High Levels of Acquired HIV Drug Resistance Following Virological Nonsuppression in HIV-Infected Women from a High-Risk Cohort in Uganda.
PMID: 32475121
2020
AIDS research and human retroviruses
Abstract: The mutation K103N was detected in 62.5% (30/48) of participants, 41.7% (20/48) had M184V/I, 14.6% had K65R, and 12.5% (6/48) had thymidine analog mutations (TAMs).
Diagnostic Accuracy of Pan-Degenerate Amplification and Adaptation Assay for HIV-1 Drug Resistance Mutation Analysis in Low- and Middle-Income Countries.
PMID: 32522826
2020
Journal of clinical microbiology
Abstract: In a cross-sectional study (June 2018 to September 2019), we evaluated the diagnostic accuracy of a simple and rapid HIVDR assay (the pan-degenerate amplification and adaptation [PANDAA] assay targeting the mutations K65R, K103NS, M184VI, Y181C, and G190A) compared to Sanger sequencing and next-generation sequencing (NGS).
Abstract: PANDAA showed strong agreement with Sanger sequencing for K65R, K103NS, M184VI, and G190A (kappa > 0.85) and substantial agreement for Y181C (kappa = 0.720).
Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs.
Abstract: Especially, compound 26 exhibited the most potent activity against wild-type and a panel of single mutations (L100I, K103N, Y181C, Y188L and E138K) with an EC50 ranging from 6.02 to 23.9 nmol/L, which were comparable to those of etravirine (ETR).
Introduction: K103N and Y181C are the two most prevalent mutations in vivo, which e
Introduction: Although they could effectively inhibit most of the RT-resistant mutations caused by the first-generation NNRTIs, they generally failed to suppress the most refractory mutations E138K and RES056 (K103N + Y181C).
HIV-1 re-suppression on a first-line regimen despite the presence of phenotypic drug resistance.
Result: A quarter (9/36 [25%]) of the samples contained both M184V and K103N mutations.
Result: Both groups of patients were on similar regimens and displayed similar genotypic resistance profiles, with the K103N (>=57%) and M184V (>=71%) mutations being the most prevalent.
Result: The most prevalent NNRTI mutations were K103N (16/36 [44%]) and V106M (9/36 [25%]).
Table: K103N
Discussion: K103N, V106M) drug resistance mutations, typically observed in patients failing an NNRTI-based regimen.
Prevalence and determinants of virological failure, genetic diversity and drug resistance among people living with HIV in a minority area in China: a population-based study.
Abstract: The most common mutations in NNRTIs, NRTIs and PIs were K103N/KN (64.69%), M184V/MV/I (36.29%) and Q58E/QE (4.93%), respectively.
Result: The most common mutations in NNRTIs were K103N/KN (64.69%), V179D/E (23.47%) and Y181C/YC/I (14.00%), they were M184V/MV/I (36.29%), T215F/FS/TNSY (7.50%) and K219Q (5.92%) in NRTIs, and they were Q58E/QE (4.93%), PMID: 32631509
2020
Bioorganic & medicinal chemistry letters
Abstract: In addition, it showed moderate inhibitory potency (EC50 = 1.329 muM) against the HIV-1 K103N/Y181C double mutant strain (MT-4 cells).
Targeting HIV-1 RNase H: N'-(2-Hydroxy-benzylidene)-3,4,5-Trihydroxybenzoylhydrazone as Selective Inhibitor Active against NNRTIs-Resistant Variants.
Abstract: Here, we characterize the mode of action of N'-(2-hydroxy-benzylidene)-3,4,5-trihydroxybenzoylhydrazone (compound 13), an N-acylhydrazone derivative that inhibited viral replication (EC50 = 10 microM), while retaining full potency against the NNRTI-resistant double mutant K103N-Y181C virus.
Method: Triplicate wells of 96-well plates containing serial dilutions of drugs were seeded with 3 x 104 MT4 cells and infected with HIV-1 NL4.3 wt or with the HIV-1 NL4-3 K103N-Y181C strain at multiplicity of infection (MOI) of 0.003 or 100 culture infective dose (CCID50) calculated using the Reed and Muench method.
Discussion: Consistently, compound 13 retained full potency of inhibition against the NNRTI drug-resistant HIV-1 strain K103N
Impact of Pre-antiretroviral Therapy CD4 Counts on Drug Resistance and Treatment Failure: A Systematic Review.
Abstract: Most frequent resistance mutations included the M184I/V for the nucleoside reverse-transcriptase inhibitors (NRTIs), K103N, and Y181 for the non-NRTIs (NNRTIs), and L90M for the Protease inhibitors.
Pre-treatment drug resistance and HIV-1 genetic diversity in the rural and urban settings of Northwest-Cameroon.
Abstract: Fifteen (15) PDR mutations were found among four patients the urban settings [6 resistance mutations to NRTIs:[M41L (2), E44D (1), K65R (1), K70E (1), M184V/I (2), K219R (1)] and 6 resistance mutations to NNRTIs: K103N (1), E138A/G (2), V179E (1), M230L (1), K238T (1), P225H (1)] against two (02) mutations found in two patients in the rural setting[2 resistant mutations to NNRTIs: E138A (1) and
Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors.
PMID: 32712537
2020
European journal of medicinal chemistry
Abstract: Among all the chiral derivatives, (S)-(-)-12a showed the best potency with the antiviral activities against wild-type (WT) and single mutant strains (L100I, K103 N, Y181C, E138K; especially Y188L), and RT enzyme in the low nanomolar concentration range.
HIV mutation literature information.
PMID: 
2020
AIDS research and human retroviruses
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