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A continued saga of Boc5, the first non-peptidic glucagon-like peptide-1 receptor agonist with in vivo activities
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
2012-02-01
DOI10.1038/aps.2011.169
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
关键词[WOS]PROTEIN-COUPLED RECEPTOR ; GLYCEMIC CONTROL ; EXENATIDE EXENDIN-4 ; CRYSTAL-STRUCTURE ; TREATED PATIENTS ; WEIGHT ; SULFONYLUREA ; SECRETION ; METFORMIN ; EFFICACY
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.
语种英语
WOS记录号WOS:000300255400002
引用统计
文献类型期刊论文
条目标识符http://cas-ir.dicp.ac.cn/handle/321008/142989
专题中国科学院大连化学物理研究所
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
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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.
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