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癌症治疗中的激酶抑制剂:展望未来。

Kinase inhibitors in cancer therapy: a look ahead.

作者信息

Sedlacek H H

机构信息

Aventis Pharma Deutschland GmbH, Central Biotechnology, Marburg, Germany.

出版信息

Drugs. 2000 Mar;59(3):435-76. doi: 10.2165/00003495-200059030-00004.

Abstract

The most essential kinases involved in cell membrane receptor activation, signal transduction and cell cycle control or programmed cell death and their interconnections are reviewed. In tumours, the genes of many of those kinases are mutated or amplified or the proteins are overexpressed. The use of key kinases offers the possibility to screen in vitro for synthetic small molecule kinase inhibitors. In view of the many interconnections of cellular kinases, their role in preventing or inducing programmed cell death and the possibility that a considerable number of signal transducing proteins are still unknown, cellular test systems are recommended in which the respective key kinase or one of its main partner molecules are overexpressed.

摘要

本文综述了参与细胞膜受体激活、信号转导、细胞周期调控或程序性细胞死亡及其相互联系的最重要激酶。在肿瘤中,许多此类激酶的基因发生突变或扩增,或蛋白质过度表达。关键激酶的应用为体外筛选合成小分子激酶抑制剂提供了可能。鉴于细胞激酶之间存在众多相互联系、它们在预防或诱导程序性细胞死亡中的作用以及相当数量的信号转导蛋白仍未知的可能性,建议采用细胞测试系统,其中相应的关键激酶或其主要伙伴分子之一过度表达。

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