小分子激酶药物的演变
Evolution of Small Molecule Kinase Drugs.
作者信息
Lightfoot Helen L, Goldberg Frederick W, Sedelmeier Joerg
机构信息
IMED Biotech Unit,Discovery Sciences, AstraZeneca, Alderley Park SK10 4TG, U.K.
Oncology, IMED Biotech Unit, Medicinal Chemistry, AstraZeneca, Cambridge CB4 0WG, U.K.
出版信息
ACS Med Chem Lett. 2018 Dec 18;10(2):153-160. doi: 10.1021/acsmedchemlett.8b00445. eCollection 2019 Feb 14.
Abstract
The development of small molecule kinase drugs is a rapidly evolving field and represents one of the most important research areas within oncology. This innovation letter provides an overview and analysis of approved kinase drugs according to their WHO registration (INN) dates, primary biological targets, and selectivity and structural similarities, which are also depicted in an associated poster. It also discusses new trends in kinase drug discovery programs such as new kinase targets, novel mechanisms of action, and diverse indications.
摘要
小分子激酶药物的研发是一个快速发展的领域，也是肿瘤学中最重要的研究领域之一。本创新快报根据世界卫生组织注册（国际非专利名称）日期、主要生物学靶点以及选择性和结构相似性，对已批准的激酶药物进行了概述和分析，相关海报中也有展示。此外，还讨论了激酶药物发现项目的新趋势，如新的激酶靶点、新的作用机制和多样的适应症。
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