Functionalized Double Strain-Promoted Stapled Peptides for Inhibiting the p53-MDM2 Interaction
Krishna Sharma, Alexander V. Strizhak, Elaine Fowler, Wenshu Xu, Ben Chappell, Hannah F. Sore, Warren R. J. D. Galloway, Matthew N. Grayson, Yu Heng Lau, Laura S. Itzhaki, David R. Spring
Abstract
-fluoro-substituted Sondheimer dialkyne was found to be the most potent inhibitor. Furthermore, through experimental studies and density functional theory calculations, we investigated the impact of the substituent on the strain-promoted double-click reactivity of Sondheimer dialkyne.
Topics & Concepts
SubstituentPeptideReagentStrain (injury)Reactivity (psychology)StereochemistryAzideCombinatorial chemistryChemistryBiochemistryOrganic chemistryBiologyPathologyMedicineAnatomyAlternative medicineClick Chemistry and ApplicationsCancer-related Molecular PathwaysUbiquitin and proteasome pathways