Dipeptide-Derived Alkynes as Potent and Selective Irreversible Inhibitors of Cysteine Cathepsins
Lydia Behring, Gloria Ruiz‐Gómez, Christian Trapp, Maryann Morales, Robert Wodtke, Martin Köckerling, Klaus Kopka, M. Teresa Pisabarro, Jens Pietzsch, Reik Löser
Abstract
). Notably, the selectivity profiles of alkynes do not necessarily reflect those of the nitriles. Inhibitory activity at the cellular level was demonstrated for selected compounds.
Topics & Concepts
DipeptideChemistryAlkyneCysteineStereochemistryCathepsinPeptideCovalent bondSelectivityDocking (animal)Cyclic peptidePeptide bondEnzymeCombinatorial chemistryBiochemistryOrganic chemistryCatalysisNursingMedicineProtease and Inhibitor MechanismsPeptidase Inhibition and AnalysisChemical Synthesis and Analysis