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Current Medicinal Chemistry


ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

The Dark Side of Protein Kinase CK2 Inhibition

Author(s): G. Cozza, F. Meggio and S. Moro

Volume 18 , Issue 19 , 2011

Page: [2867 - 2884] Pages: 18

DOI: 10.2174/092986711796150423

Price: $65


Casein kinase 2 (CK2) is a ubiquitous, highly pleiotropic and essential protein kinase whose abnormally high constitutive activity has been implicated in several human diseases. In the last decade, several ATP competitive inhibitors of CK2, characterized by an in vitro activity that ranges from micromolar to nanomolar, have been discovered. However, until now only one drug candidate has been entered in Phase I clinical trial as a potential anticancer drug. Why this constitutively active kinase is so undruggable? Can ATP competitive inhibitors be considered the most promising drug candidates for the near future?

In this review, we would like to underline how targeting binding sites outside the conventional ATP-binding could represent a new promising strategy to inhibit CK2 activity and, consequently, bear a great potentiality in discovering new drug candidates.

Keywords: Protein kinase CK2, Kinase Inhibitors, CK2 in human diseases

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