p21活化激酶抑制剂的最新进展。

Natalia Coleman, Joseph Kissil
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引用次数: 21

摘要

p21活化激酶(PAKs)是Rac和cdc42家族小g蛋白的下游效应物,对细胞增殖和存活至关重要。最近的研究也证明了PAKs作为各种类型癌症的治疗靶点的前景。基于序列相似性,PAKs被分为两大类(I类和II类)。尽管PAK组可能发挥的不同作用尚未被很好地理解,但最近的努力集中在鉴定可以区分这两组的激酶抑制剂上。在这篇综述中,这些努力和新发现的抑制剂将被描述和未来的方向讨论。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Recent advances in the development of p21-activated kinase inhibitors.

Recent advances in the development of p21-activated kinase inhibitors.
The p21-activated kinases (PAKs) are downstream effectors of the small G-proteins of the Rac and cdc42 family and have been implicated as essential for cell proliferation and survival. Recent studies have also demonstrated the promise of PAKs as therapeutic targets in various types of cancers. The PAKs are divided into two major groups (group I and II) based on sequence similarities. Although the different roles the PAK groups might play are not well understood, recent efforts have focused on the identification of kinase inhibitors that can discriminate between the two groups. In this review these efforts and newly identified inhibitors will be described and future directions „discussed.
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