Prevalence and characteristics of HIV drug resistance among antiretroviral treatment (ART) experienced adolescents and young adults living with HIV in Ndola, Zambia.
Review of Doravirine Resistance Patterns Identified in Participants During Clinical Development.
PMID: 32925358
2020
Journal of acquired immune deficiency syndromes (1999)
Introduction: Results with subtype A virus were similar to those observed with subtype B; the major resistance pathway started with the development of the RT V106A mutant at a lower DOR concentration, followed by the RT F227L mutant as DOR concentrations increased.
Introduction: The V106A, V106A/L234I, and V106A/ Introduction: The development of resistance was characterized by the selection of RT mutants with the V106A substitution, followed by the emergence of substitutions of F227L or L234I with escalating DOR concentrations.
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
Pharmaceutical, clinical, and resistance information on doravirine, a novel non-nucleoside reverse transcriptase inhibitor for the treatment of HIV-1 infection.
Introduction: It is thus possible that the F227L substitution per se may confer only low-level resistance against DOR.
Introduction: Mutations that emerged secondary to V106A/M included F227L/C/V or L234I.
Introduction: Other in vitro studies confirmed that viruses bearing both V106A and F227L substitutions reduced DOR susceptibility >500-fold.
Introduction: The double mutant viruses V106A/L234I (subtype B) and V108I/L234I (subtype A) eventually acquired a third mutation to give triple mutant viruses V106A/L234I/ PMID: 32111013
2020
Molecules (Basel, Switzerland)
Result: The pi-pi stacking interactions were reduced by Y181C and F227L mutations with decreased aromatic rings.
Result: The binding modes of 10p with double mutant (F227L + V106A, K103N + Y181C) RT were also predicted (see Figure S1, Supplementary Materials).
Result: These compounds were also tested in the MT-4 cells for their activities against the single mutant (L100I, E138K, Y181C, K103N, Y188L) and double RT mutant (K103N <
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.
Abstract: Non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance mutations, K103N, Y181C, V90I, F227L, and V106A were also prevalent.
Discussion: NNRTI associated mutations detected included V90I, K103N, Y181C, H221Y, K101H, G190A, V106A, F227L, and K238T.
HIV-1 acquired drug resistance to integrase inhibitors in a cohort of antiretroviral therapy multi-experienced Mexican patients failing to raltegravir: a cross-sectional study.
The algorithm used for the interpretation of doravirine transmitted drug resistance strongly influences clinical practice and guideline recommendations.
PMID: 32030406
2020
The Journal of antimicrobial chemotherapy
Abstract: METHODS: We used the WHO 2009 list to investigate the prevalence of NNRTI, NRTI and PI TDR, in treatment-naive HIV-1-infected patients, adding mutations E138A/G/K/Q/R, V106I, V108I, V179L, G190Q, H221Y, F227C/L/V, M230IDR, L234I, P236L and Y318F in RT.
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: 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, 0.5% versus 1.8%; M230I/L, 2.8% versus 0%; L234I, 0.1% versus 0.5%; K103N + Y181C, 3.9% versus 3.9%; K103N + P225H, 2.9% versus 4.7%; and K103N + L100I, 1.7% versus 3.9%, with a significantly higher proportion of these mutations in the
Scaffold Hopping in Discovery of HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors: From CH(CN)-DABOs to CH(CN)-DAPYs.
5Result: As shown in Figure 5A-C, B4 efficiently occupied the pockets of the single amino acid mutations K103N and E138K and the double mutants F227L + V106A with an approximately ""U"" conformation, which was one of the essential condition for the antiviral activity in the DAPY scaffold."
Result: Compound B6 exhibited the highest potency against the double mutant F227L + V106A among all target compounds with EC50 values of 1.52 muM.
Result: Furthermore, compounds B3-B6 were superior to NVP (EC50 = 4.28 muM) toward the virus with double mutations F227L + V106A.
HIV mutation literature information.
PMID: 
2020
PloS one
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