Kinetic characterisation of covalent inhibitors on the PHERAstar

Covalent drug approaches have been avoided for a long time by the pharma industry, mainly because of safety concerns.

Recently, carefully tuned reactivity of covalent compounds and specific complementarity to their targets resulted in the identification of promising drugs candidates. These show a range of advantages, particularly in the cancer field.

In this scientific talk, Dr. Agnes Martin, principal scientist at Cancer Research UK, presents biochemical strategies for the in vitro characterisation of covalent compounds. In particular, the PHERAstar plate reader was used to run kinetic binding assays. The covalent compound characterisation is illustrated by the latest discovery of a new covalent inhibitor of the, so far considered un-druggable, cancer target USP7.

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