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J Recept Signal Transduct Res. 2017 Jun;37(3):290-296. doi: 10.1080/10799893.2016.1247861. Epub 2016 Nov 3.

Discovery and pharmacological effects of a novel GPR142 antagonist.

Author information

1
a Biological Research Department , Daiichi Sankyo RD Novare Co. Ltd. , Tokyo , Japan.
2
b Pain & Neuroscience Laboratories, Research Function, R&D Division , Daiichi Sankyo Co. Ltd. , Tokyo , Japan.
3
c Biologics & Immuno-Oncology Laboratories Research Function , R&D Division , Daiichi Sankyo Co. Ltd. , Tokyo , Japan.
4
d Department of Cardio-Metabolic Disorders , Amgen, Inc. , South San Francisco , CA , USA.
5
e Immunology & Inflammatory Disease Field , Asubio Pharma Co. Ltd. , Kobe , Japan.

Abstract

GPR142 is a G-protein-coupled receptor (GPCR), whose most potent and efficacious ligand has been reported as being the natural amino acid l-tryptophan. GPR142 is highly expressed in pancreatic β-cells and immune cells, suggesting the receptor may play a role in the pathogenesis and development of diabetes or inflammatory diseases. In a previous report, we developed GPR142 agonists as insulin secretagogues. In this report, we show the discovery of a selective, potent small-molecule GPR142 antagonist, CLP-3094, and its pharmacological characteristics. These data support targeting this receptor for the treatment of chronic inflammatory diseases.

KEYWORDS:

GPR142 antagonist; KO mouse; anti-CII Ab-induced arthritis; inflammatory diseases; l-tryptophan

PMID:
27807998
DOI:
10.1080/10799893.2016.1247861
[Indexed for MEDLINE]

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