Abstract: Characterization of the observed mutations by site-directed mutagenesis in the isogenic HXB2D background demonstrated that a minimum of two or more mutations were required for significant loss of susceptibility, with the exception of Y188L, which requires a two-nucleotide change.
Abstract: Two pathways to loss of susceptibility to RO-0335 were observed, containing patterns of amino acid changes at either V106I/A plus F227C (with additional contributions from A98G, V108I, E138K, M230L and P236L) or V106I/Y188L (with a potential contribution from L100I, E138K
Constrained patterns of covariation and clustering of HIV-1 non-nucleoside reverse transcriptase inhibitor resistance mutations.
PMID: 20462946
2010
The Journal of antimicrobial chemotherapy
Method: We performed multidimensional scaling on the pairwise association data using a matrix D of dissimilarity coefficients (JD = 1 - J, where J is the Jaccard similarity coefficient) for the 22 mutations found in the significantly positively associated pairs (corrected P < 0.05): A98G, L100I, K101E, K101H, K101P, K102N, K103N, K103S, V106A, V106I, V106M, V108I, V179D, V179F, Y181C, Y188L,
Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs.
PMID: 20535242
2010
Letters in drug design & discovery
Introduction: Mutations associated with resistance to NNRTIs include L100I, K101E, K103N, V106A, V108I, V179D, Y181C, Y188C/L/H, G190A/E/S, M230L, P236L and Y318F.
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
Introduction: This region includes the following important and well-defined drug resistance mutations to nucleoside RT inhibitors (NRTIs) and non-nucleoside RT inhibitors (NNRTIs): L210W, T215Y/F and K219Q/E associated with resistance to zidovudine (AZT) and stavudine (d4T); M184I/V associated with resistance to lamivudine (3TC) and emtricitabine (FTC); and Y181C/I/V, Y188C/L/H and G190S/A associated with resistance to nevirapine (NVP), efavirenz (EFV) and etravirin (ETR).
Result: None of the five individuals had significant levels of PMID: 19111493
2009
International journal of infectious diseases
Abstract: Phenotypic drug resistance was also identified in six (4.7%) patients, four in the RT gene (in patients with mutations K103N, Y181C, M184V and Y188L) and two the protease gene (in two patients with minor PI mutations).
Abstract: RESULTS: Genotypic drug resistance was uncommon, and was only identified in six (4.7%) cases, all in the RT gene (L100I, K103N, Y181C, M184V, Y188L, and T215D).
Nevirapine resistance and breast-milk HIV transmission: effects of single and extended-dose nevirapine prophylaxis in subtype C HIV-infected infants.
Method: NVP-R was defined by mutations present at the following amino acid sites: L100I, K101E/P, K103N/S, V106A/M, V108I, Y181C/I/V, Y188C/L/H, or G190A/S/E based on recommendations from International AIDS Society-USA Drug Resistance Mutations and Stanford University drug-resistance database.
Emergence of multiclass drug-resistance in HIV-2 in antiretroviral-treated individuals in Senegal: implications for HIV-2 treatment in resouce-limited West Africa.
Result: The canonical HIV-1 nonnucleoside reverse-transcriptase inhibitor mutations Y181I and Y188L were found in virus strains from all HIV-2- infected patients.
The public health approach to identify antiretroviral therapy failure: high-level nucleoside reverse transcriptase inhibitor resistance among Malawians failing first-line antiretroviral therapy.