Abstract: One NRTI-associated (M184V/I) and three NNRTI-associated (K103N/S, Y181C/I and G190A/S) mutations had high percentages in ART-naive and ART-treated individuals, and these mutations conferred high-level resistance to 3TC, EFV and/or NVP.
Result: Furthermore, Y181C/I was predominant in B, CRF01_AE and other subtypes, whereas V106aA/M was predominant in CRF07_BC.
Result: Low percentages of NRTI and NNRTI mutations, but a very high percentage (47.7%) of PI mutation (M46I/L) occurred in CRF01_AE; in contrast, high percentages of
Pharmacophore-fusing design of pyrimidine sulfonylacetanilides as potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Comparison of HIV drug resistance profiles across HIV-1 subtypes A and D for patients receiving a tenofovir-based and zidovudine-based first line regimens in Uganda.
Result: Within the NNRTI class, G190 mutations (69.1%, p = 0.015), Y181C (78.6%, p = 0.008), L100I (82.4%, p = 0.019) were significantly more in the TDF/3TC/EFV group whereas mutation K238T (71.4%, p = 0.035) was significantly more in the AZT/3TC/EFV group.
Discussion: Within the NNRTI class, G190 mutations (38 (69.1%), p = 0.015), Y181C/I/Y (22 (78.6%), p = 0.008) and L1001 (14 (82.4%), p = 0.019) mutations were significantly noted more in TDF/3TC/EFV whereas K238T (10 (71.4%), p = 0.034) noted more in AZT/3TC/EFV regimen.
Discovery, synthesis, and optimization of an N-alkoxy indolylacetamide against HIV-1 carrying NNRTI-resistant mutations from the Isatis indigotica root.
PMID: 32004936
2020
European journal of medicinal chemistry
Conclusion: Moreover, the two candidates strongly suppressed NNRTI-resistant HIV-1 carrying the RT-K103N/Y181C mutation.
Method: The complex structure was obtained from the Protein Data Bank (WT RT: 1TL1, Y181C RT: 1JLB, K103N-Y181C double-mutated RT: 5VQY, L100I-K103N double-mutated RT: 2ZE2).
Table: Y181C
Figure: Binding modes of 10i into the NNBS of (a) HIV-1 Y181C RT (PDB code: 1JLB); (b) HIV-1 K103N/
Prevalence of doravirine-associated resistance mutations in HIV-1-infected antiretroviral-experienced patients from two large databases in France and Italy.
PMID: 31976534
2020
The Journal of antimicrobial chemotherapy
Abstract: In comparison, the prevalence of the common NNRTI mutations V90I, K101E/P, K103N/S, E138A/G/K/Q/R/S, Y181C/I/V and G190A/E/S/Q were higher (8.9%, 7.9%, 28.6%, 12.6%, 14.2% and 8.9%, respectively).
Abstract: RESULTS: The frequencies of doravirine-associated resistance mutations (total dataset versus NNRTI-failing patients) were: V106A/M, 0.8% versus 2.6%; V108I, 3.3% versus 9.2%; Y188L, 1.2% versus 2.6%; G190S, 0.3% versus 2.1%; F227C/L/V
Long-Acting Rilpivirine (RPV) Preexposure Prophylaxis Does Not Inhibit Vaginal Transmission of RPV-Resistant HIV-1 or Select for High-Frequency Drug Resistance in Humanized Mice.
Abstract: Mutations K103N, Y181C, G190A, M184V and K65R were detected by an oligonucleotide ligation assay (OLA) and confirmed by Sanger and next-generation sequencing (NGS).
Method: The OLA detected mutations conferring high-level resistance to NVP/EFV (K103N, Y181C, G190A), 3TC (M184V) and beginning in 2010 to TDF (K65R) using probes optimized for HIV type-1 subtypes A, D and C.
Discussion: An economical and easy to use point of care OLA kit that assesses NNRTI mutations K103N, Y181C, G190A
Indazolyl-substituted piperidin-4-yl-aminopyrimidines as HIV-1 NNRTIs: Design, synthesis and biological activities.
PMID: 31767136
2020
European journal of medicinal chemistry
Abstract: And also, it displayed potent activities against K103 N (EC50 = 0.077 muM), Y181C (EC50 = 0.11 muM), E138K (EC50 = 0.057 muM), and moderate activity against double mutants RES056 (EC50 = 8.7 muM).
Human Immunodeficiency Virus-1 Viral Load Is Elevated in Individuals With Reverse-Transcriptase Mutation M184V/I During Virological Failure of First-Line Antiretroviral Therapy and Is Associated With Compensatory Mutation L74I.
PMID: 31774913
2020
The Journal of infectious diseases
Result: The following NNRTI mutations were also associated: A98G, L100I, K103R, V108I, Y181C, Y188L, G190A, P225H, L228R, and M230L.
Evaluation of the management of pretreatment HIV drug resistance by oligonucleotide ligation assay: a randomised controlled trial.
Abstract: The OLA-guided therapy group had pre-ART peripheral blood mononuclear cells evaluated for drug resistance to
Method: Peripheral blood mononuclear cells were evaluated for NNRTI and NRTI drug resistance mutations, K103N, Y181C, G190A, and K65R, and M184V, using a quantitative OLA.
Method: We classified participants prospectively as positive for ART resistance if any one of the HIV pol codons K103N, Y181C, G190A, or M184V had the drug-resistant genotype detected by OLA at >=10% frequency within the individual's viral quasispecies.
HIV mutation literature information.
PMID: 
2020
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