Sensitive oligonucleotide ligation assay for low-level detection of nevirapine resistance mutations in human immunodeficiency virus type 1 quasispecies.
PMID: 17567789
2007
Journal of clinical microbiology
Abstract: Ten of 19 HIV-1 DNA samples extracted from peripheral blood mononuclear cells had a detectable K103N (0.5 to 44%) or Y181C (0.8 to 92.5%) mutation, but only one plasma HIV-1 RNA sample had a viral population with the Y181C mutation.
Abstract: This modified OLA is now capable of detecting mutants with the K103N or the Y181C mutation present in an HIV-1 population at a frequency of approximately 0.4% and is at least 10- to 30-fold more sensitive than the original protocol.
Abstract: This study has adapted the oligonucleotide ligation assay (OLA) to probe for low-level nevirapine (NVP) resistance mutations K103N and Y181C in the human immunodeficiency virus type 1 (HIV-1) population of infected mother-infant pairs from Uganda.
Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.
Abstract: A series of aryl thiotetrazolylacetanilides were synthesized and found to be potent inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.
Characterization and structural analysis of novel mutations in human immunodeficiency virus type 1 reverse transcriptase involved in the regulation of resistance to nonnucleoside inhibitors.
Abstract: In particular, L74V and H221Y, positively correlated with Y181C, were associated with an increase in Y181C-mediated resistance to nevirapine, while I135M/T mutations, positively correlated with K103N, were associated with an increase in K103N-mediated resistance to efavirenz.
[Prevalence of resistance to antiretroviral drugs in Spain].
PMID: 17692254
2007
Anales de pediatria (Barcelona, Spain
Abstract: K103N and Y181C were detected in 24 (67%) and 10 (28%) of the children respectively, while 32 (90%) showed primary mutations to PI.
Polymorphism and drug selected mutations of reverse transcriptase gene in 102 HIV-1 infected patients living in China.
Abstract: An association between H221Y and L228H/R with Y181C was noted.
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity.
PMID: 17803291
2007
Journal of medicinal chemistry
Abstract: Indolyl aryl sulfones bearing the 4,5-difluoro (10) or 5-chloro-4-fluoro (16) substitution pattern at the indole ring were potent inhibitors of HIV-1 WT and the NNRTI-resistant strains Y181C and K103N-Y181C.
Additional level of information about complex interaction between non-nucleoside inhibitor and HIV-1 reverse transcriptase using biosensor-based thermodynamic analysis.
Abstract: The thermodynamics of the interaction between mutant HIV-1 reverse transcriptase (K103N and Y181C) and a non-nucleoside reverse transcriptase inhibitor (NNRTI), the phenylethylthiazolylurea compound MIV-150, was obtained by determining the temperature dependence of the kinetic rate constants.
Synthesis and biological properties of novel 2-aminopyrimidin-4(3H)-ones highly potent against HIV-1 mutant strains.
PMID: 17910429
2007
Journal of medicinal chemistry
Abstract: The new compounds were highly active up to the subnanomolar level against both wt HIV-1 and the Y181C mutant and at the submicromolar to nanomolar range against the K103N and Y188L mutant strains.
Potent activity of the HIV-1 maturation inhibitor bevirimat in SCID-hu Thy/Liv mice.
Discussion: Single mutations in reverse transcriptase (RT) confer resistance to nucleoside RT inhibitors (M184V, K65R) and nonnucleoside RT inhibitors (Y181C) without significantly compromising viral fitness, yet these drugs are used in most antiretroviral regimens.
N348I in the connection domain of HIV-1 reverse transcriptase confers zidovudine and nevirapine resistance.
Discussion: Apart from Q145M, which has been reported to confer broad resistance to several NRTIs and NNRTIs, and Y181C/I, which may confer resistance to stavudine in addition to NVP, N348I represents the only other example of an in vivo mutation that confers decreased susceptibility to two classes of RT inhibitors.
Discussion: Furthermore, the N348I mutation is associated with M184V/I, TAMs, K103N and Y181C and is selected by NVP and AZT treatment.
Discussion: In our cohort N348I was associated with the appearance of K103N, V108l,
ViMRT
HIV mutation literature information.
PMID: 
2007
Journal of clinical microbiology
