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Indexed by:期刊论文
Date of Publication:2017-08-01
Journal:BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Included Journals:SCIE、PubMed、Scopus
Volume:27
Issue:15
Page Number:3382-3385
ISSN No.:0960-894X
Key Words:PTP1B; Varic acid; Structure-activity relationships; Insulin-sensitizing effect; Type 2 diabetes mellitus
Abstract: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.
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