Fragment-Based Substrate Activity Screening Method for the Identification of Potent Inhibitors of the Mycobacterium tuberculosis Phosphatase PtpB
Soellner MB, Rawls KA, Grundner C, Alber T, Ellman JA. Fragment-Based Substrate Activity Screening Method for the Identification of Potent Inhibitors of the Mycobacterium tuberculosis Phosphatase PtpB. Journal Of The American Chemical Society 2007, 129: 9613-9615. PMID: 17636914, DOI: 10.1021/ja0727520.Peer-Reviewed Original ResearchSubstrate‐Based Fragment Identification and Optimization for Inhibitor Discovery
Ellman J. Substrate‐Based Fragment Identification and Optimization for Inhibitor Discovery. The FASEB Journal 2007, 21: a209-a209. DOI: 10.1096/fasebj.21.5.a209-c.Peer-Reviewed Original ResearchFragment-based approachSmall molecule ligandsFragment-based methodsMolecule ligandsFragment approachInhibitor discoveryLow molecular weight inhibitorsEfficient conversionSubstrate screeningLigandsHigh-throughput methodSelective ligandsFragment identificationWeight inhibitorsSelective low molecular weight inhibitorsCleavage efficiencyThroughput methodEfficient methodSelective drugsRelevant proteasesDesign principlesFragmentsDiscoveryLow affinityConversion
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