGCCACCACCCCCACTGGGCTCTCCCTTTCCAGTCATCAGTTCTTCCATG GGGTCCCCTGGTCTGCCCCCTCCAGCTCCCCCAGGATTCTCCGGGCCTGTCAGCAGCCCC CAGATTAACTCAACAGTGTCACTCCCTGGGGGTGGGTCTGGCCCCCCTGAAGATGTGAAG CCACCAGTCTTAGGGGTCCGGGGCCTGCACTGTCCACCCCCTCCAGGTGGCCCTGGGGCT GGCAAACGGCTATGTGCAATCTGCGGGGACAGAAGCTCAGGCAAACACTACGGGGTTTAC AGCTGTGAGGGTTGCAAGGGCTTCTTCAAACGCACCATCCGCAAAGACCTTACATACTCT TGCCGGGACAACAAAGACTGCACAGTGGACAAGCGCCAGCGGAACCGCTGTCAGTACTGC CGCTATCAGAAGTGCCTGGCCACTGGCATGAAGAGGGAGGCGGTACAGGAGGAGCGTCAG CGGGGAAAGGACAAGGATGGGGATGGGGAGGGGGCTGGGGGAGCCCCCGAGGAGATGCCT GTGGACAGGATCCTGGAGGCAGAGCTTGCTGTGGAACAGAAGAGTGACCAGGGCGTTGAG GGTCCTGGGGGAACCGGGGGTAGCGGCAGCAGCCCAAATGACCCTGTGACTAACATCTGT CAGGCAGCTGACAAACAGCTATTCACGCTTGTTGAGTGGGCGAAGAGGATCCCACACTTT TCCTCCTTGCCTCTGGATGATCAGGTCATATTGCTGCGGGCAGGCTGGAATGAACTCCTC ATTGCCTCCTTCTCACACCGATCCATTGATGTTCGAGATGGCATCCTCCTTGCCACAGGT CTTCACGTGCACCGCAACTCAGCCCATTCAGCAGGAGTAGGAGCCATCTTTGATCGGTCC CTCTCCAGGGTGCTGACAGAGCTAGTGTCCAAAATGCGTGACATGAGGATGGACAAGACA GAGCTTGGCTGCCTGAGGGCAATCATTCTGTTTAATCCAGATGCCAAGGGCCTCTCCAAC CCTAGTGAGGTGGAGGTCCTGCGGGAGAAAGTGTATGCATCACTGGAGACCTACTGCAAA CAGAAGTACCCTGAGCAGCAGGGACGGTTTGCCAAGCTGCTGCTACGTCTTCCTGCCCTC CGGTCCATTGGCCTTAAGTGTCTAGAGCATCTGTTTTTCTTCAAGCTCATTGGTGACACC CCCATCGACACCTTCCTCATGGAGATGCTTGAGGCTCCCCATCAACTGGCCTGA
pfams:PF00104Hormone_recepPF00105zf-C4
go-classifiers:componentnucleoplasmcomponentnucleusfunction9-cis retinoic acid receptor activityfunctionRNA polymerase II distal enhancer sequence-specific DNA bindingfunctionRNA polymerase II regulatory region sequence-specific DNA bindingfunctionRNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA bindingfunctionsteroid hormone receptor activityfunctiontranscription coactivator activityfunctiontranscription factor activity, sequence-specific DNA bindingfunctiontranscriptional activator activity, RNA polymerase II transcription regulatory region sequence-specific bindingfunctionzinc ion bindingprocesscardiac muscle cell proliferationprocessgene expressionprocessin utero embryonic developmentprocessmaternal placenta developmentprocesspositive regulation of transcription from RNA polymerase II promoterprocesstranscription initiation from RNA polymerase II promoterprocessventricular cardiac muscle cell differentiation
id:BE0000707
name:Retinoic acid receptor RXR-gamma
organism:Humans
action:agonist
Shroot B, Michel S: Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.
Pierard GE, Pierard-Franchimont C, Paquet P, Quatresooz P: Spotlight on adapalene. Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1565-75. doi: 10.1517/17425250903386269.
Ghyselinck NB, Duester G: Retinoic acid signaling pathways. Development. 2019 Jul 4;146(13). pii: 146/13/dev167502. doi: 10.1242/dev.167502.
Kim MJ, Ciletti N, Michel S, Reichert U, Rosenfield RL: The role of specific retinoid receptors in sebocyte growth and differentiation in culture. J Invest Dermatol. 2000 Feb;114(2):349-53.
known-action:yes
name:Retinoic acid receptor RXR-gamma
general-function:Zinc ion binding
specific-function:Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. The high affinity ligand for RXRs is 9-cis retinoic acid (By similarity).
gene-name:RXRG
locus:1q22-q23
cellular-location:Nucleus
transmembrane-regions:
signal-regions:
theoretical-pi:7.67
molecular-weight:50870.72
chromosome-location:
organism:Humans
external-identifiers:HUGO Gene Nomenclature Committee (HGNC)HGNC:10479GenAtlasRXRGGenBank Gene DatabaseU38480GenBank Protein Database1053069IUPHAR612Guide to Pharmacology612UniProtKBP48443UniProt AccessionRXRG_HUMAN
synonyms:NR2B3Nuclear receptor subfamily 2 group B member 3Retinoid X receptor gamma
amino-acid-sequence:>lcl|BSEQ0016185|Retinoic acid receptor RXR-gamma MYGNYSHFMKFPAGYGGSPGHTGSTSMSPSAALSTGKPMDSHPSYTDTPVSAPRTLSAVG TPLNALGSPYRVITSAMGPPSGALAAPPGINLVAPPSSQLNVVNSVSSSEDIKPLPGLPG IGNMNYPSTSPGSLVKHICAICGDRSSGKHYGVYSCEGCKGFFKRTIRKDLIYTCRDNKD CLIDKRQRNRCQYCRYQKCLVMGMKREAVQEERQRSRERAESEAECATSGHEDMPVERIL EAELAVEPKTESYGDMNMENSTNDPVTNICHAADKQLFTLVEWAKRIPHFSDLTLEDQVI LLRAGWNELLIASFSHRSVSVQDGILLATGLHVHRSSAHSAGVGSIFDRVLTELVSKMKD MQMDKSELGCLRAIVLFNPDAKGLSNPSEVETLREKVYATLEAYTKQKYPEQPGRFAKLL LRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLETPLQIT
gene-sequence:>lcl|BSEQ0001409|1392 bp ATGTATGGAAATTATTCTCACTTCATGAAGTTTCCCGCAGGCTATGGAGGCTCCCCTGGC CACACTGGCTCTACATCCATGAGCCCATCAGCAGCCTTGTCCACAGGGAAGCCAATGGAC AGCCACCCCAGCTACACAGATACCCCAGTGAGTGCCCCACGGACTCTGAGTGCAGTGGGG ACCCCCCTCAATGCCCTGGGCTCTCCATATCGAGTCATCACCTCTGCCATGGGCCCACCC TCAGGAGCACTTGCAGCGCCTCCAGGAATCAACTTGGTTGCCCCACCCAGCTCTCAGCTA AATGTGGTCAACAGTGTCAGCAGTTCAGAGGACATCAAGCCCTTACCAGGGCTTCCCGGG ATTGGAAACATGAACTACCCATCCACCAGCCCCGGATCTCTGGTTAAACACATCTGTGCT ATCTGTGGAGACAGATCCTCAGGAAAGCACTACGGGGTATACAGTTGTGAAGGCTGCAAA GGGTTCTTCAAGAGGACGATAAGGAAGGACCTCATCTACACGTGTCGGGATAATAAAGAC TGCCTCATTGACAAGCGTCAGCGCAACCGCTGCCAGTACTGTCGCTATCAGAAGTGCCTT GTCATGGGCATGAAGAGGGAAGCTGTGCAAGAAGAAAGACAGAGGAGCCGAGAGCGAGCT GAGAGTGAGGCAGAATGTGCTACCAGTGGTCATGAAGACATGCCTGTGGAGAGGATTCTA GAAGCTGAACTTGCTGTTGAACCAAAGACAGAATCCTATGGTGACATGAATATGGAGAAC TCGACAAATGACCCTGTTACCAACATATGTCATGCTGCTGACAAGCAGCTTTTCACCCTC GTTGAATGGGCCAAGCGTATTCCCCACTTCTCTGACCTCACCTTGGAGGACCAGGTCATT TTGCTTCGGGCAGGGTGGAATGAATTGCTGATTGCCTCTTTCTCCCACCGCTCAGTTTCC GTGCAGGATGGCATCCTTCTGGCCACGGGTTTACATGTCCACCGGAGCAGTGCCCACAGT GCTGGGGTCGGCTCCATCTTTGACAGAGTTCTAACTGAGCTGGTTTCCAAAATGAAAGAC ATGCAGATGGACAAGTCGGAACTGGGATGCCTGCGAGCCATTGTACTCTTTAACCCAGAT GCCAAGGGCCTGTCCAACCCCTCTGAGGTGGAGACTCTGCGAGAGAAGGTTTATGCCACC CTTGAGGCCTACACCAAGCAGAAGTATCCGGAACAGCCAGGCAGGTTTGCCAAGCTGCTG CTGCGCCTCCCAGCTCTGCGTTCCATTGGCTTGAAATGCCTGGAGCACCTCTTCTTCTTC AAGCTCATCGGGGACACCCCCATTGACACCTTCCTCATGGAGATGTTGGAGACCCCGCTG CAGATCACCTGA
pfams:PF00104Hormone_recepPF00105zf-C4PF11825Nuc_recep-AF1
go-classifiers:componentnucleoplasmfunction9-cis retinoic acid receptor activityfunctionRNA polymerase II regulatory region sequence-specific DNA bindingfunctionsteroid hormone receptor activityfunctionzinc ion bindingprocessgene expressionprocesspositive regulation of transcription from RNA polymerase II promoter involved in cellular response to chemical stimulusprocessprotein homotetramerizationprocesstranscription initiation from RNA polymerase II promoter
id:BE0000412
name:Retinoic acid receptor RXR-alpha
organism:Humans
action:agonist
Shroot B, Michel S: Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.
Pierard GE, Pierard-Franchimont C, Paquet P, Quatresooz P: Spotlight on adapalene. Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1565-75. doi: 10.1517/17425250903386269.
Ghyselinck NB, Duester G: Retinoic acid signaling pathways. Development. 2019 Jul 4;146(13). pii: 146/13/dev167502. doi: 10.1242/dev.167502.
Kim MJ, Ciletti N, Michel S, Reichert U, Rosenfield RL: The role of specific retinoid receptors in sebocyte growth and differentiation in culture. J Invest Dermatol. 2000 Feb;114(2):349-53.
known-action:yes
name:Retinoic acid receptor RXR-alpha
general-function:Zinc ion binding
specific-function:Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RAR/RXR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. The high affinity ligand for RXRs is 9-cis retinoic acid. RXRA serves as a common heterodimeric partner for a number of nuclear receptors. The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone acetylation, chromatin condensation and transcriptional suppression. On ligand binding, the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation. The RXRA/PPARA heterodimer is required for PPARA transcriptional activity on fatty acid oxidation genes such as ACOX1 and the P450 system genes.
gene-name:RXRA
locus:9q34.3
cellular-location:Nucleus
transmembrane-regions:
signal-regions:
theoretical-pi:7.86
molecular-weight:50810.835
chromosome-location:
organism:Humans
external-identifiers:HUGO Gene Nomenclature Committee (HGNC)HGNC:10477GenAtlasRXRAGenBank Gene DatabaseX52773GenBank Protein Database35885IUPHAR610Guide to Pharmacology610UniProtKBP19793UniProt AccessionRXRA_HUMAN
synonyms:NR2B1Nuclear receptor subfamily 2 group B member 1Retinoid X receptor alpha
amino-acid-sequence:>lcl|BSEQ0000821|Retinoic acid receptor RXR-alpha MDTKHFLPLDFSTQVNSSLTSPTGRGSMAAPSLHPSLGPGIGSPGQLHSPISTLSSPING MGPPFSVISSPMGPHSMSVPTTPTLGFSTGSPQLSSPMNPVSSSEDIKPPLGLNGVLKVP AHPSGNMASFTKHICAICGDRSSGKHYGVYSCEGCKGFFKRTVRKDLTYTCRDNKDCLID KRQRNRCQYCRYQKCLAMGMKREAVQEERQRGKDRNENEVESTSSANEDMPVERILEAEL AVEPKTETYVEANMGLNPSSPNDPVTNICQAADKQLFTLVEWAKRIPHFSELPLDDQVIL LRAGWNELLIASFSHRSIAVKDGILLATGLHVHRNSAHSAGVGAIFDRVLTELVSKMRDM QMDKTELGCLRAIVLFNPDSKGLSNPAEVEALREKVYASLEAYCKHKYPEQPGRFAKLLL RLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLEAPHQMT
gene-sequence:>lcl|BSEQ0000820|1389 bp ATGGACACCAAACATTTCCTGCCGCTCGATTTCTCCACCCAGGTGAACTCCTCCCTCACC TCCCCGACGGGGCGAGGCTCCATGGCTGCCCCCTCGCTGCACCCGTCCCTGGGGCCTGGC ATCGGCTCCCCGGGACAGCTGCATTCTCCCATCAGCACCCTGAGCTCCCCCATCAACGGC ATGGGCCCGCCTTTCTCGGTCATCAGCTCCCCCATGGGCCCCCACTCCATGTCGGTGCCC ACCACACCCACCCTGGGCTTCAGCACTGGCAGCCCCCAGCTCAGCTCACCTATGAACCCC GTCAGCAGCAGCGAGGACATCAAGCCCCCCCTGGGCCTCAATGGCGTCCTCAAGGTCCCC GCCCACCCCTCAGGAAACATGGCTTCCTTCACCAAGCACATCTGCGCCATCTGCGGGGAC CGCTCCTCAGGCAAGCACTATGGAGTGTACAGCTGCGAGGGGTGCAAGGGCTTCTTCAAG CGGACGGTGCGCAAGGACCTGACCTACACCTGCCGCGACAACAAGGACTGCCTGATTGAC AAGCGGCAGCGGAACCGGTGCCAGTACTGCCGCTACCAGAAGTGCCTGGCCATGGGCATG AAGCGGGAAGCCGTGCAGGAGGAGCGGCAGCGTGGCAAGGACCGGAACGAGAATGAGGTG GAGTCGACCAGCAGCGCCAACGAGGACATGCCGGTGGAGAGGATCCTGGAGGCTGAGCTG GCCGTGGAGCCCAAGACCGAGACCTACGTGGAGGCAAACATGGGGCTGAACCCCAGCTCG CCGAACGACCCTGTCACCAACATTTGCCAAGCAGCCGACAAACAGCTTTTCACCCTGGTG GAGTGGGCCAAGCGGATCCCACACTTCTCAGAGCTGCCCCTGGACGACCAGGTCATCCTG CTGCGGGCAGGCTGGAATGAGCTGCTCATCGCCTCCTTCTCCCACCGCTCCATCGCCGTG AAGGACGGGATCCTCCTGGCCACCGGGCTGCACGTCCACCGGAACAGCGCCCACAGCGCA GGGGTGGGCGCCATCTTTGACAGGGTGCTGACGGAGCTTGTGTCCAAGATGCGGGACATG CAGATGGACAAGACGGAGCTGGGCTGCCTGCGCGCCATCGTCCTCTTTAACCCTGACTCC AAGGGGCTCTCGAACCCGGCCGAGGTGGAGGCGCTGAGGGAGAAGGTCTATGCGTCCTTG GAGGCCTACTGCAAGCACAAGTACCCAGAGCAGCCGGGAAGGTTCGCTAAGCTCTTGCTC CGCCTGCCGGCTCTGCGCTCCATCGGGCTCAAATGCCTGGAACATCTCTTCTTCTTCAAG CTCATCGGGGACACACCCATTGACACCTTCCTTATGGAGATGCTGGAGGCGCCGCACCAA ATGACTTAG
pfams:PF00104Hormone_recepPF00105zf-C4PF11825Nuc_recep-AF1
go-classifiers:componentaxoncomponentnuclear chromatincomponentnucleoplasmcomponentnucleuscomponentreceptor complexcomponentRNA polymerase II transcription factor complexfunction9-cis retinoic acid receptor activityfunctionchromatin DNA bindingfunctionDNA bindingfunctionenzyme bindingfunctionprotein heterodimerization activityfunctionretinoic acid receptor activityfunctionretinoic acid-responsive element bindingfunctionRNA polymerase II regulatory region sequence-specific DNA bindingfunctionRNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA bindingfunctionsequence-specific DNA bindingfunctionsteroid hormone receptor activityfunctiontranscription coactivator activityfunctiontranscription factor activity, sequence-specific DNA bindingfunctionvitamin D receptor bindingfunctionzinc ion bindingprocessagingprocessaxon regenerationprocessbile acid and bile salt transportprocessbile acid metabolic processprocesscamera-type eye developmentprocesscellular lipid metabolic processprocesscellular response to insulin stimulusprocesscholesterol metabolic processprocessembryo implantationprocessgene expressionprocessin utero embryonic developmentprocessinflammatory responseprocessliver developmentprocessmaternal placenta developmentprocessmidgut developmentprocessmodulation by virus of host morphology or physiologyprocessnegative regulation of cell proliferationprocessnegative regulation of transcription from RNA polymerase II promoterprocessperoxisome proliferator activated receptor signaling pathwayprocesspositive regulation of apoptotic processprocesspositive regulation of transcription from RNA polymerase II promoterprocesspositive regulation of transcription from RNA polymerase II promoter involved in cellular response to chemical stimulusprocesspositive regulation of translational initiation by ironprocessprotein homotetramerizationprocessregulation of branching involved in prostate gland morphogenesisprocessregulation of myelinationprocessresponse to ethanolprocessresponse to glucocorticoidprocessresponse to retinoic acidprocessresponse to selenium ionprocessresponse to vitamin Aprocessresponse to vitamin Dprocessretinoic acid receptor signaling pathwayprocesssecretory columnal luminar epithelial cell differentiation involved in prostate glandular acinus developmentprocesssmall molecule metabolic processprocesstranscription initiation from RNA polymerase II promoterprocessventricular cardiac muscle cell differentiationprocessventricular cardiac muscle tissue morphogenesisprocessvitamin metabolic process
id:BE0001040
name:Transcription factor AP-1
organism:Humans
action:antagonist
Leyden J: Recent advances in the use of adapalene 0.1%/benzoyl peroxide 2.5% to treat patients with moderate to severe acne. J Dermatolog Treat. 2016;27 Suppl 1:S4-13. doi: 10.3109/09546634.2016.1145338.
Lefebvre P, Martin PJ, Flajollet S, Dedieu S, Billaut X, Lefebvre B: Transcriptional activities of retinoic acid receptors. Vitam Horm. 2005;70:199-264. doi: 10.1016/S0083-6729(05)70007-8.
known-action:yes
name:Transcription factor AP-1
general-function:Transcriptional activator activity, rna polymerase ii transcription factor binding
specific-function:Transcription factor that recognizes and binds to the enhancer heptamer motif 5'-TGA[CG]TCA-3'. Promotes activity of NR5A1 when phosphorylated by HIPK3 leading to increased steroidogenic gene expression upon cAMP signaling pathway stimulation.
gene-name:JUN
locus:1p32-p31
cellular-location:Nucleus
transmembrane-regions:
signal-regions:
theoretical-pi:9.11
molecular-weight:35675.32
chromosome-location:1
organism:Humans
external-identifiers:HUGO Gene Nomenclature Committee (HGNC)HGNC:6204GenAtlasJUNGenBank Gene DatabaseJ04111GenBank Protein Database386839UniProtKBP05412UniProt AccessionJUN_HUMAN
synonyms:Activator protein 1AP1p39Proto-oncogene c-JunV-jun avian sarcoma virus 17 oncogene homolog
amino-acid-sequence:>lcl|BSEQ0016292|Transcription factor AP-1 MTAKMETTFYDDALNASFLPSESGPYGYSNPKILKQSMTLNLADPVGSLKPHLRAKNSDL LTSPDVGLLKLASPELERLIIQSSNGHITTTPTPTQFLCPKNVTDEQEGFAEGFVRALAE LHSQNTLPSVTSAAQPVNGAGMVAPAVASVAGGSGSGGFSASLHSEPPVYANLSNFNPGA LSSGGGAPSYGAAGLAFPAQPQQQQQPPHHLPQQMPVQHPRLQALKEEPQTVPEMPGETP PLSPIDMESQERIKAERKRMRNRIAASKCRKRKLERIARLEEKVKTLKAQNSELASTANM LREQVAQLKQKVMNHVNSGCQLMLTQQLQTF
gene-sequence:>lcl|BSEQ0016293|Transcription factor AP-1 (JUN) ATGACTGCAAAGATGGAAACGACCTTCTATGACGATGCCCTCAACGCCTCGTTCCTCCCG TCCGAGAGCGGACCTTATGGCTACAGTAACCCCAAGATCCTGAAACAGAGCATGACCCTG AACCTGGCCGACCCAGTGGGGAGCCTGAAGCCGCACCTCCGCGCCAAGAACTCGGACCTC CTCACCTCGCCCGACGTGGGGCTGCTCAAGCTGGCGTCGCCCGAGCTGGAGCGCCTGATA ATCCAGTCCAGCAACGGGCACATCACCACCACGCCGACCCCCACCCAGTTCCTGTGCCCC AAGAACGTGACAGATGAGCAGGAGGGCTTCGCCGAGGGCTTCGTGCGCGCCCTGGCCGAA CTGCACAGCCAGAACACGCTGCCCAGCGTCACGTCGGCGGCGCAGCCGGTCAACGGGGCA GGCATGGTGGCTCCCGCGGTAGCCTCGGTGGCAGGGGGCAGCGGCAGCGGCGGCTTCAGC GCCAGCCTGCACAGCGAGCCGCCGGTCTACGCAAACCTCAGCAACTTCAACCCAGGCGCG CTGAGCAGCGGCGGCGGGGCGCCCTCCTACGGCGCGGCCGGCCTGGCCTTTCCCGCGCAA CCCCAGCAGCAGCAGCAGCCGCCGCACCACCTGCCCCAGCAGATGCCCGTGCAGCACCCG CGGCTGCAGGCCCTGAAGGAGGAGCCTCAGACAGTGCCCGAGATGCCCGGCGAGACACCG CCCCTGTCCCCCATCGACATGGAGTCCCAGGAGCGGATCAAGGCGGAGAGGAAGCGCATG AGGAACCGCATCGCTGCCTCCAAGTGCCGAAAAAGGAAGCTGGAGAGAATCGCCCGGCTG GAGGAAAAAGTGAAAACCTTGAAAGCTCAGAACTCGGAGCTGGCGTCCACGGCCAACATG CTCAGGGAACAGGTGGCACAGCTTAAACAGAAAGTCATGAACCACGTTAACAGTGGGTGC CAACTCATGCTAACGCAGCAGTTGCAAACATTTTGA
pfams:PF00170bZIP_1PF03957Jun
go-classifiers:componentcytosolcomponentnuclear chromosomecomponentnuclear euchromatincomponentnucleoplasmcomponentnucleuscomponenttranscription factor complexcomponenttranscriptional repressor complexfunctioncAMP response element bindingfunctionchromatin bindingfunctionDNA bindingfunctionenzyme bindingfunctionGTPase activator activityfunctionpoly(A) RNA bindingfunctionR-SMAD bindingfunctionRNA polymerase II activating transcription factor bindingfunctionRNA polymerase II core promoter proximal region sequence-specific DNA bindingfunctionRNA polymerase II distal enhancer sequence-specific DNA bindingfunctionRNA polymerase II transcription factor activity, sequence-specific DNA bindingfunctiontranscription coactivator activityfunctiontranscription factor activity, RNA polymerase II distal enhancer sequence-specific bindingfunctiontranscription factor activity, sequence-specific DNA bindingfunctiontranscription factor bindingfunctiontranscription regulatory region DNA bindingfunctiontranscriptional activator activity, RNA polymerase II core promoter proximal region sequence-specific bindingfunctiontranscriptional activator activity, RNA polymerase II transcription factor bindingprocessagingprocessangiogenesisprocessaxon regenerationprocesscellular response to calcium ionprocesscellular response to hormone stimulusprocesscellular response to potassium ion starvationprocesscircadian rhythmprocessFc-epsilon receptor signaling pathwayprocessinnate immune responseprocessleading edge cell differentiationprocesslearningprocessliver developmentprocessmembrane depolarizationprocessmicroglial cell activationprocessmonocyte differentiationprocessMyD88-dependent toll-like receptor signaling pathwayprocessMyD88-independent toll-like receptor signaling pathwayprocessnegative regulation by host of viral transcriptionprocessnegative regulation of cell proliferationprocessnegative regulation of DNA bindingprocessnegative regulation of neuron apoptotic processprocessnegative regulation of protein autophosphorylationprocessnegative regulation of transcription from RNA polymerase II promoter in response to endoplasmic reticulum stressprocessnegative regulation of transcription, DNA-templatedprocessoutflow tract morphogenesisprocesspositive regulation by host of viral transcriptionprocesspositive regulation of cell differentiationprocesspositive regulation of DNA replicationprocesspositive regulation of DNA-templated transcription, initiationprocesspositive regulation of endothelial cell proliferationprocesspositive regulation of fibroblast proliferationprocesspositive regulation of GTPase activityprocesspositive regulation of monocyte differentiationprocesspositive regulation of neuron apoptotic processprocesspositive regulation of pri-miRNA transcription from RNA polymerase II promoterprocesspositive regulation of smooth muscle cell proliferationprocesspositive regulation of transcription from RNA polymerase II promoterprocesspositive regulation of transcription, DNA-templatedprocessregulation of cell cycleprocessregulation of cell deathprocessregulation of cell proliferationprocessregulation of sequence-specific DNA binding transcription factor activityprocessrelease of cytochrome c from mitochondriaprocessresponse to cAMPprocessresponse to cytokineprocessresponse to drugprocessresponse to hydrogen peroxideprocessresponse to lipopolysaccharideprocessresponse to mechanical stimulusprocessresponse to muscle stretchprocessresponse to radiationprocessSMAD protein import into nucleusprocessSMAD protein signal transductionprocessstress-activated MAPK cascadeprocesstoll-like receptor 10 signaling pathwayprocesstoll-like receptor 2 signaling pathwayprocesstoll-like receptor 3 signaling pathwayprocesstoll-like receptor 4 signaling pathwayprocesstoll-like receptor 5 signaling pathwayprocesstoll-like receptor 9 signaling pathwayprocesstoll-like receptor signaling pathwayprocesstoll-like receptor TLR1processtoll-like receptor TLR6processtransforming growth factor beta receptor signaling pathwayprocessTRIF-dependent toll-like receptor signaling pathway
id:BE0001164
name:Toll-like receptor 2
organism:Humans
action:antagonist
Tenaud I, Khammari A, Dreno B: In vitro modulation of TLR-2, CD1d and IL-10 by adapalene on normal human skin and acne inflammatory lesions. Exp Dermatol. 2007 Jun;16(6):500-6. doi: 10.1111/j.1600-0625.2007.00552.x.
Leyden J: Recent advances in the use of adapalene 0.1%/benzoyl peroxide 2.5% to treat patients with moderate to severe acne. J Dermatolog Treat. 2016;27 Suppl 1:S4-13. doi: 10.3109/09546634.2016.1145338.
known-action:yes
name:Toll-like receptor 2
general-function:Triacyl lipopeptide binding
specific-function:Cooperates with LY96 to mediate the innate immune response to bacterial lipoproteins and other microbial cell wall components. Cooperates with TLR1 or TLR6 to mediate the innate immune response to bacterial lipoproteins or lipopeptides (PubMed:17889651). Acts via MYD88 and TRAF6, leading to NF-kappa-B activation, cytokine secretion and the inflammatory response. May also promote apoptosis in response to lipoproteins (PubMed:10426996). Recognizes mycoplasmal macrophage-activating lipopeptide-2kD (MALP-2), soluble tuberculosis factor (STF), phenol-soluble modulin (PSM) and B.burgdorferi outer surface protein A lipoprotein (OspA-L) cooperatively with TLR6 (PubMed:11441107). Acts as a receptor for M.tuberculosis lipoproteins LprA, LprG, LpqH and PhoS1 (pstS1), some lipoproteins are dependent on other coreceptors (TLR1, CD14 and/or CD36).The lipoproteins act as agonists to modulate antigen presenting cell functions in response to the pathogen (PubMed:19362712). Forms activation clusters composed of several receptors depending on the ligand, these clusters trigger signaling from the cell surface and subsequently are targeted to the Golgi in a lipid-raft dependent pathway. Forms the cluster TLR2:TLR6:CD14:CD36 in response to diacylated lipopeptides and TLR2:TLR1:CD14 in response to triacylated lipopeptides (PubMed:16880211).
gene-name:TLR2
locus:4q32
cellular-location:Membrane
transmembrane-regions:589-609
signal-regions:1-18
theoretical-pi:6.59
molecular-weight:89836.575
chromosome-location:4
organism:Humans
external-identifiers:HUGO Gene Nomenclature Committee (HGNC)HGNC:11848GenAtlasTLR2GenBank Gene DatabaseAF051152GenBank Protein Database3132528UniProtKBO60603UniProt AccessionTLR2_HUMAN
synonyms:TIL4Toll/interleukin-1 receptor-like protein 4
amino-acid-sequence:>lcl|BSEQ0010812|Toll-like receptor 2 MPHTLWMVWVLGVIISLSKEESSNQASLSCDRNGICKGSSGSLNSIPSGLTEAVKSLDLS NNRITYISNSDLQRCVNLQALVLTSNGINTIEEDSFSSLGSLEHLDLSYNYLSNLSSSWF KPLSSLTFLNLLGNPYKTLGETSLFSHLTKLQILRVGNMDTFTKIQRKDFAGLTFLEELE IDASDLQSYEPKSLKSIQNVSHLILHMKQHILLLEIFVDVTSSVECLELRDTDLDTFHFS ELSTGETNSLIKKFTFRNVKITDESLFQVMKLLNQISGLLELEFDDCTLNGVGNFRASDN DRVIDPGKVETLTIRRLHIPRFYLFYDLSTLYSLTERVKRITVENSKVFLVPCLLSQHLK SLEYLDLSENLMVEEYLKNSACEDAWPSLQTLILRQNHLASLEKTGETLLTLKNLTNIDI SKNSFHSMPETCQWPEKMKYLNLSSTRIHSVTGCIPKTLEILDVSNNNLNLFSLNLPQLK ELYISRNKLMTLPDASLLPMLLVLKISRNAITTFSKEQLDSFHTLKTLEAGGNNFICSCE FLSFTQEQQALAKVLIDWPANYLCDSPSHVRGQQVQDVRLSVSECHRTALVSGMCCALFL LILLTGVLCHRFHGLWYMKMMWAWLQAKRKPRKAPSRNICYDAFVSYSERDAYWVENLMV QELENFNPPFKLCLHKRDFIPGKWIIDNIIDSIEKSHKTVFVLSENFVKSEWCKYELDFS HFRLFDENNDAAILILLEPIEKKAIPQRFCKLRKIMNTKTYLEWPMDEAQREGFWVNLRA AIKS
gene-sequence:>lcl|BSEQ0010813|Toll-like receptor 2 (TLR2) ATGCCACATACTTTGTGGATGGTGTGGGTCTTGGGGGTCATCATCAGCCTCTCCAAGGAA GAATCCTCCAATCAGGCTTCTCTGTCTTGTGACCGCAATGGTATCTGCAAGGGCAGCTCA GGATCTTTAAACTCCATTCCCTCAGGGCTCACAGAAGCTGTAAAAAGCCTTGACCTGTCC AACAACAGGATCACCTACATTAGCAACAGTGACCTACAGAGGTGTGTGAACCTCCAGGCT CTGGTGCTGACATCCAATGGAATTAACACAATAGAGGAAGATTCTTTTTCTTCCCTGGGC AGTCTTGAACATTTAGACTTATCCTATAATTACTTATCTAATTTATCGTCTTCCTGGTTC AAGCCCCTTTCTTCTTTAACATTCTTAAACTTACTGGGAAATCCTTACAAAACCCTAGGG GAAACATCTCTTTTTTCTCATCTCACAAAATTGCAAATCCTGAGAGTGGGAAATATGGAC ACCTTCACTAAGATTCAAAGAAAAGATTTTGCTGGACTTACCTTCCTTGAGGAACTTGAG ATTGATGCTTCAGATCTACAGAGCTATGAGCCAAAAAGTTTGAAGTCAATTCAGAATGTA AGTCATCTGATCCTTCATATGAAGCAGCATATTTTACTGCTGGAGATTTTTGTAGATGTT ACAAGTTCCGTGGAATGTTTGGAACTGCGAGATACTGATTTGGACACTTTCCATTTTTCA GAACTATCCACTGGTGAAACAAATTCATTGATTAAAAAGTTTACATTTAGAAATGTGAAA ATCACCGATGAAAGTTTGTTTCAGGTTATGAAACTTTTGAATCAGATTTCTGGATTGTTA GAATTAGAGTTTGATGACTGTACCCTTAATGGAGTTGGTAATTTTAGAGCATCTGATAAT GACAGAGTTATAGATCCAGGTAAAGTGGAAACGTTAACAATCCGGAGGCTGCATATTCCA AGGTTTTACTTATTTTATGATCTGAGCACTTTATATTCACTTACAGAAAGAGTTAAAAGA ATCACAGTAGAAAACAGTAAAGTTTTTCTGGTTCCTTGTTTACTTTCACAACATTTAAAA TCATTAGAATACTTGGATCTCAGTGAAAATTTGATGGTTGAAGAATACTTGAAAAATTCA GCCTGTGAGGATGCCTGGCCCTCTCTACAAACTTTAATTTTAAGGCAAAATCATTTGGCA TCATTGGAAAAAACCGGAGAGACTTTGCTCACTCTGAAAAACTTGACTAACATTGATATC AGTAAGAATAGTTTTCATTCTATGCCTGAAACTTGTCAGTGGCCAGAAAAGATGAAATAT TTGAACTTATCCAGCACACGAATACACAGTGTAACAGGCTGCATTCCCAAGACACTGGAA ATTTTAGATGTTAGCAACAACAATCTCAATTTATTTTCTTTGAATTTGCCGCAACTCAAA GAACTTTATATTTCCAGAAATAAGTTGATGACTCTACCAGATGCCTCCCTCTTACCCATG TTACTAGTATTGAAAATCAGTAGGAATGCAATAACTACGTTTTCTAAGGAGCAACTTGAC TCATTTCACACACTGAAGACTTTGGAAGCTGGTGGCAATAACTTCATTTGCTCCTGTGAA TTCCTCTCCTTCACTCAGGAGCAGCAAGCACTGGCCAAAGTCTTGATTGATTGGCCAGCA AATTACCTGTGTGACTCTCCATCCCATGTGCGTGGCCAGCAGGTTCAGGATGTCCGCCTC TCGGTGTCGGAATGTCACAGGACAGCACTGGTGTCTGGCATGTGCTGTGCTCTGTTCCTG CTGATCCTGCTCACGGGGGTCCTGTGCCACCGTTTCCATGGCCTGTGGTATATGAAAATG ATGTGGGCCTGGCTCCAGGCCAAAAGGAAGCCCAGGAAAGCTCCCAGCAGGAACATCTGC TATGATGCATTTGTTTCTTACAGTGAGCGGGATGCCTACTGGGTGGAGAACCTTATGGTC CAGGAGCTGGAGAACTTCAATCCCCCCTTCAAGTTGTGTCTTCATAAGCGGGACTTCATT CCTGGCAAGTGGATCATTGACAATATCATTGACTCCATTGAAAAGAGCCACAAAACTGTC TTTGTGCTTTCTGAAAACTTTGTGAAGAGTGAGTGGTGCAAGTATGAACTGGACTTCTCC CATTTCCGTCTTTTTGATGAGAACAATGATGCTGCCATTCTCATTCTTCTGGAGCCCATT GAGAAAAAAGCCATTCCCCAGCGCTTCTGCAAGCTGCGGAAGATAATGAACACCAAGACC TACCTGGAGTGGCCCATGGACGAGGCTCAGCGGGAAGGATTTTGGGTAAATCTGAGAGCT GCGATAAAGTCCTAG
pfams:PF01463LRRCTPF01582TIRPF13855LRR_8
go-classifiers:componentcell surfacecomponentcytoplasmcomponentexternal side of plasma membranecomponentGolgi apparatuscomponentintegral component of plasma membranecomponentintrinsic component of plasma membranecomponentmembrane raftcomponentplasma membranecomponentToll-like receptor 1-Toll-like receptor 2 protein complexcomponentToll-like receptor 2-Toll-like receptor 6 protein complexfunctiondiacyl lipopeptide bindingfunctionlipopolysaccharide bindingfunctionlipopolysaccharide receptor activityfunctionlipoteichoic acid bindingfunctionpeptidoglycan bindingfunctionprotein heterodimerization activityfunctionreceptor activityfunctionsignaling pattern recognition receptor activityfunctionToll-like receptor bindingfunctiontransmembrane signaling receptor activityfunctiontriacyl lipopeptide bindingprocessapoptotic processprocesscell surface pattern recognition receptor signaling pathwayprocesscellular response to bacterial lipopeptideprocesscellular response to diacyl bacterial lipopeptideprocesscellular response to lipoteichoic acidprocesscellular response to peptidoglycanprocesscellular response to triacyl bacterial lipopeptideprocesschloramphenicol transportprocesscytokine secretion involved in immune responseprocessdefense response to Gram-positive bacteriumprocessdetection of diacyl bacterial lipopeptideprocessdetection of triacyl bacterial lipopeptideprocessI-kappaB phosphorylationprocessimmune responseprocessinduction by symbiont of defense-related host nitric oxide productionprocessinflammatory responseprocessinnate immune responseprocessinterleukin-10 productionprocesslipopolysaccharide-mediated signaling pathwayprocessMyD88-dependent toll-like receptor signaling pathwayprocessnegative regulation of growth of symbiont in hostprocessnegative regulation of interleukin-12 productionprocessnegative regulation of interleukin-17 productionprocesspositive regulation of chemokine productionprocesspositive regulation of cytokine secretionprocesspositive regulation of gene expressionprocesspositive regulation of inflammatory responseprocesspositive regulation of interferon-beta productionprocesspositive regulation of interleukin-12 productionprocesspositive regulation of interleukin-18 productionprocesspositive regulation of interleukin-6 productionprocesspositive regulation of interleukin-8 productionprocesspositive regulation of leukocyte migrationprocesspositive regulation of macrophage cytokine productionprocesspositive regulation of NF-kappaB import into nucleusprocesspositive regulation of NF-kappaB transcription factor activityprocesspositive regulation of nitric oxide biosynthetic processprocesspositive regulation of nitric-oxide synthase biosynthetic processprocesspositive regulation of toll-like receptor signaling pathwayprocesspositive regulation of transcription from RNA polymerase II promoterprocesspositive regulation of tumor necrosis factor biosynthetic processprocesspositive regulation of tumor necrosis factor productionprocesspositive regulation of Wnt signaling pathwayprocessregulation of dendritic cell cytokine productionprocessresponse to molecule of fungal originprocesssignal transductionprocesstoll-like receptor 2 signaling pathwayprocesstoll-like receptor 4 signaling pathwayprocesstoll-like receptor signaling pathwayprocesstoll-like receptor TLR1processtoll-like receptor TLR6
id:BE0000663
name:Retinoic acid receptor alpha
organism:Humans
Shroot B, Michel S: Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.
Pierard GE, Pierard-Franchimont C, Paquet P, Quatresooz P: Spotlight on adapalene. Expert Opin Drug Metab Toxicol. 2009 Dec;5(12):1565-75. doi: 10.1517/17425250903386269.
Ghyselinck NB, Duester G: Retinoic acid signaling pathways. Development. 2019 Jul 4;146(13). pii: 146/13/dev167502. doi: 10.1242/dev.167502.
Kim MJ, Ciletti N, Michel S, Reichert U, Rosenfield RL: The role of specific retinoid receptors in sebocyte growth and differentiation in culture. J Invest Dermatol. 2000 Feb;114(2):349-53.
known-action:unknown
name:Retinoic acid receptor alpha
general-function:Zinc ion binding
specific-function:Receptor for retinoic acid. Retinoic acid receptors bind as heterodimers to their target response elements in response to their ligands, all-trans or 9-cis retinoic acid, and regulate gene expression in various biological processes. The RXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence of ligand, the RXR-RAR heterodimers associate with a multiprotein complex containing transcription corepressors that induce histone acetylation, chromatin condensation and transcriptional suppression. On ligand binding, the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation. RARA plays an essential role in the regulation of retinoic acid-induced germ cell development during spermatogenesis. Has a role in the survival of early spermatocytes at the beginning prophase of meiosis. In Sertoli cells, may promote the survival and development of early meiotic prophase spermatocytes. In concert with RARG, required for skeletal growth, matrix homeostasis and growth plate function (By similarity). Regulates expression of target genes in a ligand-dependent manner by recruiting chromatin complexes containing KMT2E/MLL5. Mediates retinoic acid-induced granulopoiesis.
gene-name:RARA
locus:17q21
cellular-location:Nucleus
transmembrane-regions:
signal-regions:
theoretical-pi:7.95
molecular-weight:50770.805
chromosome-location:17
organism:Humans
external-identifiers:HUGO Gene Nomenclature Committee (HGNC)HGNC:9864GenAtlasRARAGenBank Gene DatabaseX06614GenBank Protein Database36157IUPHAR590Guide to Pharmacology590UniProtKBP10276UniProt AccessionRARA_HUMAN
synonyms:NR1B1Nuclear receptor subfamily 1 group B member 1RAR-alpha
amino-acid-sequence:>lcl|BSEQ0001322|Retinoic acid receptor alpha MASNSSSCPTPGGGHLNGYPVPPYAFFFPPMLGGLSPPGALTTLQHQLPVSGYSTPSPAT IETQSSSSEEIVPSPPSPPPLPRIYKPCFVCQDKSSGYHYGVSACEGCKGFFRRSIQKNM VYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKESVRNDRNKKKKEVPKPECSESYTL TPEVGELIEKVRKAHQETFPALCQLGKYTTNNSSEQRVSLDIDLWDKFSELSTKCIIKTV EFAKQLPGFTTLTIADQITLLKAACLDILILRICTRYTPEQDTMTFSDGLTLNRTQMHNA GFGPLTDLVFAFANQLLPLEMDDAETGLLSAICLICGDRQDLEQPDRVDMLQEPLLEALK VYVRKRRPSRPHMFPKMLMKITDLRSISAKGAERVITLKMEIPGSMPPLIQEMLENSEGL DTLSGQPGGGGRDGGGLAPPPGSCSPSLSPSSNRSSPATHSP
gene-sequence:>lcl|BSEQ0016168|Retinoic acid receptor alpha (RARA) ATGGCCAGCAACAGCAGCTCCTGCCCGACACCTGGGGGCGGGCACCTCAATGGGTACCCG GTGCCTCCCTACGCCTTCTTCTTCCCCCCTATGCTGGGTGGACTCTCCCCGCCAGGCGCT CTGACCACTCTCCAGCACCAGCTTCCAGTTAGTGGATATAGCACACCATCCCCAGCCACC ATTGAGACCCAGAGCAGCAGTTCTGAAGAGATAGTGCCCAGCCCTCCCTCGCCACCCCCT CTACCCCGCATCTACAAGCCTTGCTTTGTCTGTCAGGACAAGTCCTCAGGCTACCACTAT GGGGTCAGCGCCTGTGAGGGCTGCAAGGGCTTCTTCCGCCGCAGCATCCAGAAGAACATG GTGTACACGTGTCACCGGGACAAGAACTGCATCATCAACAAGGTGACCCGGAACCGCTGC CAGTACTGCCGACTGCAGAAGTGCTTTGAAGTGGGCATGTCCAAGGAGTCTGTGAGAAAC GACCGAAACAAGAAGAAGAAGGAGGTGCCCAAGCCCGAGTGCTCTGAGAGCTACACGCTG ACGCCGGAGGTGGGGGAGCTCATTGAGAAGGTGCGCAAAGCGCACCAGGAAACCTTCCCT GCCCTCTGCCAGCTGGGCAAATACACTACGAACAACAGCTCAGAACAACGTGTCTCTCTG GACATTGACCTCTGGGACAAGTTCAGTGAACTCTCCACCAAGTGCATCATTAAGACTGTG GAGTTCGCCAAGCAGCTGCCCGGCTTCACCACCCTCACCATCGCCGACCAGATCACCCTC CTCAAGGCTGCCTGCCTGGACATCCTGATCCTGCGGATCTGCACGCGGTACACGCCCGAG CAGGACACCATGACCTTCTCGGACGGGCTGACCCTGAACCGGACCCAGATGCACAACGCT GGCTTCGGCCCCCTCACCGACCTGGTCTTTGCCTTCGCCAACCAGCTGCTGCCCCTGGAG ATGGATGATGCGGAGACGGGGCTGCTCAGCGCCATCTGCCTCATCTGCGGAGACCGCCAG GACCTGGAGCAGCCGGACCGGGTGGACATGCTGCAGGAGCCGCTGCTGGAGGCGCTAAAG GTCTACGTGCGGAAGCGGAGGCCCAGCCGCCCCCACATGTTCCCCAAGATGCTAATGAAG ATTACTGACCTGCGAAGCATCAGCGCCAAGGGGGCTGAGCGGGTGATCACGCTGAAGATG GAGATCCCGGGCTCCATGCCGCCTCTCATCCAGGAAATGTTGGAGAACTCAGAGGGCCTG GACACTCTGAGCGGACAGCCGGGGGGTGGGGGGCGGGACGGGGGTGGCCTGGCCCCCCCG CCAGGCAGCTGTAGCCCCAGCCTCAGCCCCAGCTCCAACAGAAGCAGCCCGGCCACCCAC TCCCCGTGA
pfams:PF00104Hormone_recepPF00105zf-C4
go-classifiers:componentactin cytoskeletoncomponentcell surfacecomponentcytoplasmcomponentdendritecomponentneuronal cell bodycomponentnuclear chromatincomponentnucleoplasmcomponentnucleusfunctionalpha-actinin bindingfunctionchromatin DNA bindingfunctionenzyme bindingfunctionprotein domain specific bindingfunctionprotein heterodimerization activityfunctionprotein kinase A bindingfunctionprotein kinase B bindingfunctionreceptor bindingfunctionretinoic acid bindingfunctionretinoic acid receptor activityfunctionretinoic acid-responsive element bindingfunctionRNA polymerase II regulatory region sequence-specific DNA bindingfunctionsteroid hormone receptor activityfunctiontranscription coactivator activityfunctiontranscription corepressor activityfunctiontranscription factor activity, sequence-specific DNA bindingfunctiontranscription factor bindingfunctionzinc ion bindingprocessapoptotic cell clearanceprocesscellular response to estrogen stimulusprocesscellular response to lipopolysaccharideprocesscellular response to retinoic acidprocesschondroblast differentiationprocessembryonic camera-type eye developmentprocessface developmentprocessgene expressionprocessgerm cell developmentprocessglandular epithelial cell developmentprocessgrowth plate cartilage developmentprocesslimb developmentprocessmulticellular organism growthprocessnegative regulation of apoptotic processprocessnegative regulation of cartilage developmentprocessnegative regulation of granulocyte differentiationprocessnegative regulation of interferon-gamma productionprocessnegative regulation of transcription from RNA polymerase II promoterprocessnegative regulation of transcription, DNA-templatedprocessnegative regulation of translational initiationprocessnegative regulation of tumor necrosis factor productionprocessneural tube closureprocessoutflow tract septum morphogenesisprocesspositive regulation of bindingprocesspositive regulation of cell cycleprocesspositive regulation of cell proliferationprocesspositive regulation of interleukin-13 productionprocesspositive regulation of interleukin-4 productionprocesspositive regulation of interleukin-5 productionprocesspositive regulation of T-helper 2 cell differentiationprocesspositive regulation of transcription from RNA polymerase II promoterprocesspositive regulation of transcription, DNA-templatedprocessprotein phosphorylationprocessresponse to retinoic acidprocessretinoic acid receptor signaling pathwayprocessSertoli cell fate commitmentprocesssignal transductionprocessspermatogenesisprocesstrachea cartilage developmentprocesstranscription initiation from RNA polymerase II promoterprocessureteric bud developmentprocessventricular cardiac muscle cell differentiation
id:BE0000529
name:Aspartate aminotransferase, cytoplasmic
organism:Humans
action:inhibitor
Wang Q, Zhang Q, Luan S, Yang K, Zheng M, Li K, Chen L, Li H: Adapalene inhibits ovarian cancer ES-2 cells growth by targeting glutamic-oxaloacetic transaminase 1. Bioorg Chem. 2019 Dec;93:103315. doi: 10.1016/j.bioorg.2019.103315. Epub 2019 Sep 26.
known-action:unknown
name:Aspartate aminotransferase, cytoplasmic
general-function:Pyridoxal phosphate binding
specific-function:Biosynthesis of L-glutamate from L-aspartate or L-cysteine. Important regulator of levels of glutamate, the major excitatory neurotransmitter of the vertebrate central nervous system. Acts as a scavenger of glutamate in brain neuroprotection. The aspartate aminotransferase activity is involved in hepatic glucose synthesis during development and in adipocyte glyceroneogenesis. Using L-cysteine as substrate, regulates levels of mercaptopyruvate, an important source of hydrogen sulfide. Mercaptopyruvate is converted into H(2)S via the action of 3-mercaptopyruvate sulfurtransferase (3MST). Hydrogen sulfide is an important synaptic modulator and neuroprotectant in the brain.
gene-name:GOT1
locus:10q24.1-q25.1
cellular-location:Cytoplasm
transmembrane-regions:
signal-regions:
theoretical-pi:7.01
molecular-weight:46247.14
chromosome-location:10
organism:Humans
external-identifiers:HUGO Gene Nomenclature Committee (HGNC)HGNC:4432GenAtlasGOT1GenBank Gene DatabaseM37400GenBank Protein Database179067UniProtKBP17174UniProt AccessionAATC_HUMAN
synonyms:2.6.1.1cAspATcCATCysteine aminotransferase, cytoplasmicCysteine transaminase, cytoplasmicGlutamate oxaloacetate transaminase 1Transaminase A
amino-acid-sequence:>lcl|BSEQ0037039|Aspartate aminotransferase, cytoplasmic MAPPSVFAEVPQAQPVLVFKLTADFREDPDPRKVNLGVGAYRTDDCHPWVLPVVKKVEQK IANDNSLNHEYLPILGLAEFRSCASRLALGDDSPALKEKRVGGVQSLGGTGALRIGADFL ARWYNGTNNKNTPVYVSSPTWENHNAVFSAAGFKDIRSYRYWDAEKRGLDLQGFLNDLEN APEFSIVVLHACAHNPTGIDPTPEQWKQIASVMKHRFLFPFFDSAYQGFASGNLERDAWA IRYFVSEGFEFFCAQSFSKNFGLYNERVGNLTVVGKEPESILQVLSQMEKIVRITWSNPP AQGARIVASTLSNPELFEEWTGNVKTMADRILTMRSELRARLEALKTPGTWNHITDQIGM FSFTGLNPKQVEYLVNEKHIYLLPSGRINVSGLTTKNLDYVATSIHEAVTKIQ
gene-sequence:>lcl|BSEQ0010371|Aspartate aminotransferase, cytoplasmic (GOT1) ATGGCACCTCCGTCAGTCTTTGCCGAGGTTCCGCAGGCCCAGCCTGTCCTGGTCTTCAAG CTCACTGCCGACTTCAGGGAGGATCCGGACCCCCGCAAGGTCAACCTGGGAGTGGGAGCA TATCGCACGGATGACTGCCATCCCTGGGTTTTGCCAGTAGTGAAGAAAGTGGAGCAGAAG ATTGCTAATGACAATAGCCTAAATCACGAGTATCTGCCAATCCTGGGCCTGGCTGAGTTC CGGAGCTGTGCTTCTCGTCTTGCCCTTGGGGATGACAGCCCAGCACTCAAGGAGAAGCGG GTAGGAGGTGTGCAATCTTTGGGGGGAACAGGTGCACTTCGAATTGGAGCTGATTTCTTA GCGCGTTGGTACAATGGAACAAACAACAAGAACACACCTGTCTATGTGTCCTCACCAACC TGGGAGAATCACAATGCTGTGTTTTCCGCTGCTGGTTTTAAAGACATTCGGTCCTATCGC TACTGGGATGCAGAGAAGAGAGGATTGGACCTCCAGGGCTTCCTGAATGATCTGGAGAAT GCTCCTGAGTTCTCCATTGTTGTCCTCCACGCCTGTGCACACAACCCAACTGGGATTGAC CCAACTCCGGAGCAGTGGAAGCAGATTGCTTCTGTCATGAAGCACCGGTTTCTGTTCCCC TTCTTTGACTCAGCCTATCAGGGCTTCGCATCTGGAAACCTGGAGAGAGATGCCTGGGCC ATTCGCTATTTTGTGTCTGAAGGCTTCGAGTTCTTCTGTGCCCAGTCCTTCTCCAAGAAC TTCGGGCTCTACAATGAGAGAGTCGGGAATCTGACTGTGGTTGGAAAAGAACCTGAGAGC ATCCTGCAAGTCCTTTCCCAGATGGAGAAGATCGTGCGGATTACTTGGTCCAATCCCCCC GCCCAGGGAGCACGAATTGTGGCCAGCACCCTCTCTAACCCTGAGCTCTTTGAGGAATGG ACAGGTAATGTGAAGACAATGGCTGACCGGATTCTGACCATGAGATCTGAACTCAGGGCA CGACTAGAAGCCCTCAAAACCCCTGGGACCTGGAACCACATCACTGATCAAATTGGCATG TTCAGCTTCACTGGGTTGAACCCCAAGCAGGTTGAGTATCTGGTCAATGAAAAGCACATC TACCTGCTGCCAAGTGGTCGAATCAACGTGAGTGGCTTAACCACCAAAAATCTAGATTAC GTGGCCACCTCCATCCATGAAGCAGTCACCAAAATCCAGTGA
pfams:PF00155Aminotran_1_2
go-classifiers:componentaxon terminuscomponentcytoplasmcomponentcytosolcomponentextracellular exosomecomponentlysosomecomponentnucleusfunctioncarboxylic acid bindingfunctionidentical protein bindingfunctionL-aspartatefunctionL-cysteinefunctionL-phenylalaninefunctionphosphatidylserine decarboxylase activityfunctionpyridoxal phosphate bindingprocess2-oxoglutarate metabolic processprocessaspartate biosynthetic processprocessaspartate catabolic processprocessaspartate metabolic processprocesscarbohydrate metabolic processprocesscellular amino acid biosynthetic processprocesscellular nitrogen compound metabolic processprocesscellular response to insulin stimulusprocessfatty acid homeostasisprocessgluconeogenesisprocessglucose metabolic processprocessglutamate catabolic process to 2-oxoglutarateprocessglutamate catabolic process to aspartateprocessglutamate metabolic processprocessglycerol biosynthetic processprocessL-methionine biosynthetic process from methylthioadenosineprocessNotch signaling pathwayprocessoxaloacetate metabolic processprocesspolyamine metabolic processprocessresponse to glucocorticoidprocesssmall molecule metabolic processprocesssulfur amino acid metabolic process

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