Protein kinase CK2 inhibitors: a patent review.
BACKGROUND
CK2 is a pleiotropic, ubiquitous and constitutively active protein kinase, localized in both cytosolic and nuclear compartments, where it catalyzes the phosphorylation of hundreds of proteins. CK2 is generally described as a tetramer composed of two catalytic (α and/or α') and two regulatory subunits (β), however, the free α/α' subunits are catalytically active by themselves. CK2 plays a key role in several physiological and pathological processes and has been connected to many neoplastic, inflammatory, autoimmune and infectious disorders. In the last 20 years, several inhibitors of CK2 have been discovered though only one of these, CX-4945, has recently entered into Phase II clinical trials as potential anticancer drug.


METHODS
The main objective of the present review is to describe the development of CK2 activity modulators over the years according to the timeline of their patent registration.


CONCLUSIONS
CK2 was discovered in 1954, but the first patent on CK2 modulators was deposited only 50 years later, in 2004. However, in the last 5 years an increasing number of patents on CK2 inhibitors have been registered, reflecting an increased interest in this kind of drug candidates and their possible therapeutic applications.
University of Padova, Department of Biomedical Sciences, Padova 35121, Italy.
Giorgio
G
Cozza
Lorenzo A
LA
Pinna
Stefano
S
Moro
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology; D047390:Casein Kinase II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017322:Clinical Trials, Phase II as Topic; D015195:Drug Design; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000473:pathology; D010330:Patents as Topic; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*
D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D047390:Casein Kinase II