Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate.
Abstract: In the L100I/K103N RT/TMC278 structure, the binding mode of TMC278 is significantly altered so that the drug conforms to changes in the binding pocket primarily caused by the L100I mutation.
Abstract: In the K103N/Y181C RT/TMC278 structure, loss of the aromatic ring interaction caused by the Y181C mutation is counterbalanced by interactions between the cyanovinyl group of TMC278 and the aromatic side chain of Y183, which is facilitated by an approximately 1.5 A shift of the conserved Y(183)MDD motif.
Abstract: The crystal structures of TMC278 in complexes with the double mutant K103N/Y181C (2.1 A) and PMID: 18267363
2008
Bioorganic & medicinal chemistry
Abstract: Among them, the 6-(3,5-dimethylbenzyl) analogue 5p was identified as the most promising compound (EC(50)=0.010 microM, SI>31,800) associated with moderate activity against the HIV-1 double mutant RT strain K103N+Y181C.
Trend of drug-resistant HIV type 1 emergence among therapy-naive patients in Nagoya, Japan: an 8-year surveillance from 1999 to 2006.
PMID: 18275342
2008
AIDS research and human retroviruses
Abstract: The 402 viruses were phylogenetically analyzed, revealing three independent clusters comprising PI-resistant variants with the M46I or L90M mutation, NNRTI-resistant variants with the K103N mutation, and 215-revertant variants.
Prevalence of genotypic resistance to nucleoside analogues, nonnucleoside analogues, and protease inhibitors in HIV-infected persons in Athens, Greece.
PMID: 18275347
2008
AIDS research and human retroviruses
Abstract: M184V (63.6%) and K103N (25.2%) were the most frequent mutations related to NRTIs and NNRTIs, respectively.
Abstract: The most prevalent mutations related to NNRTIs were K103N [present in 59 tests (25.2%)], G190A [50 (21.4%)], and Y181C [48 (20.5%].
Prevalence of primary antiretroviral resistance: trends in Korea.
PMID: 18275351
2008
AIDS research and human retroviruses
Abstract: Two (2.5%) were infected with primary drug-resistant virus: M41L and K103N, respectively.
A radiolabeled oligonucleotide ligation assay demonstrates the high frequency of nevirapine resistance mutations in HIV type 1 quasispecies of NVP-treated and untreated mother-infant pairs from Uganda.
PMID: 18284323
2008
AIDS research and human retroviruses
Abstract: By OLA, 43% of the NVP-treated group had K103N and/or Y181C mutations in their HIV-1 population, using >0.6% cutoff based on a comparative clonal analysis of clinical isolates.
Abstract: Only 16% of the NVP-treated infected mothers and infants harbored either the K103N or the Y181C at 6 weeks postdelivery.
Abstract: Surprisingly, an equal fraction of the untreated and NVP-treated mother-infant group had the K103N mutation in their HIV-1 population in the range of 0.6-5%.
Abstract: The majority of these samples (n = 107) were then analyzed using a radiolabeled oligonucleotide ligation assay (OLA) specific for K70R, K103N, and Y181C, using nonstandard bases to accommodate sequence heterog
Improvement in allele-specific PCR assay with the use of polymorphism-specific primers for the analysis of minor variant drug resistance in HIV-1 subtype C.
PMID: 18295909
2008
Journal of virological methods
1Abstract: Specifically, the use of a ""universal"" set of ASPCR primers caused an overestimation of the K103N (ntAAC) mutation at position 103 of reverse transcriptase when primer binding site polymorphisms resided close to the 3' end of the allele-specific primer."
Structural basis for drug resistance mechanisms for non-nucleoside inhibitors of HIV reverse transcriptase.
HIV mutation literature information.
PMID: 
2008
Bioorganic & medicinal chemistry
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