A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities
文献类型：期刊论文
| 作者 | He, Min1,2; Guan, Ni2; Gao, Wei-wei1; Liu, Qing1,2; Wu, Xiao-yan1; Ma, Da-wei3; Zhong, Da-fang2 ; Ge, Guang-bo4; Li, Chuan2; Chen, Xiao-yan2
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| 刊名 | ACTA PHARMACOLOGICA SINICA
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| 出版日期 | 2012-02 |
| 卷号 | 33期号:2页码:148-154 |
| 关键词 | type 2 diabetes glucagon-like peptide-1 non-peptidic agonist Boc5 G-protein coupled receptor |
| ISSN号 | 1671-4083 |
| DOI | 10.1038/aps.2011.169 |
| 文献子类 | Review |
| 英文摘要 | Glucagon-like peptide-1 (GLP-1)-based therapy presents a promising option for treating type 2 diabetes. However, there are several limitations relative to the peptidic GLP-1 mimetics currently on the market or under development. This concern has led to a continued interest in the search for non-peptidic agonists for GLP-1 receptor (GLP-1R). Here, we briefly review the discovery, characterization and current status of a novel class of cyclobutane-derivative-based non-peptidic agonists for GLP-1R, including Boc5 and its newly discovered analogue WB4-24. Although the oral bioavailability of such compounds still poses great challenges, the progress made so far encourages us to identify a truly 'druggable' small molecule agonist for GLP-1R. |
| WOS关键词 | PROTEIN-COUPLED RECEPTOR ; GLYCEMIC CONTROL ; EXENATIDE EXENDIN-4 ; CRYSTAL-STRUCTURE ; TREATED PATIENTS ; WEIGHT ; SULFONYLUREA ; SECRETION ; METFORMIN ; EFFICACY |
| 资助项目 | Ministry of Science and Technology of China[2009ZX09302-001] ; Ministry of Science and Technology of China[2012ZX093004011] ; Chinese Academy of Sciences[KSCX1-YW-02-2] ; Chinese Academy of Sciences[KSCX2-YW-R-17] ; Shanghai Science and Technology Development Fund[074319114] ; Shanghai Science and Technology Development Fund[08DZ2291300] ; Shanghai Science and Technology Development Fund[09DZ2291200] ; K C Wong Education Foundation[00000000] ; CAS[00000000] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4437481 |
| WOS记录号 | WOS:000300255400002 |
| 出版者 | ACTA PHARMACOLOGICA SINICA |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278199]  |
| 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.Chinese Acad Sci, Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China; 4.Chinese Acad Sci, Dalian Inst Chem Phys, Dalian 116023, Peoples R China; 5.Univ Calif Riverside, Dept Bioengn, Riverside, CA 92521 USA |
| 推荐引用方式 GB/T 7714 | He, Min,Guan, Ni,Gao, Wei-wei,et al. A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities[J]. ACTA PHARMACOLOGICA SINICA,2012,33(2):148-154. |
| APA | He, Min.,Guan, Ni.,Gao, Wei-wei.,Liu, Qing.,Wu, Xiao-yan.,...&Wang, Ming-wei.(2012).A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities.ACTA PHARMACOLOGICA SINICA,33(2),148-154. |
| MLA | He, Min,et al."A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities".ACTA PHARMACOLOGICA SINICA 33.2(2012):148-154. |
入库方式： OAI收割
来源：上海药物研究所
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