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Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity 期刊论文

编号：

69f0bd26-0e6c-4846-ab3e-90b7c8bcccb3
作者：

Liu, Peihong^[1] Du, Yongli^[1] Song, Lianhua^[1] Shen, Jingkang^[2] Li, Qunyi^[3]
语种：

English
期刊：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY ISSN：0223-5234 2016 年 118 卷 (27 - 33) ; AUG 8
收录：
关键词：

Type 2 diabetes mellitus Methyl salicylate derivatives ABC type PTP1B inhibitor
摘要：

Protein tyrosine phosphatase 1B (PTP1B) as a key negative regulator of both insulin and leptin receptor pathways has been an attractive therapeutic target for the treatment of type 2 diabetes mellitus (T2DM) and obesity. With the goal of enhancing potency and selectivity of the PTP1B inhibitors, a series of methyl salicylate derivatives as ABC type PTP1B inhibitors (P1-P7) were discovered. More importantly, compound P6 exhibited high potent inhibitory activity (IC50 = 50 nM) for PTP1B with 15-fold selectivity over T-cell PTPase (TCPTP). Further studies on cellular activities revealed that compound P6 could enhance insulin-mediated insulin receptor beta (IR beta) phosphorylation and insulin-stimulated glucose uptake. (C) 2016 Elsevier Masson SAS. All rights reserved.
推荐引用方式
GB/T 7714：

Liu Peihong,Du Yongli,Song Lianhua, et al. Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity [J].EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2016,118:27-33.
APA：

Liu Peihong,Du Yongli,Song Lianhua,Shen Jingkang,&Li Qunyi.(2016).Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity .EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,118:27-33.
MLA：

Liu Peihong, et al. "Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity" .EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 118(2016):27-33.

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