Abstract: Fourteen major mutations of codon 99-191 on the RT gene were selected (K103N, V106A/M, V108I, Q151M, Y181C/I, M184V/I, Y188C/L/H, and G190S/A) at a cost of testing of 35 USD.
Abstract: The prevalence of each HIVDR mutation were K103N 6.0%, V106I 1.1%, V108I 0.4%, Y181C 2.3%, Y181I 0.7%, Y181V 0.4%, M184V 3.0%, M184I 1.5%, and PMID: 26833152
2016
Antimicrobial agents and chemotherapy
Abstract: DOR displayed IQs of 39, 27, and 25 against the K103N, Y181C, and K103N/Y181C mutants, respectively.
Abstract: DOR exhibits potent antiviral activity against wild-type virus and K103N, Y181C, and K103N/Y181C mutant viruses, with 50% inhibitory concentrations (IC50s) of 12, 21, 31, and 33 nM, respectively, when measured in 100% normal human serum (NHS).
Abstract: No viral breakthrough was observed with DOR, whereas breakthrough viruses were readily detected with RPV and EFV against Y181C and K103N viruses, respectively.
Abstract: Resistance selections were conducted with K103N,
Time to Viremia for Patients Taking their First Antiretroviral Regimen and the Subsequent Resistance Profiles.
Abstract: One new NNRTI (Y181C) mutation was identified and three patients taking PI-based regimens developed NRTI mutations (M184 V, M184I, and T215Y).
Clinical Outcomes of Virologically-Suppressed Patients with Pre-existing HIV-1 Drug Resistance Mutations Switching to Rilpivirine/Emtricitabine/Tenofovir Disoproxil Fumarate in the SPIRIT Study.
Abstract: Mutations potentially affecting RPV activity, including E138A/G/K/Q, Y181C, and H221Y, were detected in isolates from 11 patients by one or both assays.
Abstract: One patient with pre-existing Y181Y/C and M184I by proviral DNA genotyping experienced virologic failure.
The Antiviral Activity of Approved and Novel Drugs against HIV-1 Mutations Evaluated under the Consideration of Dose-Response Curve Slope.
Result: However, the K103NH221YY181CT215Y mutation led to an intermediate shift in IC50 but a marked reduction in slope (Fig 3B).
Figure: (A) is the curve of the dose-response of 3 viruses (V179EH221YT215Y, V179EY181CT215Y and WT NL4.3) in d4T.
Figure: (B) is the curve of the dose-response of 2 viruses (K103NH221YY181CT215Y and WT NL4.3) in EFV.
Design, synthesis and evaluation of novel HIV-1 NNRTIs with dual structural conformations targeting the entrance channel of the NNRTI binding pocket.
PMID: 26994843
2016
European journal of medicinal chemistry
Abstract: Among them, compound 15b was identified as the most potent inhibitor with EC50 values of 0.11 muM and 2.18 muM against wt and K103N/Y181C double mutant HIV-1 strain (RES056), respectively.
Increasing HIV-1 pretreatment drug resistance among antiretroviral-naive adults initiating treatment between 2006 and 2014 in Nairobi, Kenya.
Abstract: Antiretroviral-naive adults initiating antiretroviral therapy in Nairobi, Kenya were tested for HIV-1 drug resistance at codons K103N, Y181C, G190A, M184V, and K65R using an oligonucleotide ligation assay.
Introduction: Fifteen of the participants had mutations only to NNRTI (K103N, Y181C, G190A), and three had mutations to NNRTI plus lamivudine (M184V).
Introduction: OLA examined point mutations at K103N, Y181C, G190A, and M184V across all s
Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.
PMID: 27070547
2016
Journal of medicinal chemistry
Result: Moreover, eight active compounds (EC50 < 5 nM against IIIB) were further tested in the MT-2 cell line against the multi-NRTI-resistant A17 viral strain with mutants K103N and Y181C, the two major mutants from the first-generation NNRTI drugs.
Rapid and Simultaneous Detection of Major Drug Resistance Mutations in Reverse Transcriptase Gene for HIV-1 CRF01_AE, CRF07_BC and Subtype B in China Using Sequenom MassARRAY(R) System.
Abstract: Y181C was the most common NVP-associated RAM (54.3% vs.
Result: For example, Y181C (52.7%) was the most common NNRTI-RAM detected in patients that failed NVP-based regimen compared to those that failed EFV-based regimen (14.0%; p<0.01).
Result: Overall, th
Discussion: Y181C is notoriously well-known for conferring a 5-fold reduction in susceptibility to ETR and a 3-fold reduction in susceptibility to RPV.
Discussion: The most common mutation for RPV in patients who failed NVP-based regimen, compared to the EFV-based regimen, was Y181C (52.7% vs.
Discussion: This particular nonpolymorphic mutation, Y181C, is one of the worst NNRTI-RAM and it has an intermediate-level resistance to both ETR and RPV.
HIV mutation literature information.
PMID: 
2016
PloS one
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