General Information of Drug Therapeutic Target (DTT) (ID: TT1Q3IE)

DTT Name Retinoic acid receptor gamma (RARG)
Synonyms RAR-gamma; Nuclear receptor subfamily 1 group B member 3; NR1B3
Gene Name RARG
DTT Type
Successful target
[1]
BioChemical Class
Nuclear hormone receptor
UniProt ID
RARG_HUMAN
TTD ID
T82146
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MATNKERLFAAGALGPGSGYPGAGFPFAFPGALRGSPPFEMLSPSFRGLGQPDLPKEMAS
LSVETQSTSSEEMVPSSPSPPPPPRVYKPCFVCNDKSSGYHYGVSSCEGCKGFFRRSIQK
NMVYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKEAVRNDRNKKKKEVKEEGSPDSY
ELSPQLEELITKVSKAHQETFPSLCQLGKYTTNSSADHRVQLDLGLWDKFSELATKCIIK
IVEFAKRLPGFTGLSIADQITLLKAACLDILMLRICTRYTPEQDTMTFSDGLTLNRTQMH
NAGFGPLTDLVFAFAGQLLPLEMDDTETGLLSAICLICGDRMDLEEPEKVDKLQEPLLEA
LRLYARRRRPSQPYMFPRMLMKITDLRGISTKGAERAITLKMEIPGPMPPLIREMLENPE
MFEDDSSQPGPHPNASSEDEVPGGQGKGGLKSPA
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).
Reactome Pathway
Nuclear Receptor transcription pathway (R-HSA-383280 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
5 Approved Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Alitretinoin DMME8LH Kaposi sarcoma 2B57 Approved [2]
Palovarotene DMAD2OZ Fibrodysplasia ossificans progressiva FB31.1 Approved [3]
Tazarotene DM8SMD1 Acne vulgaris ED80 Approved [1]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [4]
Trifarotene DMOL793 Acne vulgaris ED80 Approved [5]
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6 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID27336223-Compound-11 DMBN6KU N. A. N. A. Patented [6]
PMID27336223-Compound-12 DMT4P7K N. A. N. A. Patented [6]
PMID27336223-Compound-13 DMSZLYD N. A. N. A. Patented [6]
PMID27336223-Compound-14 DMC41MA N. A. N. A. Patented [6]
PMID27336223-Compound-15 DMIYCFE N. A. N. A. Patented [6]
PMID27336223-Compound-9 DM6V13W N. A. N. A. Patented [6]
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⏷ Show the Full List of 6 Patented Agent(s)
10 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
AGN193109 DMC0YOE Discovery agent N.A. Investigative [7]
AHPN DM8G6O4 Discovery agent N.A. Investigative [8]
BMS184394 DMGE82R Discovery agent N.A. Investigative [9]
BMS270394 DM82SJP Discovery agent N.A. Investigative [10]
CD2665 DM05M9X Discovery agent N.A. Investigative [11]
CD564 DMZ2LPO Discovery agent N.A. Investigative [9]
CD666 DMC8X9Y Discovery agent N.A. Investigative [12]
Dodecyl-Alpha-D-Maltoside DMMDG92 Discovery agent N.A. Investigative [13]
MM 11253 DMT1NP8 Discovery agent N.A. Investigative [14]
SR11254 DMBA297 Discovery agent N.A. Investigative [9]
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⏷ Show the Full List of 10 Investigative Drug(s)

Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Sarcoma 2C82 Muscle tissue 5.43E-04 -0.14 -0.37
Psoriasis EA90 Skin 2.11E-08 -0.77 -0.93
Chronic obstructive pulmonary disease CA23 Lung tissue 1.81E-01 0.07 0.2
Chronic obstructive pulmonary disease CA23 Small airway epithelium 1.45E-03 -0.13 -0.39
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References

1 Recent developments in receptor-selective retinoids. Curr Pharm Des. 2000 Jun;6(9):919-31.
2 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.
3 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.
4 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.
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2019
6 Therapeutic use of selective synthetic ligands for retinoic acid receptors: a patent review.Expert Opin Ther Pat. 2016 Aug;26(8):957-71.
7 Therapeutic applications for ligands of retinoid receptors. Curr Pharm Des. 2000 Jan;6(1):25-58.
8 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.
9 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
10 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.
11 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.
12 Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma. Biochem Biophys Res Commun. 1992 Jul 31;186(2):977-83.
13 DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41.
14 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.