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题名: A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities
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;  Yang, Ling4;  Liao, Jia-yu5;  Wang, Ming-wei1, 2
关键词: type 2 diabetes ;  glucagon-like peptide-1 ;  non-peptidic agonist ;  Boc5 ;  G-protein coupled receptor
刊名: ACTA PHARMACOLOGICA SINICA
发表日期: 2012-02-01
DOI: 10.1038/aps.2011.169
卷: 33, 期:2, 页:148-154
收录类别: SCI
文章类型: Review
WOS标题词: Science & Technology ;  Physical Sciences ;  Life Sciences & Biomedicine
类目[WOS]: Chemistry, Multidisciplinary ;  Pharmacology & Pharmacy
研究领域[WOS]: Chemistry ;  Pharmacology & Pharmacy
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.
关键词[WOS]: PROTEIN-COUPLED RECEPTOR ;  GLYCEMIC CONTROL ;  EXENATIDE EXENDIN-4 ;  CRYSTAL-STRUCTURE ;  TREATED PATIENTS ;  WEIGHT ;  SULFONYLUREA ;  SECRETION ;  METFORMIN ;  EFFICACY
语种: 英语
WOS记录号: WOS:000300255400002
Citation statistics: 
内容类型: 期刊论文
URI标识: http://cas-ir.dicp.ac.cn/handle/321008/142989
Appears in Collections:中国科学院大连化学物理研究所_期刊论文

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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

Recommended Citation:
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.
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