Bioscience, Oncology, IMED Biotech Unit, AstraZeneca, Cambridge, U.K.
Biochem Soc Trans. 2018 Oct 19;46(5):1303-1311. doi: 10.1042/BST20170529. Epub 2018 Aug 28.
Oncogenic mutations in genes underlie the pathogenesis of many human tumours, and there has been intense effort for over 30 years to develop effective and tolerated targeted therapeutics for patients with Ras-driven cancers. This review summarises the progress made in Ras drug discovery, highlighting some of the recent developments in directly targeting Ras through advances in small molecule drug design and novel therapeutic strategies.
基因中的致癌突变是许多人类肿瘤发病机制的基础,30 多年来,人们一直致力于为 Ras 驱动型癌症患者开发有效且耐受的靶向治疗药物。本文总结了 Ras 药物发现方面的进展,重点介绍了通过小分子药物设计和新型治疗策略方面的进展,直接靶向 Ras 取得的一些最新进展。