Department of Chemistry, University of Cambridge , Lensfield Road, Cambridge, CB2 1EW, United Kingdom.
J Am Chem Soc. 2016 Nov 2;138(43):14303-14311. doi: 10.1021/jacs.6b07440. Epub 2016 Oct 20.
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.
鉴定能够诱导组成型蛋白质-蛋白质界面破坏的小分子是一个具有挑战性的目标。在这里,采用了靶向生物物理筛选级联方法,专门鉴定能够破坏 CK2β 内组成型同源二聚体蛋白质-蛋白质界面的小分子。这种方法可能被应用于实现其他同源寡聚体蛋白质的亚基解体,作为调节蛋白质功能的一种手段。