Thu, 23 Nov 2017, 16:00 CET (Berlin)

Dr. Anita Wegert, Mercachem BV, Nijmegen, The Netherlands

CDK8 inhibitors — long residence time by design (canceled)

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.

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