General Information of Drug Therapeutic Target (DTT) (ID: TTSDVTR)

DTT Name G-protein coupled bile acid receptor 1 (GPBAR1)
Synonyms hGPCR19; hBG37; TGR5; Membrane-type receptor for bile acids; M-BAR; G-protein coupled receptor GPCR19; BG37
Gene Name GPBAR1
DTT Type
Clinical trial target
[1]
BioChemical Class
GPCR rhodopsin
UniProt ID
GPBAR_HUMAN
TTD ID
T86273
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTPNSTGEVPSPIPKGALGLSLALASLIITANLLLALGIAWDRRLRSPPAGCFFLSLLLA
GLLTGLALPTLPGLWNQSRRGYWSCLLVYLAPNFSFLSLLANLLLVHGERYMAVLRPLQP
PGSIRLALLLTWAGPLLFASLPALGWNHWTPGANCSSQAIFPAPYLYLEVYGLLLPAVGA
AAFLSVRVLATAHRQLQDICRLERAVCRDEPSALARALTWRQARAQAGAMLLFGLCWGPY
VATLLLSVLAYEQRPPLGPGTLLSLLSLGSASAAAVPVAMGLGDQRYTAPWRAAAQRCLQ
GLWGRASRDSPGPSIAYHPSSQSSVDLDLN
Function
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. Receptor for bile acid.
Reactome Pathway
G alpha (s) signalling events (R-HSA-418555 )
Class A/1 (Rhodopsin-like receptors) (R-HSA-373076 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
2 Clinical Trial Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Sodium taurocholate DM3GO0J Type-2 diabetes 5A11 Phase 1/2 [1]
Bile acid DM9UZD7 Discovery agent N.A. Phase 1 [2]
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2 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
PMID29649907-Compound-8 DMV2D5M N. A. N. A. Patented [3]
PMID29649907-Compound-INT767 DMA0RI8 N. A. N. A. Patented [3]
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2 Preclinical Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
INT-767 DMRJ9P4 Hepatic fibrosis DB93.0 Preclinical [4]
XL475 DMD8TNK Type-2 diabetes 5A11 Preclinical [5]
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1 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
INT-777 DMTPB8A Metabolic disorder 5C50-5D2Z Investigative [6]
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Molecular Expression Atlas (MEA) of This DTT

Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This DTT
Disease Name ICD 11 Studied Tissue p-value Fold-Change Z-score
Type 2 diabetes 5A11 Liver tissue 4.60E-01 0.02 0.09
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References

1 Bile acids and sphingosine-1-phosphate receptor 2 in hepatic lipid metabolism.Acta Pharmaceutica Sinica B Volume 5, Issue 2, March 2015, Pages 151-157.
2 Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5718-21.
3 Farnesoid X receptor modulators 2014-present: a patent review.Expert Opin Ther Pat. 2018 May;28(5):351-364.
4 FXR/TGR5 Dual Agonist Prevents Progression of Nephropathy in Diabetes and Obesity. J Am Soc Nephrol. 2018 Jan;29(1):118-137.
5 Clinical pipeline report, company report or official report of Exelixis (2011).
6 URL: 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).