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个人信息Personal Information
副教授
博士生导师
硕士生导师
性别：男
毕业院校：中国协和医科大学
学位：博士
所在单位：生物工程学院
学科：生物化工. 微生物学. 微生物与生化药学
办公地点：辽宁省大连市高新园区凌工路2号大连理工大学西部校区生物工程学院309室
联系方式：辽宁省大连市高新园区凌工路2号大连理工大学生物工程学院
电子邮箱：yshdong@dlut.edu.cn
Varic acid analogues from fungus as PTP1B inhibitors: Biological evaluation and structure-activity relationships
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论文类型：期刊论文
发表时间：2017-08-01
发表刊物：BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
收录刊物：SCIE、PubMed、Scopus
卷号：27
期号：15
页面范围：3382-3385
ISSN号：0960-894X
关键字：PTP1B; Varic acid; Structure-activity relationships; Insulin-sensitizing effect; Type 2 diabetes mellitus
摘要：Protein tyrosine phosphatase 1B ( PTP1B) inhibitors as potential therapies for diabetes and obesity have attracted much attention in recent years. Six varic acid analogues were isolated from two strains of fungi and evaluated for PTP1B inhibition activities. The structure-activity relationships were also characterized and predicted by molecular modeling. Further kinetic studies indicated the reversible and competitive inhibition manner of varic acid analogues. Trivaric acid showed insulin-sensitizing effect not only in vitro but also in vivo, representing a promising lead compound for further optimization. (C) 2017 Elsevier Ltd. All rights reserved.