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癌症研究与治疗中的极光激酶抑制剂。

The Aurora kinase inhibitors in cancer research and therapy.

作者信息

Cicenas Jonas

机构信息

CALIPHO Group, Swiss Institute of Bioinformatics, CMU-1, rue Michel Servet, 1211, Geneva 4, Switzerland.

MAP Kinase Resource, Melchiorstrasse 9, 3027, Bern, Switzerland.

出版信息

J Cancer Res Clin Oncol. 2016 Sep;142(9):1995-2012. doi: 10.1007/s00432-016-2136-1. Epub 2016 Mar 1.

Abstract

Compounds that affect enzymatic function of kinases are valuable for the understanding of the complex biochemical processes in cells. Aurora kinases (AURKs) play a key role in the control of the mitosis. These kinases are frequently deregulated in different human cancers: overexpression, amplifications, translocations and deletions were reported in many cancer cell lines as well as patient tissues. These findings steered a rigorous hunt for small-molecule AURK inhibitors not only for research purposes as well as for therapeutic uses. In this review, we describe a number of AURK inhibitors and their use in cancer research and/or therapy. We hope to assist researchers and clinicians in deciding which inhibitor is most appropriate for their specific purpose. The review will also provide a broad overview of the clinical studies performed with some of these inhibitors (if such studies have been performed).

摘要

影响激酶酶功能的化合物对于理解细胞内复杂的生化过程具有重要价值。极光激酶(AURKs)在有丝分裂的控制中起关键作用。这些激酶在不同的人类癌症中经常失调:在许多癌细胞系以及患者组织中都报道了过表达、扩增、易位和缺失。这些发现促使人们严格寻找小分子AURK抑制剂,不仅用于研究目的,也用于治疗用途。在本综述中,我们描述了一些AURK抑制剂及其在癌症研究和/或治疗中的应用。我们希望帮助研究人员和临床医生决定哪种抑制剂最适合他们的特定目的。本综述还将对使用其中一些抑制剂进行的临床研究(如果已进行此类研究)进行广泛概述。

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