Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists
文献类型：期刊论文
| 作者 | Li, Jia1,2,3,4 ; Feng, Yang5; Li, Huihui2,3,4; Shu, Shuangjie2,3,4; Dai, Antao5; Cai, Xiaoqing5; Wang, Jiang2,3,4; Yang, Dehua3,4,5; Ma, Dakota5; Wang, Ming-Wei3,4,5
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| 刊名 | CHEMICAL BIOLOGY & DRUG DESIGN
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| 出版日期 | 2018-07 |
| 卷号 | 92期号:1页码:1241-1254 |
| 关键词 | biaryl amide glucagon receptor antagonist molecular simulation |
| ISSN号 | 1747-0277 |
| DOI | 10.1111/cbdd.13184 |
| 文献子类 | Article |
| 英文摘要 | A novel series of thiophene-containing biaryl amide glucagon receptor (GCGR) antagonists were designed and synthesized. Two compounds of this series, 14f and 14h, exhibited good GCGR binding (IC50=6.1 and 4.4m, respectively) and cAMP functional activities (IC50=4.4 and 14.4m, respectively). The possible binding modes of compounds 14f and 14h with GCGR were explored by molecular simulation. |
| WOS关键词 | TYPE-2 DIABETES-MELLITUS ; GLUCOSE ; METABOLISM ; EXCRETION ; AGONISTS |
| 资助项目 | National Natural Science Foundation of China[21632008] ; National Natural Science Foundation of China[81620108027] ; National Natural Science Foundation of China[21672231] ; National Natural Science Foundation of China[21472209] ; Major Project of Chinese National Programs for Fundamental Research and Development[2015CB910304] ; SA-SIBS Scholarship Program[00000000] ; Shanghai Science and Technology Development Fund[15DZ2291600] ; Shanghai Science and Technology Development Fund[15QA1404400] ; Thousand Talents Program in China[00000000] ; Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12040201] ; Strategic Priority Research Program of the Chinese Academy of Sciences[XDA12040202] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000436403500008 |
| 出版者 | WILEY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279686]  |
| 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 药物化学研究室 药物安全性评价中心 |
| 通讯作者 | Wang, Ming-Wei; Liu, Hong |
| 作者单位 | 1.China Pharmaceut Univ, Sch Pharm, Nanjing, Jiangsu, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai, Peoples R China; 4.Univ Chinese Acad Sci, Beijing, Peoples R China; 5.Natl Ctr Drug Screening, Shanghai, Peoples R China |
| 推荐引用方式 GB/T 7714 | Li, Jia,Feng, Yang,Li, Huihui,et al. Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2018,92(1):1241-1254. |
| APA | Li, Jia.,Feng, Yang.,Li, Huihui.,Shu, Shuangjie.,Dai, Antao.,...&Liu, Hong.(2018).Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists.CHEMICAL BIOLOGY & DRUG DESIGN,92(1),1241-1254. |
| MLA | Li, Jia,et al."Discovery of thiophene-containing biaryl amide derivatives as novel glucagon receptor antagonists".CHEMICAL BIOLOGY & DRUG DESIGN 92.1(2018):1241-1254. |
入库方式： OAI收割
来源：上海药物研究所
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