2008
C-2-Aryl O-substituted HI-236 derivatives as non-nucleoside HIV-1 reverse-transcriptase inhibitors
Hunter R, Younis Y, Muhanji C, Curtin T, Naidoo K, Petersen M, Bailey C, Basavapathruni A, Anderson K. C-2-Aryl O-substituted HI-236 derivatives as non-nucleoside HIV-1 reverse-transcriptase inhibitors. Bioorganic & Medicinal Chemistry 2008, 16: 10270-10280. PMID: 18996020, PMCID: PMC2639753, DOI: 10.1016/j.bmc.2008.10.048.Peer-Reviewed Original ResearchConceptsThiourea derivativesHI-236C-2 arylationC-2 oxygenStructure-activity profilePhenyl ringAnti-HIV activityNNRTI pocketC-2Drug designCell-free RT assaysDocking modelThioureaDerivativesInhibitory activityBifunctional inhibitorsImproved leadsPhenylAutoDockDockingRingCompoundsPocketSpatial characteristicsMT-2 cell cultures
2003
Detection and characterization of enzyme intermediates: utility of rapid chemical quench methodology and single enzyme turnover experiments
Anderson K. Detection and characterization of enzyme intermediates: utility of rapid chemical quench methodology and single enzyme turnover experiments. 2003, 19-48. DOI: 10.1093/oso/9780198524946.003.0002.Peer-Reviewed Original ResearchEnzyme active siteEnzyme intermediateProtein structure-function studiesSteady-state kinetic studiesStructure-function studiesTransient kinetic approachActive siteMolecule of substrateEnzyme catalysisQuenching methodologyEnzymeTurnover experimentsTransient kinetic techniquesStructure-based drug designEnzyme Transition StatesDrug designMechanistic informationKinetic techniquesSubstrate(sMillisecond time scaleProteinSitesPathwayKinetic studiesIntermediate