Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement.
PMID: 27750153
2017
European journal of medicinal chemistry
Abstract: Furthermore, most compounds maintained high activity agaist various single HIV-1 mutants (L100I, K103N, E138K, Y181C) as well as one double mutant (F227L/V106A) with EC50 values in low-micromolar to double-digit nanomolar concentration ranges.
Pretreatment HIV-1 drug resistance in Argentina: results from a surveillance study performed according to WHO-proposed new methodology in 2014-15.
PMID: 27789684
2017
The Journal of antimicrobial chemotherapy
Abstract: The most common mutation was K103N.
Rapid Detection of Common HIV-1 Drug Resistance Mutations by Use of High-Resolution Melting Analysis and Unlabeled Probes.
PMID: 27795333
2017
Journal of clinical microbiology
Abstract: The analytical sensitivities of the HRMA assays were 5% of mixed species for K103N and Y181C and 20% for M184V.
Abstract: When applied to 153 HIV-1 patient specimens previously genotyped by Sanger population sequencing, HRMA correctly assigned drug sensitivity or resistance profiles to 80% of the samples at codon 103 (K103K/N) (Cohen's kappa coefficient [kappa] > 0.6; P < 0.05), 90% at 181 (Y181Y/C) (kappa > 0.74, P < 0.05), and 80% at 184 (M184M/V) (kappa > 0.62; P < 0.05).
Low Rates of Transmitted Drug Resistance Among Newly Identified HIV-1 Seroconverters in Rural Rakai, Uganda.
PMID: 27798967
2017
AIDS research and human retroviruses
Abstract: Two individuals had a single non-nucleoside reverse transcriptase inhibitor mutation each, K101E and K103N, and one had a single protease inhibitor mutation, M46I.
Frequent Cross-Resistance to Dapivirine in HIV-1 Subtype C-Infected Individuals after First-Line Antiretroviral Therapy Failure in South Africa.
PMID: 27895013
2017
Antimicrobial agents and chemotherapy
Abstract: Mutations L100I and K103N were significantly more frequent in samples with >500-fold resistance to DPV compared to samples with a <=500-fold resistance.
Use of Capillary Electrophoresis to Study the Binding Interaction of Aptamers with Wild-Type, K103N, and Double Mutant (K103N/Y181C) HIV-1 RT : Studying the Binding Interaction of Wild-Type, K103N, and Double Mutant (K103N/Y181C) HIV-1 RT with Aptamers by Performing the Capillary Electrophoresis.
PMID: 27900665
2017
Applied biochemistry and biotechnology
Abstract: In addition, RT1t49 could bind specifically with the wild-type, K103N, and double mutants in Escherichia coli lysate.
Abstract: Therefore, we utilized non-equilibrium capillary electrophoresis of equilibrium mixture (NECEEM) to study the interaction of three HIV-1 RTs (wild type, K103N, and double mutant (K103N/Y181C)) with RT1t49 and RT12 aptamers.
Trends and predictors of HIV-1 acquired drug resistance in Minas Gerais, Brazil: 2002-2012.
PMID: 28017554
2017
The Brazilian journal of infectious diseases
Abstract: Resistance to NNRTI increased from 74.4% to 81.6%, mainly because of K103N mutation.
Early virological failure and HIV drug resistance in Ugandan adults co-infected with tuberculosis.
Abstract: Genotypic resistance testing was available for 16/22 (72.7%) patients, of which 15 (93.8%) had at least one major mutation, most commonly M184V (81.2%) and K103NS (68.8%).
Result: The most common mutations found were M184V (81.2%) reflecting treatment with the nucleoside/nucleotide reverse transcriptase inhibitor (NRTI) lamivudine, and K103NS (68.8%) reflecting prior treatment with the non-nucleoside reverse transcriptase inhibitors (NNRTI) nevirapine or efavirenz.
Discussion: M184 V and K103NS were the most prevalent mutations found, reflecting prior treatment with lamivudine, efavirenz or nevirap
Polymorphisms and Mutational Covariation Associated with Death in a Prospective Cohort of HIV/AIDS Patients Receiving Long-Term ART in China.
Abstract: Among them, 7 polymorphisms (L74I, K103N, V106A, Y181C, G190A, T215I and P225H) were known to be drug resistance mutations, 7 polymorphisms (E6D, E35D, S37N, I93L, E169D, T200V and T200E were considered to be potential drug resistance mutations, and 6 polymorphisms (T39A, K43E, S68N, Q197K,
Table: K103N
HIV-1 drug-resistant mutations and related risk factors among HIV-1-positive individuals experiencing treatment failure in Hebei Province, China.
Result: In NNRTI coding regions, K103 N was the most frequent mutation, accounting for 15.9% (34/214), followed by Y181C (11.7%, 25/214), G190A (5.1%, 11/214), and G190S (3.7%, 8/214).
Result: One participant infected through heterosexual contact harbored dual mutations in NRTIs (T69N, M184V, and T215Y) and NNRTIs (K103N and M230L), and presented with high-level resistance to lamivudine (3TC) and emtricitabine (FTC) with M184V, intermediate-level resistance to zidovudine (AZT) and stavudine (D4T) with
HIV mutation literature information.
PMID: 
2017
European journal of medicinal chemistry
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