Fullerene derivatives as a new class of inhibitors of protein tyrosine phosphatases

被引：22

作者：

Kobzar, Oleksandr L. ^{[1
]}

Trush, Viacheslav V. ^{[1
]}

Tanchuk, Vsevolod Yu ^{[1
]}

Zhilenkov, Alexander V. ^{[2
]}

Troshin, Pavel A. ^{[2
]}

Vovk, Andriy I. ^{[1
]}

机构：

[1] Natl Acad Sci Ukraine, Inst Bioorgan Chem & Petrochem, UA-02660 Kiev 94, Ukraine

[2] Russian Acad Sci, Inst Problems Chem Phys, Chernogolovka 142432, Moscow Region, Russia

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 14期

基金：

俄罗斯基础研究基金会;

关键词：

Protein tyrosine phosphatase; Fullerene; Inhibition; Molecular docking; METHYLENEBISPHOSPHONIC ACIDS; POLYMERASE INHIBITION; SELECTIVE INHIBITORS; STRUCTURAL BASIS; POTENT; PTP1B; DESIGN; ALPHA; CD45; TOXICITY;

D O I：

10.1016/j.bmcl.2014.04.110

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In this study, we identified water-soluble C-60 and C-70 fullerene derivatives as a novel class of protein tyrosine phosphatase inhibitors. The evaluated compounds were found to inhibit CD45, PTP1B, TC-PTP, SHP2, and PTPB with IC50 values in the low micromolar to high nanomolar range. These results demonstrate a new strategy for designing effective nanoscale protein tyrosine phosphatase inhibitors. (C) 2014 Elsevier Ltd. All rights reserved.

引用

页码：3175 / 3179

页数：5

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