Development of Human Immunodeficiency Virus Type 1 Resistance to 4′-Ethynyl-2-Fluoro-2′-Deoxyadenosine Starting with Wild-Type or Nucleoside Reverse Transcriptase Inhibitor-Resistant Strains
Maria E. Cilento, Aaron B. Reeve, Eleftherios Michailidis, Tatiana V. Ilina, Eva Nagy, Hiroaki Mitsuya, Michael A. Parniak, Philip R. Tedbury, Stefan G. Sarafianos
Abstract
4′-Ethynyl-2-fluoro-2′-deoxyadenosine (EFdA, MK-8591, islatravir) is a nucleoside reverse transcriptase translocation inhibitor (NRTTI) with exceptional potency against wild-type (WT) and drug-resistant HIV-1 in phase III clinical trials. EFdA resistance is not well characterized.
Topics & Concepts
Reverse transcriptaseResistance mutationVirologyRNase HBiologyNucleotidyltransferaseCapsidMutantMolecular biologyZidovudineVirusReverse-transcriptase inhibitorEnzymeMutationNucleosideRecombinant DNAViral replicationProtein subunitNucleoside analogueNucleoside Reverse Transcriptase InhibitorDrug resistanceViral entryChemistryHIV/AIDS drug development and treatmentBiochemical and Molecular ResearchCancer-related Molecular Pathways