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Updated: Oct 15, 2025
Identification of Novel CK2 Kinase Substrates Using a Versatile Biochemical Approach
Published on: February 21, 2019
Targeting CK2 in cancer: a valuable strategy or a waste of time?
Mauro Salvi1, Christian Borgo1, Lorenzo A Pinna2,3
1Deptartment Biomedical Sciences, University of Padova, Padova, Italy.
Abstract:
CK2 is a protein kinase involved in several human diseases (ranging from neurological and cardiovascular diseases to autoimmune disorders, diabetes, and infections, including COVID-19), but its best-known implications are in cancer, where it is considered a pharmacological target. Several CK2 inhibitors are available and clinical trials are underway in different cancer types. Recently, the suitability of CK2 as a broad anticancer target has been questioned by the finding that a newly developed compound, named SGC-CK2-1, which is more selective than any other known CK2 inhibitor, is poorly effective in reducing cell growth in different cancer lines, prompting the conclusion that the anticancer efficacy of CX-4945, the commonly used clinical-grade CK2 inhibitor, is to be attributed to its off-target effects. Here we perform a detailed scrutiny of published studies on CK2 targeting and a more in-depth analysis of the available data on SGC-CK2-1 vs. CX-4945 efficacy, providing a different perspective about the actual reliance of cancer cells on CK2. Collectively taken, our arguments would indicate that the pretended dispensability of CK2 in cancer is far from having been proved and warn against premature conclusions, which could discourage ongoing investigations on a potentially valuable drug target.
Insights
The protein kinase CK2 is a potential cancer target, but recent studies question its efficacy. This analysis suggests CK2
Area of Science:
- Biochemistry
- Oncology
- Pharmacology
Background:
- Protein kinase CK2 (casein kinase 2) is implicated in various human diseases, notably cancer.
- CK2 is a validated pharmacological target, with several inhibitors in clinical trials for cancer treatment.
- Recent findings challenge CK2's role as a broad anticancer target, citing poor efficacy of a selective inhibitor (SGC-CK2-1) and attributing efficacy of a clinical inhibitor (CX-4945) to off-target effects.
Purpose of the Study:
- To critically re-evaluate the published data on CK2 targeting in cancer.
- To analyze the comparative efficacy of selective (SGC-CK2-1) and clinical-grade (CX-4945) CK2 inhibitors.
- To provide a nuanced perspective on the essentiality of CK2 for cancer cell survival.
Main Methods:
- Comprehensive review of existing scientific literature on CK2 inhibitors and cancer.
- In-depth analysis of experimental data comparing SGC-CK2-1 and CX-4945 in cancer models.
- Critical assessment of the evidence supporting or refuting CK2's dispensability in cancer.
Main Results:
- The efficacy of the clinical CK2 inhibitor CX-4945 may not solely rely on direct CK2 inhibition.
- The selective inhibitor SGC-CK2-1's limited efficacy does not definitively prove CK2's dispensability in cancer.
- Evidence suggests that cancer cells may still significantly depend on CK2 activity.
Conclusions:
- The claim that CK2 is dispensable in cancer is not adequately supported by current evidence.
- Premature conclusions regarding CK2's lack of therapeutic value could hinder promising cancer research.
- Further investigation is warranted to fully elucidate CK2's role and therapeutic potential in oncology.
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