Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design

doi:10.1016/j.bmc.2015.05.032

	Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design
	Du, Yongli 2; Ling, Hao 2; Zhang, Meng 1; Shen, Jingkang 3; Li, Qunyi 4
刊名	BIOORGANIC & MEDICINAL CHEMISTRY
	2015-08-01
卷号	23 期号:15 页码:4891-4898
关键词	Protein tyrosine phosphatase 1B inhibitor N-(2,5-Diethoxy-phenyl)-methanesulfonamide Type 2 diabetes mellitus Insulin signaling
ISSN号	0968-0896
DOI	10.1016/j.bmc.2015.05.032
文献子类	Article
英文摘要	Fragment-docking-oriented de novel design for both the catalytic site and the C phosphotyrosine binding site led to the discovery of novel scaffold and chemical easy N-(2,5-diethoxy-phenyl)-methanesulfonamide based phosphotyrosine mimetics that when incorporated into ureas are high potent and selective inhibitors of protein tyrosine phosphatase 1B. Among them, compound 15 was shown to be the most potent PTP1B inhibitor with great selectivity over the highly homologous T-cell protein tyrosine phosphatase. (C) 2015 Elsevier Ltd. All rights reserved.
资助项目	National Natural Science Foundation of China[81202389] ; National Natural Science Foundation of China[81302853]
WOS关键词	TYROSINE-PHOSPHATASE 1B ; PHOSPHOTYROSINE BINDING-SITE ; PROTEIN ; GLUCOSE ; OBESITY ; PROTEIN-TYROSINE-PHOSPHATASE-1B ; IDENTIFICATION ; STRATEGY ; RECEPTOR ; ACIDS
WOS研究方向	Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000358440000081
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/276455]
专题	药物化学研究室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	Du, Yongli
作者单位	1.Brunswick Labs China, Suzhou 215021, Peoples R China; 2.Qilu Univ Technol, Sch Chem & Pharmaceut Engn, Jinan 250353, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 4.Fudan Univ, Huashan Hosp, Clin Pharm Lab, Shanghai 200040, Peoples R China
推荐引用方式 GB/T 7714	Du, Yongli,Ling, Hao,Zhang, Meng,et al. Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2015,23(15):4891-4898.
APA	Du, Yongli,Ling, Hao,Zhang, Meng,Shen, Jingkang,&Li, Qunyi.(2015).Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design.BIOORGANIC & MEDICINAL CHEMISTRY,23(15),4891-4898.
MLA	Du, Yongli,et al."Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design".BIOORGANIC & MEDICINAL CHEMISTRY 23.15(2015):4891-4898.