​​Many pathologies, such as cancer, are linked to the dysregulation of the CK2 protein kinase, which is why medical research aims to inhibit it. However, the CK2 inhibitors developed to date have a lack of specificity potentially targeting several other protein kinases, which can be a source of side-effects.

Researchers at IRIG and the Faculty of Pharmacy in Lyon have synthetized and characterized the AB668 molecule​ which inhibits CK2 activity with a high degree of specificity. This bivalent molecule binds simultaneously to the catalytic site of CK2 and to an adjacent hydrophobic pocket, giving it a unique inhibition mechanism (Figure A).
​ What's more, AB668 has no adverse side-effects because it induces apoptotic death in numerous cell lines derived from aggressive cancers (kidney, breast, melanoma, pancreas, colon), while sparing healthy cells (Figure B).

The AB668 molecule could therefore be a promising new anti-cancer agent. The next step will be to test the molecule, after optimization by medicinal chemistry, in pre-clinical models of various cancers.​
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Figure A: An allosteric inhibitor of CK2 with anti-cancer properties. A) AB668 is a bivalent molecule that inhibits CK2 activity by binding simultaneously with high affinity (Kd: 86 nM) to its catalytic site and to an adjacent hydrophobic pocket.
Figure ​B: AB668 induces tumour cell death by apoptosis while preserving healthy cells. Credit CEA​