title: Disrupting the Constitutive, Homodimeric Protein-Protein Interface in CK2β Using a Biophysical Fragment-Based Approach.
abstract: Identifying small molecules that induce the disruption of constitutive protein-protein interfaces is a challenging objective. Here, a targeted biophysical screening cascade was employed to specifically identify small molecules that could disrupt the constitutive, homodimeric protein-protein interface within CK2β. This approach could potentially be applied to achieve subunit disassembly of other homo-oligomeric proteins as a means of modulating protein function.
authors.affiliation: Department of Chemistry, University of Cambridge , Lensfield Road, Cambridge, CB2 1EW, United Kingdom.
authors.forename: Wei-Guang
authors.initials: WG
authors.lastname: Seetoh
authors.affiliation: Department of Chemistry, University of Cambridge , Lensfield Road, Cambridge, CB2 1EW, United Kingdom.
authors.forename: Chris
authors.initials: C
authors.lastname: Abell
mesh_terms: D055592:Biophysical Phenomena; D047390:Casein Kinase II / Q000737:chemistry* / Q000235:genetics / Q000378:metabolism; D004353:Drug Evaluation, Preclinical; D004795:Enzyme Stability / Q000187:drug effects; D006801:Humans; D008024:Ligands; D009154:Mutation; D055503:Protein Multimerization / Q000187:drug effects*; D020836:Protein Structure, Quaternary; D054852:Small Molecule Libraries / Q000494:pharmacology*; D013696:Temperature
chemical_list: D008024:Ligands; D054852:Small Molecule Libraries; D047390:Casein Kinase II