Substrate Activity Screening: A Fragment-Based Method for the Rapid Identification of Nonpeptidic Protease Inhibitors
Wood WJ, Patterson AW, Tsuruoka H, Jain RK, Ellman JA. Substrate Activity Screening: A Fragment-Based Method for the Rapid Identification of Nonpeptidic Protease Inhibitors. Journal Of The American Chemical Society 2005, 127: 15521-15527. PMID: 16262416, DOI: 10.1021/ja0547230.Peer-Reviewed Original ResearchConceptsSubstrate Activity ScreeningRapid analog synthesisSimple fluorescence-based assayFragment-based methodsSubstrate-based methodLow molecular weightN-acyl groupAnalog synthesisNonpeptidic inhibitorsFluorescence-based assaySubstrate classesMolecular weightActivity screeningAldehyde inhibitorsAminocoumarinsMultiple distinct classesProtease substratesSAS methodNanomolar affinityCleavage efficiencyCysteine protease cathepsin SSubstrateRapid identificationProtease cathepsin SDirect replacement
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