Development of small cyclic peptides targeting the CK2α/β interface. Issue 30 (28th March 2022)

• Record Type: Journal Article
• Authors: Atkinson, Eleanor L.; Iegre, Jessica; D'Amore, Claudio; Brear, Paul; Salvi, Mauro; Hyvönen, Marko; Spring, David R.
• Is Part Of: Chemical communications. Volume 58:Issue 30(2022)
• Page Start: 4791
• Page End: 4794
• Publication Date: 2022-03-28
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d2cc00707j
• Languages: English
• ISSNs: 1359-7345

Abstract

Abstract : Development of a small CK2α/β protein–protein interaction-inhibiting peptide, which is easily synthesisable and functionalisable, with good enzymatic and cellular activity. Abstract : In this work, an iterative cycle of enzymatic assays, X-ray crystallography, molecular modelling and cellular assays were used to develop a functionalisable chemical probe for the CK2α/β PPI. The lead peptide, P8C9, successfully binds to CK2α at the PPI site, is easily synthesisable and functionalisable, highly stable in serum and small enough to accommodate further optimisation.