Target Information

Target General Infomation
Target ID
T46456
Former ID
TTDR01075
Target Name
Retinoic acid receptor RXR-gamma
Gene Name
RXRG
Synonyms
Nuclear receptor subfamily 2 group B member 3; Retinoid X receptor gamma; RXRG
Target Type
Successful
Disease Cancer [ICD9: 140-229; ICD10: C00-C96]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Night blindness [ICD9: 368.6; ICD10: H53.6]
Prostate cancer [ICD9: 185; ICD10: C61]
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).
BioChemical Class
Nuclear hormone receptor
Target Validation
T46456
UniProt ID
P48443
Sequence
MYGNYSHFMKFPAGYGGSPGHTGSTSMSPSAALSTGKPMDSHPSYTDTPVSAPRTLSAVG
TPLNALGSPYRVITSAMGPPSGALAAPPGINLVAPPSSQLNVVNSVSSSEDIKPLPGLPG
IGNMNYPSTSPGSLVKHICAICGDRSSGKHYGVYSCEGCKGFFKRTIRKDLIYTCRDNKD
CLIDKRQRNRCQYCRYQKCLVMGMKREAVQEERQRSRERAESEAECATSGHEDMPVERIL
EAELAVEPKTESYGDMNMENSTNDPVTNICHAADKQLFTLVEWAKRIPHFSDLTLEDQVI
LLRAGWNELLIASFSHRSVSVQDGILLATGLHVHRSSAHSAGVGSIFDRVLTELVSKMKD
MQMDKSELGCLRAIVLFNPDAKGLSNPSEVETLREKVYATLEAYTKQKYPEQPGRFAKLL
LRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLETPLQIT
Structure
2GL8
Drugs and Mode of Action
Drug(s) Vitamin A Drug Info Approved Night blindness [537623], [540652]
NRX-4204 Drug Info Phase 2 Diabetes [523805], [539853]
9cUAB-30 Drug Info Phase 1 Cancer [528795]
IRX4204 Drug Info Phase 1 Prostate cancer [525182]
SR-11237 Drug Info Terminated Cancer [539850], [545989]
Modulator 9cUAB-30 Drug Info [528795]
IRX4204 Drug Info
NRX-4204 Drug Info
SR-11237 Drug Info [530188]
Inhibitor AGN-34 Drug Info [527690]
Antagonist LG100754 Drug Info [534228]
Binder Vitamin A Drug Info [537623]
Agonist [3H]9-cis-retinoic acid Drug Info [534000]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway PPAR signaling pathway
Thyroid hormone signaling pathway
Adipocytokine signaling pathway
Pathways in cancer
Transcriptional misregulation in cancer
Thyroid cancer
Small cell lung cancer
Non-small cell lung cancer
Pathway Interaction Database Regulation of Androgen receptor activity
RXR and RAR heterodimerization with other nuclear receptor
Retinoic acid receptors-mediated signaling
a6b1 and a6b4 Integrin signaling
Reactome Nuclear Receptor transcription pathway
WikiPathways Vitamin A and Carotenoid Metabolism
Adipogenesis
Nuclear Receptors
References
Ref 523805ClinicalTrials.gov (NCT01540071) Trial of NRX 194204 in Castration- and Taxane-Resistant Prostate Cancer. U.S. National Institutes of Health.
Ref 525182ClinicalTrials.gov (NCT02438215) Study of IRX4204 for Treatment of Early Parkinson's Disease. U.S. National Institutes of Health.
Ref 528795In vitro metabolic characterization, phenotyping, and kinetic studies of 9cUAB30, a retinoid X receptor-specific retinoid. Drug Metab Dispos. 2007 Jul;35(7):1157-64. Epub 2007 Apr 19.
Ref 537623Vitamins and cofactors: highlights of ESBOC 2009. Nat Chem Biol. 2009 Aug;5(8):530-3.
Ref 539850(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: 2809).
Ref 539853(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: 2811).
Ref 540652(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: 4053).
Ref 545989Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005745)
Ref 527690J Med Chem. 2005 Aug 25;48(17):5383-403.Farnesoid X receptor: from structure to potential clinical applications.
Ref 528795In vitro metabolic characterization, phenotyping, and kinetic studies of 9cUAB30, a retinoid X receptor-specific retinoid. Drug Metab Dispos. 2007 Jul;35(7):1157-64. Epub 2007 Apr 19.
Ref 530188Silicon analogues of the RXR-selective retinoid agonist SR11237 (BMS649): chemistry and biology. ChemMedChem. 2009 Jul;4(7):1143-52.
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 534228Activation of specific RXR heterodimers by an antagonist of RXR homodimers. Nature. 1996 Oct 3;383(6599):450-3.
Ref 537623Vitamins and cofactors: highlights of ESBOC 2009. Nat Chem Biol. 2009 Aug;5(8):530-3.

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