Cyclobutane Derivatives As Novel Nonpeptidic Small Molecule Agonists of Glucagon-Like Peptide-1 Receptor

doi:10.1021/jm201150j

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	Cyclobutane Derivatives As Novel Nonpeptidic Small Molecule Agonists of Glucagon-Like Peptide-1 Receptor
	Liu, Qing 1; Li, Na 1; Yuan, Yunyun 1; Lu, Huili 1; Wu, Xiaoyan 1; Zhou, Caihong 1,2; He, Min 1,2; Su, Haoran 1; Zhang, Meng 1; Wang, Jia1
刊名	JOURNAL OF MEDICINAL CHEMISTRY
	2012-01-12
卷号	55 期号:1 页码:250-267
ISSN号	0022-2623
DOI	10.1021/jm201150j
文献子类	Article
英文摘要	A novel cyclobutane class of nonpeptidic glucagon-like peptide-1 (GLP-1) receptor agonists, exemplified by 3, was identified using receptor binding and multiple response element/cAMP response element (MRE/CRE)-driven reporter gene assays. The structures of 3 and its three isomers were elucidated by NMR, HRESIMS, and X-ray crystallography. A series of structural modifications were also made based on the core structure of 3 with different substitution groups at the west and east ends. Among these analogues, compound 16 was found to be 4- to 5-fold more potent than 3 both in vitro and in vivo.
资助项目	Ministry of Science and Technology of China[2009ZX09302-001] ; Ministry of Science and Technology of China[2012ZX09304-011] ; Chinese Academy of Sciences[KSCX1-YW-02-2] ; Chinese Academy of Sciences[KSCX2-YW-R-17] ; Natural Science Foundation of China[30628024] ; Natural Science Foundation of China[30623008] ; Shanghai Science and Technology Development Fund[074319114] ; Shanghai Science and Technology Development Fund[08DZ2291300] ; Shanghai Science and Technology Development Fund[09DZ2291200] ; CAS-Novo Nordisk[00000000]
WOS关键词	PHOTODIMERIZATION ; ACID ; EFFICACY ; THERAPY ; MICE
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000298978800019
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/278220]
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.Natl Ctr Drug Screening, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China; 4.Currenta GmbH & Co OHG, D-20833 Leverkusen, Amtsgericht Kol, Germany; 5.Bayer CropSci Aktiengesell, D-40789 Monheim, Germany
推荐引用方式 GB/T 7714	Liu, Qing,Li, Na,Yuan, Yunyun,et al. Cyclobutane Derivatives As Novel Nonpeptidic Small Molecule Agonists of Glucagon-Like Peptide-1 Receptor[J]. JOURNAL OF MEDICINAL CHEMISTRY,2012,55(1):250-267.
APA	Liu, Qing.,Li, Na.,Yuan, Yunyun.,Lu, Huili.,Wu, Xiaoyan.,...&Wang, Ming-Wei.(2012).Cyclobutane Derivatives As Novel Nonpeptidic Small Molecule Agonists of Glucagon-Like Peptide-1 Receptor.JOURNAL OF MEDICINAL CHEMISTRY,55(1),250-267.
MLA	Liu, Qing,et al."Cyclobutane Derivatives As Novel Nonpeptidic Small Molecule Agonists of Glucagon-Like Peptide-1 Receptor".JOURNAL OF MEDICINAL CHEMISTRY 55.1(2012):250-267.