Target Information
Target General Infomation | |||||
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Target ID |
T46456
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Former ID |
TTDR01075
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Target Name |
Retinoic acid receptor RXR-gamma
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Gene Name |
RXRG
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Synonyms |
Nuclear receptor subfamily 2 group B member 3; Retinoid X receptor gamma; RXRG
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Target Type |
Successful
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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).
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BioChemical Class |
Nuclear hormone receptor
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Target Validation |
T46456
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UniProt ID | |||||
Sequence |
MYGNYSHFMKFPAGYGGSPGHTGSTSMSPSAALSTGKPMDSHPSYTDTPVSAPRTLSAVG
TPLNALGSPYRVITSAMGPPSGALAAPPGINLVAPPSSQLNVVNSVSSSEDIKPLPGLPG IGNMNYPSTSPGSLVKHICAICGDRSSGKHYGVYSCEGCKGFFKRTIRKDLIYTCRDNKD CLIDKRQRNRCQYCRYQKCLVMGMKREAVQEERQRSRERAESEAECATSGHEDMPVERIL EAELAVEPKTESYGDMNMENSTNDPVTNICHAADKQLFTLVEWAKRIPHFSDLTLEDQVI LLRAGWNELLIASFSHRSVSVQDGILLATGLHVHRSSAHSAGVGSIFDRVLTELVSKMKD MQMDKSELGCLRAIVLFNPDAKGLSNPSEVETLREKVYATLEAYTKQKYPEQPGRFAKLL LRLPALRSIGLKCLEHLFFFKLIGDTPIDTFLMEMLETPLQIT |
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Structure |
2GL8
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Drugs and Mode of Action | |||||
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 523805 | ClinicalTrials.gov (NCT01540071) Trial of NRX 194204 in Castration- and Taxane-Resistant Prostate Cancer. U.S. National Institutes of Health. | ||||
Ref 525182 | ClinicalTrials.gov (NCT02438215) Study of IRX4204 for Treatment of Early Parkinson's Disease. U.S. National Institutes of Health. | ||||
Ref 528795 | In 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 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 527690 | J Med Chem. 2005 Aug 25;48(17):5383-403.Farnesoid X receptor: from structure to potential clinical applications. | ||||
Ref 528795 | In 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 530188 | Silicon analogues of the RXR-selective retinoid agonist SR11237 (BMS649): chemistry and biology. ChemMedChem. 2009 Jul;4(7):1143-52. | ||||
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. |
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