Structure and biological activity of endogenous and synthetic agonists of GPR119

A G-protein-coupled receptor, GPR119, is a promising pharmacological target for a new class of hypoglycaemic drugs with an original mechanism of action, namely, increase in the glucose-dependent incretin and insulin secretion. In 2005, the first ligands were found and in the subsequent years, a larg...

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Bibliographic Details
Published in:Russian chemical reviews 2018-02, Vol.87 (2), p.151-166
Main Authors: Tyurenkov, Ivan N., Ozerov, Alexander A., Kurkin, Denis V., Logvinova, Ekaterina O., Bakulin, Dmitry A., Volotova, Elena V., Borodin, Dmitry D.
Format: Article
Language:English
Subjects:
Biological activity
Design modifications
Diabetes mellitus
Insulin
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Summary:A G-protein-coupled receptor, GPR119, is a promising pharmacological target for a new class of hypoglycaemic drugs with an original mechanism of action, namely, increase in the glucose-dependent incretin and insulin secretion. In 2005, the first ligands were found and in the subsequent years, a large number of GPR119 agonists were synthesized in laboratories in various countries; the safest and most promising agonists have entered phase I and II clinical trials as agents for the treatment of type 2 diabetes mellitus and obesity. The review describes the major endogenous GPR119 agonists and the main trends in the design and modification of synthetic structures for increasing the hypoglycaemic activity. The data on synthetic agonists are arranged according to the type of the central core of the molecules. The bibliography includes 104 references.
ISSN:0036-021X
1468-4837
DOI:10.1070/RCR4737