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.
Patterns of acquired HIV-1 drug resistance mutations and predictors of virological failure in Moshi, Northern Tanzania.
HIV Drug Resistance Mutations in Patients with HIV and HIV-TB Coinfection After Failure of First-Line Therapy: A Prevalence Study in a Resource-Limited Setting.
PMID: 31117863
2019
Journal of the International Association of Providers of AIDS Care
Table: F227L
Prevalence of predicted resistance to doravirine in HIV-1-positive patients after exposure to non-nucleoside reverse transcriptase inhibitors.
PMID: 30769200
2019
International journal of antimicrobial agents
Abstract: High-level DOR resistance was defined as detection of any of Y188L, M230L, G190E, V106A/M+F227L, and V106A/M+L234I.
Identification of Dihydrofuro[3,4- d]pyrimidine Derivatives as Novel HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors with Promising Antiviral Activities and Desirable Physicochemical Properties.
PMID: 30624934
2019
Journal of medicinal chemistry
Abstract: Meanwhile, both compounds exhibited comparable activities with ETV toward the virus with double mutations F227L+V106A and K103N+Y181C.
Result: Five mutations (L100I, Y181C, Y188L, F227L, and V106) are located in the hydrophobic pocket that accommodates the benzonitrile and benzamide moieties of the ligand.
Result: For F227L+V106A, 13c3 (EC50 = 7.2 nM) showed the highest potency and was 2.7-fold more potent than ETV (EC50 = 19.7 nM).
Result: Moreover, 13a1, 13c1, 13c2, and 13c4 also inhibited F227L+V106A (EC50 = 13.7, 12.7, 19.0, and 10.5 nM) to
Rare occurrence of doravirine resistance-associated mutations in HIV-1-infected treatment-naive patients.
PMID: 30476106
2019
The Journal of antimicrobial chemotherapy
Abstract: We studied the prevalence of doravirine resistance-associated mutations previously identified in vitro: V106A/M, V108I, Y188L, V190S, H221Y, F227C/L/V, M230I/L, L234I, P236L, Y318F and K103N/Y181C.
Discovery of novel indolylarylsulfones as potent HIV-1 NNRTIs via structure-guided scaffold morphing.
PMID: 31434039
2019
European journal of medicinal chemistry
Abstract: Furthermore, some compounds maintained excellent activity against various single HIV-1 mutants (L100I, K103 N, E138K, Y181C) as well as one double mutant (F227L/V106A) with EC50 values in low-micromolar concentration ranges.
Abstract: Notably, 34 displayed outstanding potency against F227L/V106A (EC50 = 0.094 muM), and also showed exceptional activity against E138K (EC50 = 0.014 muM), L100I (EC50 = 0.011 muM) and K103 N (EC50 = 0.025 muM).
Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1.
PMID: 29353724
2018
European journal of medicinal chemistry
Abstract: Compound 4b displayed an EC50 value of 1 nM against HIV-1 IIIB, 1.3 nM against L100I, 0.84 nM against K103 N, 1.5 nM against Y181C, 11 nM against Y188L, 2 nM against E138K, 10 nM against K103 N + Y181C, and almost 110 nM against F227L + V106.
HIV mutation literature information.
PMID: 
2020
European journal of medicinal chemistry
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