Target Information

Target General Infomation
Target ID
T82146
Former ID
TTDS00075
Target Name
Retinoic acid receptor gamma
Gene Name
RARG
Synonyms
Nuclear receptor subfamily 1 group B member 3; RAR-gamma; RARG
Target Type
Successful
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.
BioChemical Class
Nuclear hormone receptor
Target Validation
T82146
UniProt ID
P13631
Sequence
MATNKERLFAAGALGPGSGYPGAGFPFAFPGALRGSPPFEMLSPSFRGLGQPDLPKEMAS
LSVETQSTSSEEMVPSSPSPPPPPRVYKPCFVCNDKSSGYHYGVSSCEGCKGFFRRSIQK
NMVYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKEAVRNDRNKKKKEVKEEGSPDSY
ELSPQLEELITKVSKAHQETFPSLCQLGKYTTNSSADHRVQLDLGLWDKFSELATKCIIK
IVEFAKRLPGFTGLSIADQITLLKAACLDILMLRICTRYTPEQDTMTFSDGLTLNRTQMH
NAGFGPLTDLVFAFAGQLLPLEMDDTETGLLSAICLICGDRMDLEEPEKVDKLQEPLLEA
LRLYARRRRPSQPYMFPRMLMKITDLRGISTKGAERAITLKMEIPGPMPPLIREMLENPE
MFEDDSSQPGPHPNASSEDEVPGGQGKGGLKSPA
Structure
1EXA; 1EXX; 1FCX; 1FCY; 1FCZ; 1FD0; 2LBD; 3LBD; 4LBD
Drugs and Mode of Action
Drug(s) Alitretinoin Drug Info Approved Kaposi's sarcoma [536361], [539711]
Tazarotene Drug Info Approved Psoriasis [536361], [541988]
Trifarotene Drug Info Phase 3 Acne vulgaris [549388]
Palovarotene Drug Info Phase 2 Emphysema [531773], [543031]
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
Reactome Nuclear Receptor transcription pathway
WikiPathways Vitamin A and Carotenoid Metabolism
Nuclear Receptors in Lipid Metabolism and Toxicity
Mesodermal Commitment Pathway
Endoderm Differentiation
Nuclear Receptors
References
Ref 531773Randomised 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 536361Natural 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 543031(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: 8276).
Ref 549388Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036364)
Ref 525680Therapeutic applications for ligands of retinoid receptors. Curr Pharm Des. 2000 Jan;6(1):25-58.
Ref 525726Modulation 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 525782Enantiomer 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 526744Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma. Biochem Biophys Res Commun. 1992 Jul 31;186(2):977-83.
Ref 531773Randomised 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 534000Retinoic 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 534078Synthesis, 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 534402Induction 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 534998Recent developments in receptor-selective retinoids. Curr Pharm Des. 2000 Jun;6(9):919-31.
Ref 536030Targacept 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 536652Alitretinoin: a comprehensive review. Expert Opin Investig Drugs. 2008 Mar;17(3):437-43.
Ref 549389Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800036364)
Ref 551391DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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