Result: In our covariation analysis, four death-associated mutations (T39A, K43E, L74I, and Y181C) were significantly associated with M184V.
Result: In the network, drug resistance mutations with higher covariation (e.g., M41L, D67N, K101E, K103N, Y181C, M184V, L210W, T215F, and T215I) were more likely to influence the other mutations.
Result: Most drug resistance mutations (L74I, Table: Y181C
HIV-1 drug-resistant mutations and related risk factors among HIV-1-positive individuals experiencing treatment failure in Hebei Province, China.
Result: In NNRTI coding regions, K103 N was the most frequent mutation, accounting for 15.9% (34/214), followed by Y181C (11.7%, 25/214), G190A (5.1%, 11/214), and G190S (3.7%, 8/214).
Table: Y181C
Discussion: For example, Y181C can increase HIV-1 subtype B replicative capacity.
Discussion: In this study, the most common mutations (M184V/I, K103N, Y181C, etc.) proved HIV-1 fitness to drugs, suggesting that HIV-1 resistant strains would spread out.
HIV Drug Resistance Mutations in Non-B Subtypes After Prolonged Virological Failure on NNRTI-Based First-Line Regimens in Sub-Saharan Africa.
PMID: 28129253
2017
Journal of acquired immune deficiency syndromes (1999)
Result: After adjustment, participants on zidovudine at failure were more likely to have T215F, T215Y, M41L, K70R, D67N, L210W, type-1 thymidine analog, type-2 thymidine analog, and any thymidine analogue mutations (TAMs); those on tenofovir to have K65R, K70E, Y115F, and M184I; those on efavirenz to have K103N, P225H, Y188L, and L100I; and those on nevirapine to have Y181C and G190A.
Result: Supplemental Digital Content, Table 1b, htt
Surveillance of HIV-1 pol transmitted drug resistance in acutely and recently infected antiretroviral drug-naive persons in rural western Kenya.
Etravirine combined with antiretrovirals other than darunavir/ritonavir for HIV-1-infected, treatment-experienced adults: Week 48 results of a phase IV trial.
Abstract: The most frequently emerging etravirine resistance-associated mutations in virologic failures were Y181C, E138A, and M230L.
Result: The most frequently emerging etravirine RAMs (developing in >=5 VFs) were Y181C (18/49), E138A (5/49), and M230L (5/49).
Discussion: The most frequently emerging etravirine RAMs, Y181C, E138A, and M230L (>=5 VFs) have also been observed previously in patients with VF in etravirine trials, as has the only other NNRTI RAM that emerged in >=5 VFs, H221Y.
Transmission fitness of drug-resistant HIV revealed in a surveillance system transmission network.
Abstract: K103N, Y181C, and L90M) had transmission fitness that was indistinguishable from or exceeded wild-type fitness, permitting the establishment of large, self-sustaining drug resistance reservoirs.
Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
PMID: 28481112
2017
Journal of medicinal chemistry
Abstract: Compound 25a was exceptionally potent against the whole viral panel, affording 3-4-fold enhancement of in vitro antiviral potency against WT, L100I, K103N, Y181C, Y188L, E138K, and K103N+Y181C and 10-fold enhancement against F227L+V106A relative to the reference drug etravirine (ETV) in the same cellular assay.
In Vitro Cross-Resistance Profiles of Rilpivirine, Dapivirine, and MIV-150, Nonnucleoside Reverse Transcriptase Inhibitor Microbicides in Clinical Development for the Prevention of HIV-1 Infection.
PMID: 28507107
2017
Antimicrobial agents and chemotherapy
Abstract: However, MIV-150 genital tract concentrations may be insufficient to inhibit many resistant viruses, including those harboring K103N or Y181C.
Use of Proviral DNA to Investigate Virus Resistance Mutations in HIV-infected Zimbabweans.
Abstract: Six-percent (n=6) had at least one HIVDR mutation, comprising NRTI-associated mutations, (M184V, T69D, T69N and V75I); NNRTI-associated mutations (G190A, K103N, V106M, Y181C) and thymidine analogue associated mutations (D67N, K70R, K219Q, L210W, M41L, T215Y).
Result: The mutations observed were; NRTI mutations T69D, T69N
Inhibition activities of catechol diether based non-nucleoside inhibitors against the HIV reverse transcriptase variants: Insights from molecular docking and ONIOM calculations.
PMID: 28623781
2017
Journal of molecular graphics & modelling
Abstract: The binding efficacies of the inhibitors are significantly suppressed by the Y181C and K103N mutations, as revealed by the computed interaction energies at the ONIOM [B3LYP/6-31G(d,p):PM6] level of theory.