Protein kinase CK2 sustains de novo fatty acid synthesis by regulating the expression of SCD-1 in human renal cancer cells.

Background: Clear cell renal cell carcinoma (ccRCC) is a type of cancer characterized by a vast intracellular accumulation of lipids that are critical to sustain growth and viability of the cells in the tumour microenvironment. Stearoyl-CoA 9-desaturase 1 (SCD-1) is an essential enzyme for the synthesis of monounsaturated fatty acids and consistently overexpressed in all stages of ccRCC growth.

Methods: Human clear cell renal cell carcinoma lines were treated with small-molecule inhibitors of protein kinase CK2.

Towards the CSNK2 phosphoproteome - With lessons from the COVID-19 pandemic to revealing the secrets of CSNK2 and its promise as a therapeutic target.

Dramatic advances in phosphoproteomics and the development of a selective chemical probe have presented new opportunities for revealing the cellular landscape of substrates for CSNK2 (formerly known as CK2 or casein kinase II). In addition to deciphering the role(s) of CSNK2 in physiology and pathophysiology, the CSNK2 phosphoproteome offers the promise of instructing the development of CSNK2-targeted therapy.

Chemical Genetic Validation of CSNK2 Substrates Using an Inhibitor-Resistant Mutant in Combination with Triple SILAC Quantitative Phosphoproteomics.

Casein Kinase 2 (CSNK2) is an extremely pleiotropic, ubiquitously expressed protein kinase involved in the regulation of numerous key biological processes. Mapping the CSNK2-dependent phosphoproteome is necessary for better characterization of its fundamental role in cellular signalling. While ATP-competitive inhibitors have enabled the identification of many putative kinase substrates, compounds targeting the highly conserved ATP-binding pocket often exhibit off-target effects limiting their utility for definitive kinase-substrate assignment.

CK2 Regulation: Perspectives in 2021.

The protein kinase CK2 (CK2) family encompasses a small number of acidophilic serine/threonine kinases that phosphorylate substrates involved in numerous biological processes including apoptosis, cell proliferation, and the DNA damage response. CK2 has also been implicated in many human malignancies and other disorders including Alzheimer's and Parkinson's diseases, and COVID-19. Interestingly, no single mechanism describes how CK2 is regulated, including activation by external proteins or domains, phosphorylation, or dimerization.