Targeting protein kinase Ck2alpha from outside the active site (360G-Wellcome-107714_Z_15_Z)

It is estimates that half of the people born after 1960 will be affected by one or another type of cancer during their lifetime. These are complex, heterogeneous and hard to treat diseases with significant impact on the society and novel therapeutic solutions are desperately needed. Different types of cancers, due to their genetic heterogeneity, require different, specialised treatments, and many cancers have no effective therapies. We hope to contribute to the fight against cancer by targeting a ubiquitous, constitutively active protein kinase CK2a that promotes cellular survival and suppresses apoptosis. We have identified new binding sites for small molecule inhibitors in Ck2a and will exploit this finding to develop more potent inhibitors with novel mechanism of inhibition and better specificity than currently available CK2a inhibitor in clinical trials. We will use structure-guided drug design to achieve this goal, and to obtain proof-of-concept data to support future funding applications to progress these molecules towards clinical candidates.