2025
Exploring Possible Drug-Resistant Variants of SARS-CoV‑2 Main Protease (Mpro) with Noncovalent Preclinical Candidate, Mpro61
Kenneson J, Papini C, Tang S, Huynh K, Zhang C, Jorgensen W, Anderson K. Exploring Possible Drug-Resistant Variants of SARS-CoV‑2 Main Protease (Mpro) with Noncovalent Preclinical Candidate, Mpro61. ACS Bio & Med Chem Au 2025, 5: 215-226. PMID: 39990941, PMCID: PMC11843330, DOI: 10.1021/acsbiomedchemau.4c00109.Peer-Reviewed Original ResearchDrug resistance mutationsViral passaging experimentsDrug-resistant clinical isolatesCOVID infectionDrug-resistant variantsSARS-CoV-2 MClinical isolatesPassage experimentsIncreased up to 10-foldClinical useSARS-CoV-2 main proteaseWild typePreclinical candidateDouble variantInhibitorsMutationsDrug developmentInfectionNirmatrelvirMain proteaseProlonged usageMedicinal chemistry modificationsVariantsTarget-based approachPatients
2023
Pharmacological disruption of mSWI/SNF complex activity restricts SARS-CoV-2 infection
Wei J, Patil A, Collings C, Alfajaro M, Liang Y, Cai W, Strine M, Filler R, DeWeirdt P, Hanna R, Menasche B, Ökten A, Peña-Hernández M, Klein J, McNamara A, Rosales R, McGovern B, Luis Rodriguez M, García-Sastre A, White K, Qin Y, Doench J, Yan Q, Iwasaki A, Zwaka T, Qi J, Kadoch C, Wilen C. Pharmacological disruption of mSWI/SNF complex activity restricts SARS-CoV-2 infection. Nature Genetics 2023, 55: 471-483. PMID: 36894709, PMCID: PMC10011139, DOI: 10.1038/s41588-023-01307-z.Peer-Reviewed Original ResearchConceptsMSWI/SNF complexesAcute respiratory syndrome coronavirus 2 infectionSevere acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infectionHost-directed therapeutic targetSyndrome coronavirus 2 infectionSARS-CoV-2 infectionSWItch/Sucrose Non-Fermentable (SWI/SNF) chromatinSARS-CoV-2 susceptibilityNon-fermentable (SWI/SNF) chromatinCoronavirus 2 infectionEnzyme 2 (ACE2) expressionSARS-CoV-2 variantsHuman cell typesPrimary human cell typesAirway epithelial cellsDrug-resistant variantsNew drug targetsChromatin accessibilitySNF complexACE2 locusACE2 expressionFactor complexHost determinantsTherapeutic targetConfer resistance
2017
Structural and Preclinical Studies of Computationally Designed Non-Nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection
Kudalkar SN, Beloor J, Chan AH, Lee WG, Jorgensen WL, Kumar P, Anderson KS. Structural and Preclinical Studies of Computationally Designed Non-Nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection. Molecular Pharmacology 2017, 91: 383-391. PMID: 28167742, PMCID: PMC5363707, DOI: 10.1124/mol.116.107755.Peer-Reviewed Original ResearchConceptsNon-nucleoside reverse transcriptase inhibitorBALB/c miceReverse transcriptase inhibitorHIV infectionC miceTranscriptase inhibitorAntiviral activityCompound INew non-nucleoside reverse transcriptase inhibitorHIV-1 non-nucleoside reverse transcriptase inhibitorDetectable acute toxicityTreating HIV InfectionSingle intraperitoneal doseAnti-HIV-1 potencyMT-2 cellsDrug-resistant variantsCompound IISerum residence timeAnti-viral potencyHIV-1 RTClinical benefitClinical efficacyIntraperitoneal doseWild-type HIV-1 RTPlasma clearance
2009
Low-Abundance HIV Drug-Resistant Viral Variants in Treatment-Experienced Persons Correlate with Historical Antiretroviral Use
Le T, Chiarella J, Simen BB, Hanczaruk B, Egholm M, Landry ML, Dieckhaus K, Rosen MI, Kozal MJ. Low-Abundance HIV Drug-Resistant Viral Variants in Treatment-Experienced Persons Correlate with Historical Antiretroviral Use. PLOS ONE 2009, 4: e6079. PMID: 19562031, PMCID: PMC2698118, DOI: 10.1371/journal.pone.0006079.Peer-Reviewed Original ResearchConceptsAntiretroviral treatment historyDrug-resistant mutationsVirologic failureAntiretroviral useDrug-resistant variantsTreatment historyOverall burdenGenotypic resistanceHIV drug-resistant mutationsHIV drug-resistant variantsStanford HIV database algorithmDrug-resistant viral variantsSubsequent antiretroviral regimensTreatment-experienced patientsConventional genotypingPrior treatment historyUltra-deep pyrosequencingSanger sequencingAntiretroviral regimensMore antiretroviralsChart reviewAntiretroviral drugsUltra-deep sequencingClinical implicationsViral variants
2000
Evaluation of 11C-colchicine for PET imaging of multiple drug resistance.
Levchenko A, Mehta B, Lee J, Humm J, Augensen F, Squire O, Kothari P, Finn R, Leonard E, Larson S. Evaluation of 11C-colchicine for PET imaging of multiple drug resistance. Journal Of Nuclear Medicine 2000, 41: 493-501. PMID: 10716325.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsATP Binding Cassette Transporter, Subfamily B, Member 1Carbon RadioisotopesColchicineDrug Resistance, MultipleFlow CytometryHumansMiceMice, Inbred BALB CModels, TheoreticalNeuroblastomaRatsRats, NudeTissue DistributionTomography, Emission-ComputedTransplantation, HeterologousTumor Cells, CulturedConceptsResistant tumorsPET imagingMultiple drug resistance phenotypeDrug-resistant variantsQuality of lifeCell linesMultiple drug resistanceResistant cell linesC cell lineP-gp actionDrug resistance phenotypeEarly diagnosisNude ratsFDG scansTumorsP-glycoproteinDrug resistanceBiodistribution experimentsCytotoxic agentsChemotherapeutic interventionResistant strainsCancer cellsIntracellular accumulationVivo experimentsScans
1998
Public Health Implications of Antiretroviral Therapy and HIV Drug Resistance
Wainberg M, Friedland G. Public Health Implications of Antiretroviral Therapy and HIV Drug Resistance. JAMA 1998, 279: 1977-1983. PMID: 9643862, DOI: 10.1001/jama.279.24.1977.Peer-Reviewed Original ResearchConceptsHuman immunodeficiency virusDrug-resistant variantsDrug-resistant virusesHIV drug resistanceAntiviral therapyPublic health implicationsDrug resistanceGenital secretionsHealth implicationsPublic health importanceAntiretroviral therapyViral burdenAntiretroviral agentsPatient adherenceTreatment failureViral loadImmunodeficiency virusResistant virusesSustained reductionHealth importanceTherapyVirusChild routeBloodSecretion
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