Target intelligence / Profile preview

Casein kinase II subunit alpha (CSNK2A1) (CK2α)

Target
CK2α
Molecular classification
Enzyme, Serine/threonine-protein kinase
01

Overview

Casein kinase II subunit alpha (CK2α) is the catalytic component of the heterotetrameric Casein Kinase 2 complex, a highly conserved and constitutively active serine/threonine-protein kinase (UniProt: P68400). It plays a pivotal role in a vast array of cellular processes, including signal transduction, cell cycle progression, DNA repair, and the suppression of apoptosis (PubMed: 25108283). In many human cancers, CK2α is significantly overexpressed, creating an "addiction" state where malignant cells rely on its activity for survival and proliferation (PubMed: 24513748). This overexpression often correlates with poor prognosis and resistance to chemotherapy. Therapeutic strategies targeting CK2α primarily involve small-molecule ATP-competitive inhibitors, such as Silmitasertib, which aim to disrupt its pro-survival signaling pathways (ClinicalTrials.gov: NCT02128282). Beyond oncology, CK2α is also implicated in viral replication and neurodegenerative conditions, making it a versatile target for drug development (PubMed: 30149024).

Other names
CSNK2A1Casein kinase 2 alpha 1CKII alphaSerine/threonine-protein kinase Casein kinase II subunit alphaCK2A1
02

Mechanism of action

ATP-competitive inhibition of the catalytic subunit to prevent phosphorylation of downstream substrates (PubMed: 21148453).

03

Biological functions

Signal transductionCell cycle regulationApoptosis inhibitionCell proliferationDNA repairTranscription regulation
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Disease associations

CancerInflammationNeurodegenerative diseaseViral infection
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Safety considerations

Potential systemic toxicity due to ubiquitous expressionOff-target kinase inhibitionImpact on normal regenerative processes
06

Interacting drugs

Silmitasertib (CX-4945)

4 more in the full profile.

07

Biomarkers

CK2α protein expression levelsPhospho-Akt (Ser129)Phospho-p53 (Ser392)

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