2H-Pyrrolo[3,4-b] [1,5]benzothiazepine derivatives as potential inhibitors of HIV-1 reverse transcriptase.
PMID: 15910811
2005
Farmaco (Societa chimica italiana
Abstract: Unfortunately, none of the test compounds inhibited the multiplication of clinically relevant drug-resistant viruses (mutants of HIV-1 carrying K103N and Y181C mutations) at concentrations lower than 30 microM.
Structure-based design, parallel synthesis, structure-activity relationship, and molecular modeling studies of thiocarbamates, new potent non-nucleoside HIV-1 reverse transcriptase inhibitor isosteres of phenethylthiazolylthiourea derivatives.
PMID: 15916438
2005
Journal of medicinal chemistry
Abstract: TCs 31, 37, 39, 40, and 44 significantly reduced the multiplication of the Y181C mutant, but they were inactive against K103R and K103N + Y181C mutants.
Emergence of drug-resistant HIV-1 after intrapartum administration of single-dose nevirapine is substantially underestimated.
PMID: 15942889
2005
The Journal of infectious diseases
Abstract: By sequence analysis, 40 women had no detectable resistance mutations, and an additional 6 women were negative for Y181C after SD-NVP.
Abstract: Clonal sequencing confirmed K103N in 5 of 5 representative samples and Y181C in 4 of 4 samples.
Abstract: Four of the 5 women with newly identified Y181C also had K103N.
Abstract: Using sensitive real-time polymerase chain reaction assays for the K103N and Y181C resistance mutations, we tested genotyped virus before and after SD-NVP in 50 South African women infected with HIV-1 subtype C.
Abstract: We found K103N in 16 (40%) of 40 women and Y181C in 5 (11%) of 46
Genetic linkage of nevirapine resistance mutations in HIV type 1 seven days after single-dose nevirapine.
PMID: 15943576
2005
AIDS research and human retroviruses
Abstract: K103N and Y181C were the most common mutations detected.
Abstract: Different combinations of NVPR mutations were linked in individual clones, but none of the clones contained both K103N and Y181C.
[Efficacy of anti-HIV treatment and drug-resistance mutations in some parts of China].
Abstract: Y181C is another common mutation occurred in Henan cohort, which causes crossing drug resistance and multi-drug resistance to NNRTIs.
Novel 8-substituted dipyridodiazepinone inhibitors with a broad-spectrum of activity against HIV-1 strains resistant to non-nucleoside reverse transcriptase inhibitors.
PMID: 16107158
2005
Journal of medicinal chemistry
Abstract: A series of novel 8-substituted dipyridodiazepinone-based inhibitors were investigated for their antiviral activity against wild type human immunodeficiency virus (HIV-1) and the clinically prevalent K103N/Y181C mutant virus.
Quantum computational analysis for drug resistance of HIV-1 reverse transcriptase to nevirapine through point mutations.
Abstract: Quantum chemical calculation has been carried out to analyze binding interactions of nevirapine to HIV-1 reverse transcriptase (RT) and single point mutants Lys103 --> Asn (K103N) and Tyr181--> Cys (Y181C).
Biophysical Characterization of Novel DNA Aptamers against K103N/Y181C Double Mutant HIV-1 Reverse Transcriptase.
PMID: 16123677
2005
Journal of acquired immune deficiency syndromes (1999)
Abstract: The higher rate of NVPR in subtype D was explained by at least 2 factors: Y181C faded from detection at a greater rate in women with subtype A (odds ratio = 3.06; 95% CI, 1.04, 8.90) and K103N accumulated at a greater rate in women with subtype D (odds ratio = 1.74; 95% CI, 0.62, 4.87).
Efficacy and safety of once-daily combination therapy with didanosine, lamivudine and nevirapine in antiretroviral-naive HIV-infected patients.
Abstract: Eight out of nine patients with available genotype after virological failure showed resistance mutations to NVP (Y181C and others) and 3TC (M184V/I), and four of them also had ddI resistance (L74V).
TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments.
Abstract: Furthermore, breakthrough of virus from site-directed mutant (SDM) SDM-K103N/Y181C occurred at the same time or later with TMC125 as breakthrough from wild-type HIV-1 with efavirenz or nevirapine.
Abstract: The selection experiments identified mutations selected by TMC125 that included known NNRTI-associated mutations L100I, Y181C, G190E, M230L, and Y318F and the novel mutations V179I and V179F.
HIV mutation literature information.
PMID: 
2005
Farmaco (Societa chimica italiana
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