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Bioorg. Med. Chem. Lett. · Dec 2016
ReviewGPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space.
- Cheng Chen, He Li, and Ya-Qiu Long.
- CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Shanghai 201203, China; Department of Chemistry, Shanghai University, 99 Shangda Road, Shanghai 200444, China.
- Bioorg. Med. Chem. Lett. 2016 Dec 1; 26 (23): 5603-5612.
AbstractGPR40 belongs to the GPCR family and the activation of GPR40 has been shown to induce glucose-stimulated insulin secretion (GSIS) from pancreatic beta cells as well as incretin secretion from intestinal endocrine cells. Therefore, GPR40 has emerged as a viable and promising therapeutic target for type 2 diabetes mellitus (T2DM) without the risk of hypoglycemia. However, the termination of TAK-875 in phase III clinical trials for the hepatotoxicity issue threw doubt over the long-term safety of targeting GPR40. Herein, we summarized the newly disclosed biological characteristics and the druglikeness-based structural evolution of GPR40 agonists to advance the development of GPR40-based anti-diabetic drugs.Copyright © 2016 Elsevier Ltd. All rights reserved.
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