Kinase inhibitor research is a comparatively recent branch of medicinal chemistry and pharmacology and the first small‐molecule kinase inhibitor, imatinib, was approved for clinical use only 15 years ago. Since then, 33 more kinase inhibitor drugs have received regulatory approval for the treatment of a variety of cancers and the volume of reports on the discovery and development of kinase inhibitors has increased to an extent where it is now difficult—even for those working in the field—easily to keep an overview of the compounds that are being developed, as currently there are 231 such compounds, targeting 38 different protein and lipid kinases (not counting isoforms), in clinical use or under clinical investigation. The purpose of this review is thus to provide an overview of the biomedical rationales for the kinases being targeted on the one hand, and the design principles, as well as chemical, pharmacological, pharmaceutical, and toxicological kinase inhibitor properties, on the other hand. Two issues that are especially important in kinase inhibitor research, target selectivity and drug resistance, as well as the underlying structural concepts, are discussed in general terms and in the context of relevant kinases and their inhibitors.

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批准和实验性的小分子肿瘤激酶抑制剂药物：2016年中期概述

激酶抑制剂研究是药物化学和药理学中一个相对较新的分支，并且第一个小分子激酶抑制剂伊马替尼仅在15年前被批准用于临床。此后，又有33种激酶抑制剂药物获得了治疗多种癌症的监管批准，关于激酶抑制剂的发现和开发的报告数量也增加到了现在的程度，即使对于那些从事激酶抑制剂研究的人来说也是如此。领域-轻松概述正在开发的化合物，因为目前有231种此类化合物在临床使用或临床研究中以38种不同的蛋白质和脂质激酶（不包括异构体）为目标。因此，本综述的目的是一方面提供针对靶激酶的生物医学原理的概述，另一方面提供设计原理以及化学，药理，药物和毒理学激酶抑制剂的特性。在激酶抑制剂研究中一般性地以及在相关激酶及其抑制剂的背景下讨论了两个在激酶抑制剂研究中特别重要的问题，即靶标选择性和耐药性以及潜在的结构概念。