Target Information

Target General Infomation
Target ID
T86273
Former ID
TTDR01440
Target Name
TGR5
Gene Name
GPBAR1
Synonyms
BG37; G-protein coupled bile acid receptor 1; G-protein coupled receptor GPCR19; M-BAR; Membrane-type receptor for bile acids; hBG37; hGPCR19; GPBAR1
Target Type
Clinical Trial
Disease Metabolic disorders [ICD9: 270-279; ICD10: E70-E89]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Function
Receptor for bile acid. Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production. May be involved in the suppression of macrophage functions by bile acids.
BioChemical Class
GPCR rhodopsin
Target Validation
T86273
UniProt ID
Q8TDU6
Sequence
MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLA
GLLTGLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQP
PGSIRLALLLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGA
AAFLSVRVLATAHRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPY
VATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQ
GLWGRASRDSPGPSIAYHPSSQSSVDLDLN
Drugs and Mode of Action
Drug(s) Sodium taurocholate Drug Info Phase 1/2 Type 2 diabetes [551663]
XL475 Drug Info Preclinical Type 2 diabetes [550636]
Inhibitor Bile acid Drug Info [531132]
Agonist INT-777 Drug Info [543800]
XL475 Drug Info [550636]
Modulator Sodium taurocholate Drug Info [551663]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
Reactome Class A/1 (Rhodopsin-like receptors)
G alpha (s) signalling events
WikiPathways GPCR ligand binding
GPCR downstream signaling
References
Ref 550636Clinical pipeline report, company report or official report of Exelixis (2011).
Ref 551663Bile acids and sphingosine-1-phosphate receptor 2 in hepatic lipid metabolism.Acta Pharmaceutica Sinica B Volume 5, Issue 2, March 2015, Pages 151-157.
Ref 531132Bioorg Med Chem Lett. 2010 Oct 1;20(19):5718-21. Epub 2010 Aug 10.Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.
Ref 543800(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. (Target id: 37).
Ref 550636Clinical pipeline report, company report or official report of Exelixis (2011).
Ref 551663Bile acids and sphingosine-1-phosphate receptor 2 in hepatic lipid metabolism.Acta Pharmaceutica Sinica B Volume 5, Issue 2, March 2015, Pages 151-157.

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