Literature DB >> 21361292

Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.

Kim F McClure1, Etzer Darout, Cristiano R W Guimarães, Michael P DeNinno, Vincent Mascitti, Michael J Munchhof, Ralph P Robinson, Jeffrey Kohrt, Anthony R Harris, Dianna E Moore, Bryan Li, Lacey Samp, Bruce A Lefker, Kentaro Futatsugi, Daniel Kung, Paul D Bonin, Peter Cornelius, Ruduan Wang, Eben Salter, Sam Hornby, Amit S Kalgutkar, Yue Chen.   

Abstract

The synthesis and properties of the bridged piperidine (oxaazabicyclo) compounds 8, 9, and 11 are described. A conformational analysis of these structures is compared with the representative GPR119 ligand 1. These results and the differences in agonist pharmacology are used to formulate a conformation-based hypothesis to understand activation of the GPR119 receptor. We also show for these structures that the agonist pharmacology in rat masks the important differences in human pharmacology.

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Year:  2011        PMID： 21361292     DOI： 10.1021/jm200003p

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  7 in total

1.  Discovery of MK-8282 as a Potent G-Protein-Coupled Receptor 119 Agonist for the Treatment of Type 2 Diabetes.

Authors:  Santhosh F Neelamkavil; Andrew W Stamford; Timothy Kowalski; Dipshikha Biswas; Craig Boyle; Samuel Chackalamannil; Yan Xia; Charles Jayne; Bernard Neustadt; Jinsong Hao; Hong Liu; Xing Dai; Hana Baker; Brian Hawes; Kim O'Neill; Huadong Tang; William J Greenlee
Journal:  ACS Med Chem Lett       Date:  2018-04-10       Impact factor: 4.345

2.  Isoprenoid Derivatives of Lysophosphatidylcholines Enhance Insulin and GLP-1 Secretion through Lipid-Binding GPCRs.

Authors:  Anna Drzazga; Daria Kamińska; Anna Gliszczyńska; Edyta Gendaszewska-Darmach
Journal:  Int J Mol Sci       Date:  2021-05-27       Impact factor: 5.923

Review 3.  Pharmacology and physiology of gastrointestinal enteroendocrine cells.

Authors:  O J Mace; B Tehan; F Marshall
Journal:  Pharmacol Res Perspect       Date:  2015-07-07

4.  Glucose-lowering effects and safety of DS-8500a, a G protein-coupled receptor 119 agonist, in Japanese patients with type 2 diabetes: results of a randomized, double-blind, placebo-controlled, parallel-group, multicenter, phase II study.

Authors:  Nobuya Inagaki; Hubert S Chou; Shuji Tsukiyama; Takuo Washio; Kazuhito Shiosakai; Yasuhiko Nakatsuka; Takashi Taguchi
Journal:  BMJ Open Diabetes Res Care       Date:  2017-09-29

5.  Efficacy and Safety of GPR119 Agonist DS-8500a in Japanese Patients with Type 2 Diabetes: a Randomized, Double-Blind, Placebo-Controlled, 12-Week Study.

Authors:  Yuichiro Yamada; Yasuo Terauchi; Hirotaka Watada; Yasuhiko Nakatsuka; Kazuhito Shiosakai; Takuo Washio; Takashi Taguchi
Journal:  Adv Ther       Date:  2018-02-27       Impact factor: 3.845

6.  Lysophosphatidylcholine Containing Anisic Acid Is Able to Stimulate Insulin Secretion Targeting G Protein Coupled Receptors.

Authors:  Anna Drzazga; Marta Okulus; Magdalena Rychlicka; Łukasz Biegała; Anna Gliszczyńska; Edyta Gendaszewska-Darmach
Journal:  Nutrients       Date:  2020-04-22       Impact factor: 5.717

7.  Formation of βTC3 and MIN6 Pseudoislets Changes the Expression Pattern of Gpr40, Gpr55, and Gpr119 Receptors and Improves Lysophosphatidylcholines-Potentiated Glucose-Stimulated Insulin Secretion.

Authors:  Anna Drzazga; Eliza Cichońska; Maria Koziołkiewicz; Edyta Gendaszewska-Darmach
Journal:  Cells       Date:  2020-09-09       Impact factor: 6.600
  7 in total

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