Abstract
Cyclin-dependent kinases (CDKs) have emerged as important therapeutic targets, and a number of small molecular inhibitors acting as ATP competitors have been developed. Kinase degradation induced by proteolysis-targeting chimeras (PROTACs) provides new insights into the modulation of protein kinases, including CDKs, and represents a novel alternative approach that offers several advantages over conventional inhibitors. In the following chapters, we highlight some important features of the development of CDK PROTACs, including their efficacy and selectivity, as well as some unexpected observations.
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