Abstract:
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.
Received: 09.03.2017
Bibliographic databases:
Document Type:
Article
Language: English
Original paper language: Russian
Citation:
I. N. Tyurenkov, A. A. Ozerov, D. V. Kurkin, E. O. Logvinova, D. A. Bakulin, E. V. Volotova, D. D. Borodin, “Structure and biological activity of endogenous and synthetic agonists of GPR119”, Russian Chem. Reviews, 87:2 (2018), 151–166
\Bibitem{TyuOzeKur18}
\by I.~N.~Tyurenkov, A.~A.~Ozerov, D.~V.~Kurkin, E.~O.~Logvinova, D.~A.~Bakulin, E.~V.~Volotova, D.~D.~Borodin
\paper Structure and biological activity of endogenous and synthetic agonists of GPR119
\jour Russian Chem. Reviews
\yr 2018
\vol 87
\issue 2
\pages 151--166
\mathnet{http://mi.mathnet.ru/eng/rcr4199}
\crossref{https://doi.org/10.1070/RCR4737}
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Linking options:
https://www.mathnet.ru/eng/rcr4199
https://doi.org/10.1070/RCR4737
https://www.mathnet.ru/eng/rcr/v87/i2/p151
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D. A. Tilchenko, E. Yu. Bibik, V. V. Dotsenko, S. G. Krivokolysko, K. A. Frolov, N. A. Aksenov, I. V. Aksenova, Russ J Bioorg Chem, 50:2 (2024), 554
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L. I. Belen'kii, G. A. Gazieva, Yu. B. Evdokimenkova, N. O. Soboleva, Advances in Heterocyclic Chemistry, Vol 132, Adv. Heterocycl. Chem., Advances in Heterocyclic Chemistry, 132, ed. E. Scriven, C. Ramsden, Elsevier Academic Press Inc, 2020, 385–468
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