Amelio Ivano, Lisitsa Andrey, Knight Richard A, Melino Gerry, Antonov Alexey V
Medical Research Council Toxicology Unit, Leicester LE1 9HN, United Kingdom.
Institute of Biomedical Chemistry of the Russian Academy of Medical Sciences, Pogodinskaya Street, Moscow, Russian Federation.
Curr Drug Targets. 2017;18(5):534-543. doi: 10.2174/1389450117666160301095233.
The major drug discovery efforts in oncology have been concentrated on the development of selective molecules that are supposed to act specifically on one anticancer mechanism by modulating a single or several closely related drug targets. However, a bird's eye view on data from multiple available bioassays implies that most approved anticancer agents do, in fact, target many more proteins with different functions. Here we will review and systematize currently available information on the targets of several anticancer drugs along with revision of their potential mechanisms of action. Polypharmacology of the current antineoplastic agents suggests that drug clinical efficacy in oncology can be achieved only via modulation of multiple cellular mechanisms.
肿瘤学领域主要的药物研发工作一直集中在开发选择性分子上，这些分子被认为通过调节单个或几个密切相关的药物靶点，特异性地作用于一种抗癌机制。然而，从多个现有生物测定的数据来看，大多数已获批的抗癌药物实际上靶向更多具有不同功能的蛋白质。在此，我们将回顾并系统整理目前关于几种抗癌药物靶点的可用信息，并对其潜在作用机制进行修订。当前抗肿瘤药物的多药理学特性表明，肿瘤学中的药物临床疗效只能通过调节多种细胞机制来实现。
