Landmark studies on the glucagon subfamily of GPCRs: from small molecule modulators to a crystal structure
文献类型：期刊论文
| 作者 | Yang, De-hua ; Zhou, Cai-hong; Liu, Qing; Wang, Ming-wei1,2
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| 刊名 | ACTA PHARMACOLOGICA SINICA
 |
| 出版日期 | 2015-09 |
| 卷号 | 36期号:9页码:1033-1042 |
| 关键词 | class B GPCR GLP-1R GCGR small molecule modulators crystal structure type 2 diabetes mellitus |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2015.78 |
| 文献子类 | Review |
| 英文摘要 | The glucagon subfamily of class B G-protein-coupled receptors (GPCRs) has been proposed to be a crucial drug target for the treatment of type 2 diabetes. The challenges associated with determining the crystal structures of class B GPCRs relate to their large amino termini and the lack of available small molecule ligands to stabilize the receptor proteins. Following our discovery of non-peptidic agonists for glucagon-like peptide-1 receptor (GLP-1R) that have therapeutic effects, we initiated collaborative efforts in structural biology and recently solved the three-dimensional (3D) structure of the human glucagon receptor (GCGR) 7-transmembrane domain, providing in-depth information about the underlying signaling mechanisms. In this review, some key milestones in this endeavor are highlighted, including discoveries of small molecule ligands, their roles in receptor crystallization, conformational changes in transmembrane domains (TMDs) upon activation and structure-activity relationship analyses. |
| WOS关键词 | PROTEIN-COUPLED-RECEPTOR ; CORTICOTROPIN-RELEASING-FACTOR ; CLASS-B GPCRS ; VASOACTIVE-INTESTINAL-PEPTIDE ; TYPE-2 DIABETES-MELLITUS ; EXTRACELLULAR DOMAIN ; DRUG DISCOVERY ; MESSENGER-RNA ; HORMONE ; RECOGNITION |
| 资助项目 | National Health and Family Planning Commission[2012ZX09304-011] ; National Health and Family Planning Commission[2013ZX09401003-005] ; National Health and Family Planning Commission[2013ZX09507001] ; National Health and Family Planning Commission[2013ZX09507002] ; Shanghai Science and Technology Fund[12ZR1406900] ; Shanghai Science and Technology Fund[13DZ2290300] ; Shanghai Science and Technology Fund[15DZ2291600] ; CAS-Novo Nordisk Research Fund[00000000] ; Thousand Talents Program in China[00000000] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5510630 |
| WOS记录号 | WOS:000360840200001 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276415]  |
| 专题 | 国家新药筛选中心 |
| 通讯作者 | Wang, Ming-wei |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yang, De-hua,Zhou, Cai-hong,Liu, Qing,et al. Landmark studies on the glucagon subfamily of GPCRs: from small molecule modulators to a crystal structure[J]. ACTA PHARMACOLOGICA SINICA,2015,36(9):1033-1042. |
| APA | Yang, De-hua,Zhou, Cai-hong,Liu, Qing,&Wang, Ming-wei.(2015).Landmark studies on the glucagon subfamily of GPCRs: from small molecule modulators to a crystal structure.ACTA PHARMACOLOGICA SINICA,36(9),1033-1042. |
| MLA | Yang, De-hua,et al."Landmark studies on the glucagon subfamily of GPCRs: from small molecule modulators to a crystal structure".ACTA PHARMACOLOGICA SINICA 36.9(2015):1033-1042. |
入库方式： OAI收割
来源：上海药物研究所
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