Intracellular Metabolism and Persistence of the Anti-Human Immunodeficiency Virus Activity of 2′,3′-Didehydro-3′-Deoxy-4′-Ethynylthymidine, a Novel Thymidine Analog
Paintsil E, Dutschman GE, Hu R, Grill SP, Lam W, Baba M, Tanaka H, Cheng YC. Intracellular Metabolism and Persistence of the Anti-Human Immunodeficiency Virus Activity of 2′,3′-Didehydro-3′-Deoxy-4′-Ethynylthymidine, a Novel Thymidine Analog. Antimicrobial Agents And Chemotherapy 2007, 51: 3870-3879. PMID: 17724147, PMCID: PMC2151449, DOI: 10.1128/aac.00692-07.Peer-Reviewed Original ResearchConceptsAnti-human immunodeficiency virus (HIV) activityAnti-HIV activityDrug-resistant virusesD4TNovel thymidine analogVirus activityPotent anti-human immunodeficiency virus activityMultidrug-resistant HIVCurrent antiretroviral therapyDrug removalPatient compliance issuesIntracellular metabolismThymidine analogueLong-term toxicityPromising antiviral candidateNovel antiretroviral compoundsDose-dependent accumulationAntiretroviral therapyMonophosphate metaboliteFrequent dosingAntiretroviral compoundsT metabolitesTherapeutic benefitHIV activityAntiviral candidatesComparison of the Phosphorylation of 4′-Ethynyl 2′,3′-Dihydro-3′-Deoxythymidine with That of Other Anti-Human Immunodeficiency Virus Thymidine Analogs
Hsu CH, Hu R, Dutschman GE, Yang G, Krishnan P, Tanaka H, Baba M, Cheng YC. Comparison of the Phosphorylation of 4′-Ethynyl 2′,3′-Dihydro-3′-Deoxythymidine with That of Other Anti-Human Immunodeficiency Virus Thymidine Analogs. Antimicrobial Agents And Chemotherapy 2007, 51: 1687-1693. PMID: 17353236, PMCID: PMC1855562, DOI: 10.1128/aac.01432-06.Peer-Reviewed Original ResearchConceptsD4TAnti-human immunodeficiency virus (HIV) activityStepwise phosphorylationTMP kinaseMultidrug-resistant HIVActive triphosphate metaboliteT-lymphoid cell linesThymidine analogueNucleoside diphosphate kinaseHuman thymidine kinase 1Antiretroviral agentsAntiretroviral activityRate-limiting enzymeThymidine kinase 1Crude cellular extractsVirus activityDiphosphate kinaseTriphosphate metaboliteCreatine kinaseKinase 1Cellular extractsKinasePhosphorylation efficiencyPhosphorylationPyruvate kinase