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).
Trend of HIV transmitted drug resistance before and after implementation of HAART regimen restriction in the treatment of HIV-1 infected patients in southern Taiwan.
Abstract: Among the detected mutations, K103 N and V179D + K103R were more frequently observed after 2012.
Abstract: Four HIV-infected patients with K103 N variants were detected after 2012, and 4 of the 5 patients with V179D + K103R variants were found after 2012.
Discussion: Although there was no significant change in the prevalence of K103 N mutations before and after 2012 (P = 0.32), the K103 N TDR should be monitored closely because NNRTIs are still used as a first-line ART in Taiwan.
Discussion: As NNRTIs are still widely prescribed as a once-daily single tablet reg
National survey of pre-treatment HIV drug resistance in Cuban patients.
Abstract: The most frequent mutations detected were K103N (12.9%), G190A (6.4%) and Y181C (4.8%).
Result: The most frequent mutations were K103N (12.1%); G190A (5.7%); Y181C (4.3%), which are associated with the high values of resistance to NNRTI described in the study (Table 2).
Table: K103N
Discussion: The sustained use of NVP or EFV in the first therapeutic line could favor the accumulation of mutations associated with resistance to these drugs (K103N, G190A and Y181C) and the subsequent transmission of the variants with these changes to the population.
Surveillance of transmitted HIV drug resistance among newly diagnosed, treatment-naive individuals at a county HIV clinic in Santa Clara County.
Result: K103N (5.8%) comprised of the majority of NNRTI TDRMs.
Discussion: Atripla was commonly prescribed since its approval by the US Food and Drug Administration (FDA) in 2006, and its widespread use likely led to the preeminence of NNRTI TDR (K103N in particular).
Molecular Genetics and the Incidence of Transmitted Drug Resistance Among Pre-Treatment HIV-1 Infected Patients in the Eastern Cape, South Africa.
Abstract: K103N/S, V106M and M184V were the most common mutations identified among the viral sequences.
HIV-1 subtype diversity, drug resistance, and genetic transmission networks in men who have sex with men with virologic failure in antiretroviral therapy in Sichuan, China, 2011 to 2017.
Abstract: The most common drug resistance-associated mutations in protease inhibitors (PIs), NRTIs and NNRTIs were K20I/R, M184V/I and K103N/KN, respectively.
Result: K103N/KN (155/372,
Discussion: We observed that K103N/KN, V106M/MA/MV, G190A/AG/S, and Y188L/C are the major NNRTI-related mutations in China and other countries, which may be the result of the wide-spread use of NNRTIs.
HIV Drug Resistance after Failure of 6 Month First-line Therapy in a Hospital: A Case Series.
Abstract: The phylogenetic analyses of the amplified region of pol gene indicated that all of the 15 HIV-1-infected pediatric patients were infected by CRF35_AD, and a total of 13.3% (2/15) of these children were infected with HIV-1 variants with SDRMs (one child harbored two related SDRMs [D67N, V179F], and another child had three related SDRMs [M184V, T215F, and K103N]), according to the last algorithm of the WHO.
[Postmortem Molecular Epidemiology of HIV-1 Strains Isolated in Turkey].
HIV mutation literature information.
PMID: 
2019
European journal of medicinal chemistry
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