3-Aryl-N-aminoylsulfonylphenyl-1H-pyrazole-5-carboxamides: a new class of selective Rac inhibitors

被引：23

作者：

Ferri, Nicola ^{[1
]}

Bernini, Sergio Kevin ^{[1
]}

Corsini, Alberto ^{[1
]}

Clerici, Francesca ^{[2
]}

Erba, Emanuela ^{[2
]}

Stragliotto, Stefano ^{[2
]}

Contini, Alessandro ^{[2
]}

机构：

[1] Univ Milan, Dipartimento Sci Farmacol & Biomol, I-20133 Milan, Italy

[2] Univ Milan, Dipartimento Sci Farmaceut, Sez Chim Gen & Organ A Marchesini, I-20133 Milan, Italy

来源：

MEDCHEMCOMM | 2013年 / 4卷 / 03期

关键词：

SMALL-MOLECULE INHIBITOR; VASCULAR-PERMEABILITY; GTPASE; ACTIVATION; INTEGRINS; ADHESION; PATHWAY; RHO;

D O I：

10.1039/c2md20328f

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：

Through a computational approach, five new compounds with potent and selective Rac inhibitory activity were identified. In particular, compound 4 was shown to selectively inhibit Rac activity in a concentration-dependent manner by affecting the GEF-dependent GDP-GTP exchange. This compound was more potent than the original inhibitors previously identified.

引用

页码：537 / 541

页数：5

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