Advances in Anticancer Agents in Medicinal Chemistry

Volume: 1

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Advances in Anticancer Agents in Medicinal Chemistry is an exciting eBook series comprising a selection of updated articles previously published in the peer-reviewed journal Anti-Cancer Agents in ...
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Casein Kinase 2 (CK2) Inhibitors: Emerging Anticancer Therapeutic Agents?

Pp. 3-42 (40)

Giorgio Cozza and Stefano Moro


Protein kinase CK2 (Casein Kinase 2) is an ubiquitous, highly pleiotropic, constitutive active and essential protein kinase, with both cytosolic and nuclear localization in most mammalian cells. The holoenzyme is generally composed of two catalytic (alpha and/or alpha') and two regulatory (beta) subunits, but the free alpha/alpha' subunits are catalytically active by themselves and can be present in cells under some circumstances. CK2 catalyzes the phosphorylation of more than 300 substrates characterized by multiple acidic residues surrounding the phosphor-acceptor amino acid and, consequently, it plays a key role in several physiological and pathological processes. It’s abnormally high constitutive activity is implicated in several diseases and neoplasia, and a number of ATP competitive inhibitors of CK2 with micromolar and nanomolar in vitro activity, display a pro-apoptotic effect also in cell.


CK2, protein kinases, inhibitors, cancer, neurodegenerative diseases, viral infections


Molecular Modeling Section (MMS), Dipartimento di Scienze del Farmaco, Università di Padova, via Marzolo 5, Padova, Italy