China Pharmaceutical University Locks Short Peptides Into Helices With a 4-Mercaptoproline Cap to Block the Cancer Protein MDM2
China Pharmaceutical University chemists reported in Organic Letters that capping a peptide's starting end with 4-mercaptoproline and cross-linking it to an internal cysteine holds short peptides in the helical shape needed to block protein-protein interactions inside cells. Tuning the cap's stereochemistry and the cross-linker improved helicity, cell uptake, resistance to breakdown, and binding to MDM2, and the peptides reduced cancer cell viability, growth, and migration in lab tests.