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
2007
Epidermal Growth Factor Receptor Mutants from Human Lung Cancers Exhibit Enhanced Catalytic Activity and Increased Sensitivity to Gefitinib
Mulloy R, Ferrand A, Kim Y, Sordella R, Bell D, Haber D, Anderson K, Settleman J. Epidermal Growth Factor Receptor Mutants from Human Lung Cancers Exhibit Enhanced Catalytic Activity and Increased Sensitivity to Gefitinib. Cancer Research 2007, 67: 2325-2330. PMID: 17332364, DOI: 10.1158/0008-5472.can-06-4293.Peer-Reviewed Original ResearchConceptsEpidermal growth factor receptorEpidermal growth factor receptor mutantMultiple levels in vivoIn vitro kinase assayEpidermal growth factor receptor functionPurified recombinant proteinWild-type epidermal growth factor receptorSensitivity to kinase inhibitionNon-small cell lung cancerCOOH-terminal tyrosineHuman non-small cell lung cancerIncreased sensitivity to gefitinibSensitivity to gefitinibCell lung cancerAutophosphorylation activityGrowth factor receptorCell-based studiesEGFR kinase inhibitorsCytoplasmic domainRecombinant proteinsKinase assayEnzyme functionDownstream effectorsMutantsKinase activity
2001
Deoxythioguanosine triphosphate impairs HIV replication: a new mechanism for an old drug
KRYNETSKAIA N, FENG J, KRYNETSKI E, GARCIA J, PANETTA J, ANDERSON K, EVANS W. Deoxythioguanosine triphosphate impairs HIV replication: a new mechanism for an old drug. The FASEB Journal 2001, 15: 1902-1908. PMID: 11532970, DOI: 10.1096/fj.01-0124com.Peer-Reviewed Original ResearchConceptsAnti-retroviral agentsHIV replicationHIV-1 reverse transcriptaseReverse transcriptaseTreatment of HIVHuman lymphocyte culturesDifferent medicationsHost lymphocytesAdditive cytotoxicityHIV-1Old drugsLymphocyte culturesActive metaboliteHuman lymphocytesMinimal toxicityLymphocytesThioguanineSubstantial inhibitionTreatmentInhibitionHIV proteaseEarly stagesMedicationsHIVPatientsMechanism of Action of 1-β-d-2,6-Diaminopurine Dioxolane, a Prodrug of the Human Immunodeficiency Virus Type 1 Inhibitor 1-β-d-Dioxolane Guanosine
Furman P, Jeffrey J, Kiefer L, Feng J, Anderson K, Borroto-Esoda K, Hill E, Copeland W, Chu C, Sommadossi J, Liberman I, Schinazi R, Painter G. Mechanism of Action of 1-β-d-2,6-Diaminopurine Dioxolane, a Prodrug of the Human Immunodeficiency Virus Type 1 Inhibitor 1-β-d-Dioxolane Guanosine. Antimicrobial Agents And Chemotherapy 2001, 45: 158-165. PMID: 11120959, PMCID: PMC90254, DOI: 10.1128/aac.45.1.158-165.2001.Peer-Reviewed Original ResearchMeSH KeywordsAdenosine Deaminase InhibitorsAnti-HIV AgentsBone Marrow CellsCells, CulturedDioxolanesDNA, ViralDrug Resistance, MicrobialEnzyme InhibitorsGuanosineHIV-1HumansLactic AcidMicroscopy, ElectronMitochondriaNucleic Acid Synthesis InhibitorsProdrugsPurine NucleosidesReverse Transcriptase InhibitorsConceptsDiaminopurine dioxolaneDXG-TPNucleoside reverse transcriptase inhibitorHuman immunodeficiency virus type 1Peripheral blood mononuclear cellsImmunodeficiency virus type 1Blood mononuclear cellsReverse transcriptase inhibitorAdenosine deaminaseVirus type 1Alternative substrate inhibitorsHIV-1 RTMechanism of actionWater-soluble prodrugMononuclear cellsDioxolane guanosineTranscriptase inhibitorType 1CEM cellsInhibitor-1Mitochondrial toxicityHuman DNA polymerase alphaCalf adenosine deaminaseInhibitorsDNA polymerase gamma