Target Information
Target General Infomation | |||||
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Target ID |
T82146
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Former ID |
TTDS00075
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Target Name |
Retinoic acid receptor gamma
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Gene Name |
RARG
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Synonyms |
Nuclear receptor subfamily 1 group B member 3; RAR-gamma; RARG
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Target Type |
Successful
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Disease | Acne vulgaris [ICD9: 706.1; ICD10: L70.0] | ||||
Emphysema [ICD9: 492; ICD10: J43] | |||||
Kaposi's sarcoma [ICD9: 176; ICD10: C46] | |||||
Psoriasis [ICD9: 696; ICD10: L40] | |||||
Function |
This is a receptor for retinoic acid. This metabolite has profound effects on vertebrate development. Retinoic acid is a morphogen and is a powerful teratogen. This receptor controls cells functions by directly regulating gene expression.
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BioChemical Class |
Nuclear hormone receptor
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Target Validation |
T82146
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UniProt ID | |||||
Sequence |
MATNKERLFAAGALGPGSGYPGAGFPFAFPGALRGSPPFEMLSPSFRGLGQPDLPKEMAS
LSVETQSTSSEEMVPSSPSPPPPPRVYKPCFVCNDKSSGYHYGVSSCEGCKGFFRRSIQK NMVYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKEAVRNDRNKKKKEVKEEGSPDSY ELSPQLEELITKVSKAHQETFPSLCQLGKYTTNSSADHRVQLDLGLWDKFSELATKCIIK IVEFAKRLPGFTGLSIADQITLLKAACLDILMLRICTRYTPEQDTMTFSDGLTLNRTQMH NAGFGPLTDLVFAFAGQLLPLEMDDTETGLLSAICLICGDRMDLEEPEKVDKLQEPLLEA LRLYARRRRPSQPYMFPRMLMKITDLRGISTKGAERAITLKMEIPGPMPPLIREMLENPE MFEDDSSQPGPHPNASSEDEVPGGQGKGGLKSPA |
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Structure |
1EXA; 1EXX; 1FCX; 1FCY; 1FCZ; 1FD0; 2LBD; 3LBD; 4LBD
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Drugs and Mode of Action | |||||
Agonist | 9-cis-retinoic acid | Drug Info | [536030] | ||
9-trans-retinoic acid | Drug Info | [536030] | |||
AHPN | Drug Info | [534078] | |||
BMS270394 | Drug Info | [525782] | |||
CD666 | Drug Info | [526744] | |||
Palovarotene | Drug Info | [531773] | |||
Trifarotene | Drug Info | [549389] | |||
[3H]9-cis-retinoic acid | Drug Info | [534000] | |||
Antagonist | AGN193109 | Drug Info | [525680] | ||
CD2665 | Drug Info | [534402] | |||
MM 11253 | Drug Info | [525726] | |||
Modulator | Alitretinoin | Drug Info | [536652] | ||
Inhibitor | BMS184394 | Drug Info | [551393] | ||
CD564 | Drug Info | [551393] | |||
Dodecyl-Alpha-D-Maltoside | Drug Info | [551391] | |||
SR11254 | Drug Info | [551393] | |||
Binder | Tazarotene | Drug Info | [534998] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
References | |||||
Ref 531773 | Randomised controlled trial for emphysema with a selective agonist of the gamma-type retinoic acid receptor. Eur Respir J. 2012 Aug;40(2):306-12. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 539711 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2645). | ||||
Ref 541988 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6952). | ||||
Ref 525680 | Therapeutic applications for ligands of retinoid receptors. Curr Pharm Des. 2000 Jan;6(1):25-58. | ||||
Ref 525726 | Modulation of retinoic acid receptor function alters the growth inhibitory response of oral SCC cells to retinoids. Oncogene. 2000 Mar 9;19(11):1457-65. | ||||
Ref 525782 | Enantiomer discrimination illustrated by high-resolution crystal structures of the human nuclear receptor hRARgamma. Proc Natl Acad Sci U S A. 2000 Jun 6;97(12):6322-7. | ||||
Ref 526744 | Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma. Biochem Biophys Res Commun. 1992 Jul 31;186(2):977-83. | ||||
Ref 531773 | Randomised controlled trial for emphysema with a selective agonist of the gamma-type retinoic acid receptor. Eur Respir J. 2012 Aug;40(2):306-12. | ||||
Ref 534000 | Retinoic acid receptors and retinoid X receptors: interactions with endogenous retinoic acids. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):30-4. | ||||
Ref 534078 | Synthesis, structure-affinity relationships, and biological activities of ligands binding to retinoic acid receptor subtypes. J Med Chem. 1995 Dec 22;38(26):4993-5006. | ||||
Ref 534402 | Induction of apoptosis by retinoids and retinoic acid receptor gamma-selective compounds in mouse thymocytes through a novel apoptosis pathway. Mol Pharmacol. 1997 Jun;51(6):972-82. | ||||
Ref 534998 | Recent developments in receptor-selective retinoids. Curr Pharm Des. 2000 Jun;6(9):919-31. | ||||
Ref 536030 | Targacept active conformation search: a new method for predicting the conformation of a ligand bound to its protein target. J Med Chem. 2004 Dec 30;47(27):6831-9. | ||||
Ref 549389 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036364) |
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