title: How druggable is protein kinase CK2?
abstract: CK2 is a pleiotropic, ubiquitous, and constitutively active protein kinase (PK), with both cytosolic and nuclear localization in most mammalian cells. The holoenzyme is generally composed of two catalytic (alpha and/or alpha') and two regulatory (beta) subunits, but the free alpha/alpha' subunits are catalytically active by themselves and can be present in cells under some circumstances. CK2 catalyzes the phosphorylation of more than 300 substrates characterized by multiple acidic residues surrounding the phosphor-acceptor amino acid, and, consequently, it plays a key role in several physiological and pathological processes. But how can one kinase orchestrate all these tasks faithfully? How is it possible that one kinase can, despite all pleiotropic characteristics of PKs in general, be involved in so many different biochemical events? Is CK2 a druggable target? Several questions are still to be clearly answered, and this review is an occasion for a fruitful discussion.
authors.affiliation: Molecular Modeling Section, Dipartimento di Scienze Farmaceutiche, Università di Padova, via Marzolo 5, Padova, Italy.
authors.forename: Giorgio
authors.initials: G
authors.lastname: Cozza
authors.forename: Andrea
authors.initials: A
authors.lastname: Bortolato
authors.forename: Stefano
authors.initials: S
authors.lastname: Moro
mesh_terms: D000596:Amino Acids / Q000737:chemistry; D000818:Animals; D001665:Binding Sites; D047390:Casein Kinase II / Q000737:chemistry* / Q000378:metabolism; D002467:Cell Nucleus / Q000378:metabolism; D018360:Crystallography, X-Ray / Q000379:methods; D003600:Cytosol / Q000378:metabolism; D020035:Holoenzymes / Q000737:chemistry; D006801:Humans; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D010766:Phosphorylation; D017434:Protein Structure, Tertiary; D020543:Proteome / Q000737:chemistry; D040901:Proteomics / Q000379:methods; D051381:Rats
chemical_list: D000596:Amino Acids; D020035:Holoenzymes; D020543:Proteome; D047390:Casein Kinase II