Advances in Small-Molecule GPR40 Agonists for Treatment of Type 2 Diabetes Mellitus
文献类型：期刊论文
| 作者 | Li He; Long Yaqiu |
| 刊名 | CHINESE JOURNAL OF ORGANIC CHEMISTRY
 |
| 出版日期 | 2016-04 |
| 卷号 | 36期号:4页码:736-743 |
| 关键词 | type II diabetes mellitus GPR40 agonists glucose-stimulated insulin secretion phenylpropanoic acid |
| ISSN号 | 0253-2786 |
| DOI | 10.6023/cjoc201511011 |
| 文献子类 | Review |
| 英文摘要 | Currently, the majority of the chemotherapy for type 2 diabetes mellitus (T2DM) functions through glycemic control by administration of oral or injectable hypoglycemic drugs. Though a range of anti-diabetic drugs with different modes of action have been launched, there still remains a significant need for development of effective and highly safe anti-diabetic agents for the increasing diabetic population. GPR40 belongs to the GPCR family and the activation of GPR40 can amplify glucose-stimulated insulin secretion (GSIS). Due to the advantage of minimizing the hypoglycemia risk, GPR40 has drawn more and more attention and emerged as a promising new target for T2DM treatment. Therefore, the recent progress on the structural optimization and further development of small molecule GPR40 agonists as novel treatment for T2DM is reviewed, focused on those under clinical trials or at preclinical stage. A variety of small molecule GPR40 agonists were summarized from the literature and patents based on the pharmacophore model, including the critical phenylpropanoic acid core, the hydrophobic terminus and the linker. The structural features and advantage of different sources of GPR40 agonists were analyzed and highlighted. |
| WOS关键词 | 1 FFA1/GPR40 AGONIST ; IN-VITRO ; DISCOVERY ; POTENT ; ACIDS ; IDENTIFICATION ; OPTIMIZATION ; SECRETION ; TAK-875 ; CELLS |
| 资助项目 | National Natural Science Foundation of China[81325020] ; National Natural Science Foundation of China[81361120410] ; National Natural Science Foundation of China[8132109] ; National Natural Science Foundation of China[81123004] |
| WOS研究方向 | Chemistry |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5704336 |
| WOS记录号 | WOS:000376420700006 |
| 出版者 | SCIENCE PRESS |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276084]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Long Yaqiu |
| 作者单位 | Chinese Acad Sci, Shanghai Inst Mat Med, Key Lab Receptor Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li He,Long Yaqiu. Advances in Small-Molecule GPR40 Agonists for Treatment of Type 2 Diabetes Mellitus[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2016,36(4):736-743. |
| APA | Li He,&Long Yaqiu.(2016).Advances in Small-Molecule GPR40 Agonists for Treatment of Type 2 Diabetes Mellitus.CHINESE JOURNAL OF ORGANIC CHEMISTRY,36(4),736-743. |
| MLA | Li He,et al."Advances in Small-Molecule GPR40 Agonists for Treatment of Type 2 Diabetes Mellitus".CHINESE JOURNAL OF ORGANIC CHEMISTRY 36.4(2016):736-743. |
入库方式： OAI收割
来源：上海药物研究所
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