Cyclobutane Derivatives As Novel Nonpeptidic Small Molecule Agonists of Glucagon-Like Peptide-1 Receptor
文献类型：期刊论文
| 作者 | Liu, Qing1; Li, Na1; Yuan, Yunyun1; Lu, Huili1; Wu, Xiaoyan1; Zhou, Caihong1,2; He, Min1,2; Su, Haoran1; Zhang, Meng1; Wang, Jia1
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| 刊名 | JOURNAL OF MEDICINAL CHEMISTRY
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| 出版日期 | 2012-01-12 |
| 卷号 | 55期号:1页码:250-267 |
| ISSN号 | 0022-2623 |
| DOI | 10.1021/jm201150j |
| 文献子类 | Article |
| 英文摘要 | A novel cyclobutane class of nonpeptidic glucagon-like peptide-1 (GLP-1) receptor agonists, exemplified by 3, was identified using receptor binding and multiple response element/cAMP response element (MRE/CRE)-driven reporter gene assays. The structures of 3 and its three isomers were elucidated by NMR, HRESIMS, and X-ray crystallography. A series of structural modifications were also made based on the core structure of 3 with different substitution groups at the west and east ends. Among these analogues, compound 16 was found to be 4- to 5-fold more potent than 3 both in vitro and in vivo. |
| WOS关键词 | PHOTODIMERIZATION ; ACID ; EFFICACY ; THERAPY ; MICE |
| 资助项目 | Ministry of Science and Technology of China[2009ZX09302-001] ; Ministry of Science and Technology of China[2012ZX09304-011] ; Chinese Academy of Sciences[KSCX1-YW-02-2] ; Chinese Academy of Sciences[KSCX2-YW-R-17] ; Natural Science Foundation of China[30628024] ; Natural Science Foundation of China[30623008] ; Shanghai Science and Technology Development Fund[074319114] ; Shanghai Science and Technology Development Fund[08DZ2291300] ; Shanghai Science and Technology Development Fund[09DZ2291200] ; CAS-Novo Nordisk[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000298978800019 |
| 出版者 | AMER CHEMICAL SOC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278220]  |
| 专题 | 国家新药筛选中心 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Wang, Ming-Wei |
| 作者单位 | 1.Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China; 4.Currenta GmbH & Co OHG, D-20833 Leverkusen, Amtsgericht Kol, Germany; 5.Bayer CropSci Aktiengesell, D-40789 Monheim, Germany |
| 推荐引用方式 GB/T 7714 | Liu, Qing,Li, Na,Yuan, Yunyun,et al. Cyclobutane Derivatives As Novel Nonpeptidic Small Molecule Agonists of Glucagon-Like Peptide-1 Receptor[J]. JOURNAL OF MEDICINAL CHEMISTRY,2012,55(1):250-267. |
| APA | Liu, Qing.,Li, Na.,Yuan, Yunyun.,Lu, Huili.,Wu, Xiaoyan.,...&Wang, Ming-Wei.(2012).Cyclobutane Derivatives As Novel Nonpeptidic Small Molecule Agonists of Glucagon-Like Peptide-1 Receptor.JOURNAL OF MEDICINAL CHEMISTRY,55(1),250-267. |
| MLA | Liu, Qing,et al."Cyclobutane Derivatives As Novel Nonpeptidic Small Molecule Agonists of Glucagon-Like Peptide-1 Receptor".JOURNAL OF MEDICINAL CHEMISTRY 55.1(2012):250-267. |
入库方式： OAI收割
来源：上海药物研究所
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