High resistance to reverse transcriptase inhibitors among persons infected with human immunodeficiency virus type 1 subtype circulating recombinant form 02_AG in Ghana and on antiretroviral therapy.
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: RPV LA significantly prevented vaginal transmission of WT HIV-1 and Y181C HIV-1, which is 3-fold resistant to RPV.
Abstract: Vaginal challenges of wild-type (WT), Y181C, and Y181V HIV-1 were performed in mice left untreated or after RPV PrEP.
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.
Pretreatment HIV drug resistance spread within transmission clusters in Mexico City.
PMID: 31819984
2020
The Journal of antimicrobial chemotherapy
Result: Other commonly observed NNRTI DRMs included G190A, Y188L, Y181C and K101E (Figure 1c).