GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space
文献类型：期刊论文
| 作者 | Chen, Cheng1,2; Li, He2; Long, Ya-Qiu2 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2016-12-01 |
| 卷号 | 26期号:23页码:5603-5612 |
| 关键词 | GPR40 Glucose-stimulated insulin secretion Type 2 diabetes FFA1 Biased agonism |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2016.10.074 |
| 文献子类 | Article |
| 英文摘要 | GPR40 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. (C) 2016 Elsevier Ltd. All rights reserved. |
| WOS关键词 | ACID RECEPTOR 1 ; PROTEIN-COUPLED RECEPTORS ; INSULIN-SECRETION ; LOW LIPOPHILICITY ; FULL AGONISTS ; FATTY-ACIDS ; IN-VIVO ; DISCOVERY ; POTENT ; EFFICACY |
| 资助项目 | National Natural Science Foundation of China[81325020] ; "Personalized Medicines-Molecular Signature-based Drug Discovery and Development", Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12040311] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000389519100001 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/275785]  |
| 专题 | 上海药物代谢研究中心 药物化学研究室 |
| 通讯作者 | Long, Ya-Qiu |
| 作者单位 | 1.Shanghai Univ, Dept Chem, 99 Shangda Rd, Shanghai 200444, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Chen, Cheng,Li, He,Long, Ya-Qiu. GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2016,26(23):5603-5612. |
| APA | Chen, Cheng,Li, He,&Long, Ya-Qiu.(2016).GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,26(23),5603-5612. |
| MLA | Chen, Cheng,et al."GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 26.23(2016):5603-5612. |
入库方式： OAI收割
来源：上海药物研究所
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