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Updated: May 19, 2026

Identification of Novel CK2 Kinase Substrates Using a Versatile Biochemical Approach
Published on: February 21, 2019
Protein kinase CK2 inhibitors: a patent review
Giorgio Cozza1, Lorenzo A Pinna, Stefano Moro
1University of Padova, Department of Biomedical Sciences, Padova 35121, Italy.
Introduction:
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.
Areas Covered:
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.
Expert Opinion:
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.
Insights
The development of protein kinase CK2 (Casein kinase 2) modulators, particularly inhibitors, has seen a significant surge in patent filings since 2004. This reflects growing interest in CK2 inhibitors for potential therapeutic applications.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- Protein kinase CK2 (Casein kinase 2) is a crucial enzyme involved in numerous cellular processes.
- Dysregulation of CK2 activity is implicated in various diseases, including cancer, inflammation, and autoimmune disorders.
- While CK2 inhibitors have been explored for years, only CX-4945 has advanced to Phase II clinical trials.
Purpose of the Study:
- To review the historical development of CK2 activity modulators.
- To analyze the timeline of patent registrations for CK2 modulators.
- To highlight the recent increase in patent activity for CK2 inhibitors.
Main Methods:
- Literature review focusing on patent databases.
- Chronological analysis of patent filings related to CK2 modulators.
- Identification of trends in CK2 inhibitor development.
Main Results:
- CK2 was discovered in 1954, but the first patent for its modulators appeared in 2004.
- A notable increase in patent applications for CK2 inhibitors has occurred in the last five years.
- This trend indicates a renewed focus on developing CK2-targeted therapies.
Conclusions:
- The patent landscape reveals a delayed but accelerating interest in CK2 modulators.
- The recent surge in patents underscores the therapeutic potential of CK2 inhibitors.
- Further research and development in this area are anticipated.
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