Abstract: Among the 40 ART-naive patients, two mutations associated with nucleoside reverse transcriptase inhibitor (NRTI) resistance (two with Y115F and T215I) and three associated with non-nucleoside reverse transcriptase inhibitor (NNRTI) resistance (two with G190S and Y181C, four with V179T) were found.
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
Abstract: Lead compound 8 inhibited RT with submicromolar potency (IC50=0.73muM) and also maintained some activity against the clinically important RT mutants K103N and Y181C (IC50=9.2, 3.5muM) in cell-free assays.
Introduction: Compounds 8 and 9 also demonstrated some activity against the Y181C and E138K mutants.
Introduction: It did demonstrate some potency against the Y181C RT mutant in the cell-free assay (IC50 = 6.69 muM, data not shown), but was inactive against the K103N, V108I, and E138 K forms of the enzyme.
Introduction: The three most active compounds against wild type
Design, Synthesis, and Evaluation of Thiophene[3,2-d]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles.
PMID: 27541578
2016
Journal of medicinal chemistry
Abstract: Compound 27 was the most potent; compared with ETV, its antiviral efficacy was 3-fold greater against WT, 5-7-fold greater against Y181C, Y188L, E138K, and F227L+V106A, and nearly equipotent against L100I and K103N, though somewhat weaker against K103N+Y181C.
Cross-sectional study of virological failure and multinucleoside reverse transcriptase inhibitor resistance at 12 months of antiretroviral therapy in Western India.
Introduction: In one of the prior large study involving genotyping of 138 patients with failure from South India, M184V and Y181C emerged as most common NRTI and NNRTI mutations, respectively.
Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile.
PMID: 27645238
2016
Antimicrobial agents and chemotherapy
Method: The nonnucleoside reverse transcriptase inhibitor (NNRTI)-resistant viruses encoding RT mutation K103N, Y181C, Y188L, or L100I/Y181C were constructed by site-directed mutagenesis.
Biophysical Characterization of Novel DNA Aptamers against K103N/Y181C Double Mutant HIV-1 Reverse Transcriptase.
Introduction: Another prevalent NNRTI-resistant mutation is Y181C substitution, which is present in 15%-25% of
Method: Full-length WT and two mutant RT proteins (K103N and Y181C) were expressed in Escherichia coli BL21 (DE3) cells and purified as described previously.
Result: As expected, Y181C RT is highly resistant to NVP and DLV, but not EFV.
Result: The bio-RTs (WT, K103N, or Y181C) were tested for their susceptibility to various NNRTIs and compared with respective non-biotinylated RTs (non-bio-RTs).
HIV Drug Resistance in Antiretroviral Treatment-Naive Individuals in the Largest Public Hospital in Nicaragua, 2011-2015.
Discussion: Only four of the patients with M41L (all with long-standing infection) also presented other low-abundance DR variants (<5%): K103N, Y181C, K65R, and PR G73S.
Prevalence of HIV Antiretroviral Drug Resistance and Its Impacts on HIV-1 Virological Failures in Jiangsu, China: A Cross-Sectional Study.
Result: K103N, Y181C, G190A, and V108I were the most prevalent mutations associated with NNRTIs resistance and the frequencies were 33.70%, 29.35%, 27.17%, and 27.17%, respectively (Figure 2(b)).
Discussion: K103N causes high-level resistance to NVP and EFV and Y181C can cause high-level resistance to NVP and intermediate resistance to EFV.
Discussion: K103N, Y181C were the most prevalent mutations associated with NNRTI resistance in our study.
Synthesis and biological evaluation of benzophenone derivatives as potential HIV-1 inhibitors.
PMID: 27834135
2016
Medicinal chemistry (Shariqah (United Arab Emirates))
Abstract: GW678248, is one of the most potent benzophenone derivatives, exhibiting high potency against a panel of HIV-1 virus (wild-type, K103N mutant, Y181C, etc.) at 1 nM/L concentrations.
Correlates of infection and molecular characterization of blood-borne HIV, HCV, and HBV infections in HIV-1 infected inmates in Italy: An observational cross-sectional study.
Abstract: Variants carrying the K103N and Y181C resistance mutations to non-nucleoside reverse transcriptase inhibitors (NNRTIs) were found in 2 out of 9 patients naive for combined antiretroviral therapy (cART) (22.2%).
Result: More important, 2 out of 9 patients naive for cART (22.2%) hosted variants that carried the K103N (in one patient) and the Y181C (in the other patient) mutations, both directed to drugs of the NNRTI class.
Discussion:
Discussion: Mutations were the K103N in 1 case and the Y181C in the other case, both known to be major DRMs to NNRTI drugs, according to the Stanford database (http://hivdb.stanford.edu/).
HIV mutation literature information.
PMID: 
2016
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