Identification of a potent salicylic acid-based inhibitor of tyrosine phosphatase PTP1B

被引：9

作者：

Haftchenary, Sina ^{[1
]}

Ball, Daniel P. ^{[1
]}

Aubry, Isabelle ^{[2
,3
]}

Landry, Melissa ^{[2
,3
]}

Shahani, Vijay M. ^{[1
]}

Fletcher, Steven ^{[1
]}

Page, Brent D. G. ^{[1
]}

Jouk, Andriana O. ^{[1
]}

Tremblay, Michel L. ^{[2
,3
]}

Gunning, Patrick T. ^{[1
]}

机构：

[1] Univ Toronto, Dept Chem, Mississauga, ON L5L 1C6, Canada

[2] McGill Univ, McGill Goodman Canc Res Ctr, Montreal, PQ H3G 1Y6, Canada

[3] McGill Univ, Dept Biochem, Montreal, PQ H3G 1Y6, Canada

来源：

MEDCHEMCOMM | 2013年 / 4卷 / 06期

基金：

加拿大自然科学与工程研究理事会; 加拿大健康研究院;

关键词：

1B INHIBITORS; INSULIN SENSITIVITY; DISCOVERY; OBESITY; DISRUPTION;

D O I：

10.1039/c3md00011g

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A screen of a library of diverse small-molecules against a subset of phosphatases identified 7b and 7c, which potently inhibit TC-PTP, PTP sigma and PTP1B with no inhibition of PTP-LAR, PRL2 A/S, MKPX or papain. In CHO-IR cells these inhibitors effectively suppress PTP1B activity restoring the insulin receptor phosphorylation levels.

引用

页码：987 / 992

页数：6

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