Target Information

Target General Infomation
Target ID
T61657
Former ID
TTDR01191
Target Name
Retinoic acid receptor beta
Gene Name
RARB
Synonyms
HBV-activated protein; RAR-beta; RAR-epsilon; RARB
Target Type
Clinical Trial
Disease Alzheimer disease [ICD9: 331; ICD10: G30]
Function
Receptor for retinoic acid. Retinoicacid 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. TheRXR/RAR heterodimers bind to the retinoic acid response elements (RARE) composed of tandem 5'-AGGTCA-3' sites known as DR1-DR5. In the absence or presence of hormone ligand, acts mainly as an activator of gene expression due to weak binding to corepressors. In concert with RARG, required for skeletal growth, matrix homeostasis and growth plate function.
BioChemical Class
Nuclear hormone receptor
UniProt ID
P10826
Sequence
MTTSGHACPVPAVNGHMTHYPATPYPLLFPPVIGGLSLPPLHGLHGHPPPSGCSTPSPAT
IETQSTSSEELVPSPPSPLPPPRVYKPCFVCQDKSSGYHYGVSACEGCKGFFRRSIQKNM
IYTCHRDKNCVINKVTRNRCQYCRLQKCFEVGMSKESVRNDRNKKKKETSKQECTESYEM
TAELDDLTEKIRKAHQETFPSLCQLGKYTTNSSADHRVRLDLGLWDKFSELATKCIIKIV
EFAKRLPGFTGLTIADQITLLKAACLDILILRICTRYTPEQDTMTFSDGLTLNRTQMHNA
GFGPLTDLVFTFANQLLPLEMDDTETGLLSAICLICGDRQDLEEPTKVDKLQEPLLEALK
IYIRKRRPSKPHMFPKILMKITDLRSISAKGAERVITLKMEIPGSMPPLIQEMLENSEGH
EPLTPSSSGNTAEHSPSISPSSVENSGVSQSPLVQ
Drugs and Mode of Action
Drug(s) Tamibarotene Drug Info Phase 2/3 Alzheimer disease [529087], [539714]
Agonist AC261066 Drug Info [527881]
AC55649 Drug Info [527881]
BMS641 Drug Info [527177]
CD666 Drug Info [526744]
[3H]9-cis-retinoic acid Drug Info [534000]
Antagonist AGN193109 Drug Info [525680]
Modulator Tamibarotene Drug Info [531992]
Inhibitor TTNPB Drug Info [551371]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Pathways in cancer
Small cell lung cancer
Non-small cell lung cancer
Reactome Nuclear Receptor transcription pathway
WikiPathways Vitamin A and Carotenoid Metabolism
Nuclear Receptors in Lipid Metabolism and Toxicity
Mesodermal Commitment Pathway
Integrated Pancreatic Cancer Pathway
Nuclear Receptors
References
Ref 529087Tamibarotene. Drugs Today (Barc). 2007 Aug;43(8):563-8.
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 525680Therapeutic applications for ligands of retinoid receptors. Curr Pharm Des. 2000 Jan;6(1):25-58.
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 527177Rational design of RAR-selective ligands revealed by RARbeta crystal stucture. EMBO Rep. 2004 Sep;5(9):877-82.
Ref 527881Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist. J Med Chem. 2005 Dec 1;48(24):7517-9.
Ref 531992Tamibarotene: a candidate retinoid drug for Alzheimer's disease. Biol Pharm Bull. 2012;35(8):1206-12.
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 5513719-cis-retinoic acid analogues with bulky hydrophobic rings: new <span class="caps">RXR</span>-selective agonists. Bioorg Med Chem Lett. 2004 Dec 20;14(24):6117-22.

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