Abstract: OBJECTIVE: To develop a high-throughput, real-time reverse transcriptase (RT) polymerase chain reaction (PCR) assay to quantify non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant variants K103N (AAT or AAC alleles) at frequencies as low as 0.1%, and to apply this to monitor these variants before, during, and after NNRTI therapy.
Abstract: The rate of decay of K103N variants after stopping NNRTI therapy was highly variable.
Phenotypic drug resistance patterns in subtype A HIV-1 clones with nonnucleoside reverse transcriptase resistance mutations.
PMID: 16545016
2006
AIDS research and human retroviruses
1Abstract: Six clones had no NNRTI resistance-associated mutations (""wild type""), eight had K103N, nine had Y181C, five had G190A, and one had Y181S."
Abstract: One wild-type clone had reduced susceptibility to NVP, delavirdine (DLV), and efavirenz (EFV), one clone with K103N was susceptible to all three NNRTIs, and one clone with G190A had extreme hypersusceptibility to DLV.
Development of Novel Dihydrofuro[3,4-d]pyrimidine Derivatives as HIV-1 NNRTIs to Overcome the Highly Resistant Mutant Strains F227L/V106A and K103N/Y181C.
Abstract: CONCLUSIONS: K103N resistant variants were present in almost all women at 6 weeks post-sd-NVP but declined rapidly over time.
Abstract: DESIGN AND METHODS: We measured the frequency of K103N mutants among a cohort of HIV-1-infected pregnant women recruited at an out-patient clinic in Johannesburg, South Africa.
Abstract: OBJECTIVES: Single-dose nevirapine (sd-NVP) for prevention of mother-to-child HIV-1 transmission is associated with selection of resistant viral variants, particularly the Lysine (K) to Asparagine (N) mutation at codon 103 (K103N) of reverse transcriptase.
Abstract: Quantification of K103N mutants in maternal plasma viral RNA and cellular DNA was done using an allele-specific real-time polymerase
Biosensor-based kinetic characterization of the interaction between HIV-1 reverse transcriptase and non-nucleoside inhibitors.
PMID: 16610780
2006
Journal of medicinal chemistry
Abstract: This initial study was performed with HIV-1 reverse transcriptase mutant K103N, the phenethylthioazolylthiourea compound (PETT) MIV-150, and the three NNRTIs licensed for clinical use: nevirapine, delavirdine, and efavirenz.
Interaction kinetic characterization of HIV-1 reverse transcriptase non-nucleoside inhibitor resistance.
PMID: 16610781
2006
Journal of medicinal chemistry
Abstract: The Y181C, V108I, and P225H substitutions affected primarily the association and dissociation rate constants, while the K103N and the L100I substitutions also influenced the equilibrium between the two forms of the free enzyme.
Abstract: The K103N and the L100I substitutions were found to facilitate both the entry of the inhibitor into the binding pocket as well as its exit, in contrast to what has been reported elsewhere.
Persistence of nevirapine-resistant HIV-1 in women after single-dose nevirapine therapy for prevention of maternal-to-fetal HIV-1 transmission.
Abstract: Allele-specific PCR analysis for the two most common NVP resistance mutations (K103N and Y181C) detected NVP-resistant variants in most (16 of 21) samples that were negative for NVP resistance by standard genotype, at levels ranging from 0.1% to 20% 1 yr after treatment.
Development of Novel Dihydrofuro[3,4-d]pyrimidine Derivatives as HIV-1 NNRTIs to Overcome the Highly Resistant Mutant Strains F227L/V106A and K103N/Y181C.
PMID: 16644557
2006
SAR and QSAR in environmental research
Abstract: 124 Compounds having a GoldScore higher than that of nevirapine (55.00 and 52.00 for K103N and Y181C mutants, respectively) were first retrieved and submitted to a topological analysis with the SILVER program.
Abstract: Its efficiency is limited by drug resistant mutations, such as K103N and Y181C, so, the aim of this work was to design novel nevirapine analogues insensitive to the K103N and Y181C HIV-1 RT.
Modulation of human immunodeficiency virus type 1 synergistic inhibition by reverse transcriptase mutations.
Abstract: Efavirenz displayed a 100 nM IC50 value against WT and the efavirenz-sensitive Y181C mutant, but the efavirenz-resistant mutants K103N and K103N/Y181C required a 6-fold increase in efavirenz concentration to achieve the same effect.
HIV-1 reverse transcriptase mutants resistant to nonnucleoside reverse transcriptase inhibitors do not adversely affect DNA synthesis: pre-steady-state and steady-state kinetic studies.
PMID: 16763521
2006
Journal of acquired immune deficiency syndromes (1999)
Abstract: In this study, we evaluated the polymerase function of 3 clinically occurring NNRTI-resistant RTs (K103N, P236L, and V106A) in greater detail, under both pre-steady-state and steady-state conditions.
QSAR for non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Abstract: The optimal models found include up to seven parameters: R = 0.7991, R(l-20%-o) = 0.7233 for the case of wild-type, and R = 0.9261, R(l-5%-o) = 0.8802 for the K-103N mutation.
HIV mutation literature information.
PMID: 
2006
AIDS (London, England)
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