Details of the Drug Therapeutic Target (DTT)

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]
Related Disease	Type 2 diabetes mellitus [ICD-11: 5A11]
BioChemical Class	GPCR rhodopsin
UniProt ID	GPBAR_HUMAN
TTD ID	T86273
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
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

1 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]
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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	[2]
PMID29649907-Compound-INT767	DMA0RI8	N. A.	N. A.	Patented	[2]
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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	[3]
XL475	DMD8TNK	Type-2 diabetes	5A11	Preclinical	[4]
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2 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Bile acid	DMIY2HW	Discovery agent	N.A.	Investigative	[5]
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	Farnesoid X receptor modulators 2014-present: a patent review.Expert Opin Ther Pat. 2018 May;28(5):351-364.
3	FXR/TGR5 Dual Agonist Prevents Progression of Nephropathy in Diabetes and Obesity. J Am Soc Nephrol. 2018 Jan;29(1):118-137.
4	Clinical pipeline report, company report or official report of Exelixis (2011).
5	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.
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).