Upregulation of CDK8 has recently been described for colon cancer, gastric cancer, and melanoma, rendering CDK8 as an attractive target for the development of selective and efficacious anti-cancer drugs. Dr. Wegert will report on a structure-based approach that led to an induced-fit mechanism of new CDK8 inhibitors, the frontrunner of which is selective across a huge kinase panel.
The associated binding mechanism exhibits a pre-engineered kinetic signature keeping the molecular complexity of inhibitors at a minimum level. Detailed structure-kinetic relationships will be discussed.
