Back to Search
Start Over
Design, synthesis and biological evaluation of indane derived GPR40 agoPAMs.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2019 Jul 15; Vol. 29 (14), pp. 1842-1848. Date of Electronic Publication: 2019 May 02. - Publication Year :
- 2019
-
Abstract
- GPR40 (FFAR1 or FFA1) is a G protein-coupled receptor, primarily expressed in pancreatic islet β-cells and intestinal enteroendocrine cells. When activated by fatty acids, GPR40 elicits increased insulin secretion from islet β-cells only in the presence of elevated glucose levels. Towards this end, studies were undertaken towards discovering a novel GPR40 Agonist whose mode of action is via Positive Allosteric Modulation of the GPR40 receptor (AgoPAM). Efforts were made to identify a suitable GPR40 AgoPAM tool molecule to investigate mechanism of action and de-risk liver toxicity of GPR40 AgoPAMs due to reactive acyl-glucuronide (AG) metabolites.<br /> (Copyright © 2019 Elsevier Ltd. All rights reserved.)
- Subjects :
- Drug Design
Humans
Indans metabolism
Receptors, G-Protein-Coupled agonists
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 29
- Issue :
- 14
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 31109791
- Full Text :
- https://doi.org/10.1016/j.bmcl.2019.04.050