Target Information
Target General Infomation | |||||
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Target ID |
T94085
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Former ID |
TTDS00073
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Target Name |
Retinoic acid receptor alpha
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Gene Name |
RARA
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Synonyms |
RAR alpha; RAR-alpha; RARA
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Target Type |
Clinical Trial
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Disease | Acquired immune deficiency syndrome [ICD9: 42; ICD10: B20] | ||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
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 RXR/RAR 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, the RXR-RAR heterodimers associatewith a multiprotein complex containing transcription corepressors that induce histone acetylation, chromatin condensation and transcriptional suppression. On ligand binding, the corepressors dissociate from the receptors and associate with the coactivators leading to transcriptional activation. RARA plays an essential role in the regulation of retinoic acid-induced germ cell development during spermatogenesis. Has a role in the survival of early spermatocytes at the beginning prophase of meiosis. In Sertoli cells, may promote the survival and development of early meiotic prophase spermatocytes. In concert with RARG, required for skeletal growth, matrix homeostasis and growth plate function (By similarity). Regulates expression of target genes in a ligand- dependent manner by recruiting chromatin complexes containing KMT2E/MLL5. Mediates retinoic acid-induced granulopoiesis.
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BioChemical Class |
Nuclear hormone receptor
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Target Validation |
T94085
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UniProt ID | |||||
Sequence |
MASNSSSCPTPGGGHLNGYPVPPYAFFFPPMLGGLSPPGALTTLQHQLPVSGYSTPSPAT
IETQSSSSEEIVPSPPSPPPLPRIYKPCFVCQDKSSGYHYGVSACEGCKGFFRRSIQKNM VYTCHRDKNCIINKVTRNRCQYCRLQKCFEVGMSKESVRNDRNKKKKEVPKPECSESYTL TPEVGELIEKVRKAHQETFPALCQLGKYTTNNSSEQRVSLDIDLWDKFSELSTKCIIKTV EFAKQLPGFTTLTIADQITLLKAACLDILILRICTRYTPEQDTMTFSDGLTLNRTQMHNA GFGPLTDLVFAFANQLLPLEMDDAETGLLSAICLICGDRQDLEQPDRVDMLQEPLLEALK VYVRKRRPSRPHMFPKMLMKITDLRSISAKGAERVITLKMEIPGSMPPLIQEMLENSEGL DTLSGQPGGGGRDGGGLAPPPGSCSPSLSPSSNRSSPATHSP |
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Drugs and Mode of Action | |||||
Antagonist | AGN193109 | Drug Info | [525680] | ||
BMS614 | Drug Info | [526251] | |||
Ro 41-5253 | Drug Info | [526743] | |||
Agonist | AGN193836 | Drug Info | [526437] | ||
BMS753 | Drug Info | [525545] | |||
CD666 | Drug Info | [526744] | |||
IRX-5183 | Drug Info | [526923], [529087] | |||
LG100268 | Drug Info | [537277] | |||
Ro 40-6055 | Drug Info | [528094] | |||
Ro-40-0655 | Drug Info | [529087] | |||
[3H]9-cis-retinoic acid | Drug Info | [534000] | |||
Modulator | Tamibarotene | Drug Info | [531992] | ||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
Pathways | |||||
KEGG Pathway | Pathways in cancer | ||||
Transcriptional misregulation in cancer | |||||
Acute myeloid leukemia | |||||
Pathway Interaction Database | Retinoic acid receptors-mediated signaling | ||||
Reactome | Nuclear Receptor transcription pathway | ||||
WikiPathways | Vitamin A and Carotenoid Metabolism | ||||
Nuclear Receptors in Lipid Metabolism and Toxicity | |||||
Integrated Pancreatic Cancer Pathway | |||||
Adipogenesis | |||||
Nuclear Receptors | |||||
References | |||||
Ref 539714 | (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: 2648). | ||||
Ref 539849 | (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: 2808). | ||||
Ref 525545 | Structural basis for engineering of retinoic acid receptor isotype-selective agonists and antagonists. Chem Biol. 1999 Aug;6(8):519-29. | ||||
Ref 525680 | Therapeutic applications for ligands of retinoid receptors. Curr Pharm Des. 2000 Jan;6(1):25-58. | ||||
Ref 526251 | Co-regulator recruitment and the mechanism of retinoic acid receptor synergy. Nature. 2002 Jan 10;415(6868):187-92. | ||||
Ref 526437 | Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8.Synthesis and biological activity of retinoic acid receptor-alpha specific amides. | ||||
Ref 526743 | A retinoic acid receptor alpha antagonist selectively counteracts retinoic acid effects. Proc Natl Acad Sci U S A. 1992 Aug 1;89(15):7129-33. | ||||
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 526923 | Retinoic acid receptor alpha and retinoid X receptor specific agonists reduce renal injury in established chronic glomerulonephritis of the rat. J Mol Med (Berl). 2004 Feb;82(2):116-25. Epub 2004 Jan 8. | ||||
Ref 528094 | Selective high affinity retinoic acid receptor alpha or beta-gamma ligands. Mol Pharmacol. 1991 Oct;40(4):556-62. | ||||
Ref 531992 | Tamibarotene: a candidate retinoid drug for Alzheimer's disease. Biol Pharm Bull. 2012;35(8):1206-12. |
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