Rational design of Harakiri (HRK)-derived constrained peptides as BCL-xL inhibitors
Peiyu Zhang1,2, Martin Walko1,2, Andrew J Wilson1,2
1School of Chemistry, University of Leeds, Woodhouse Lane, Leeds, LS2 9JT, UK. a.j.wilson@leeds.ac.uk.
Abstract:
Using the HRK BH3 domain, sequence hybridization and in silico methods we show dibromomaleimide staple scanning can be used to inform the design of BCL-xL selective peptidomimetic ligands. These HRK-inspired reagents may serve as starting points for the discovery of therapeutics to target BCL-xL-overexpressed cancers.


