Abstract: A few of these hybrids displayed moderate inhibitory activity against wt HIV-1 replication at submicromolar level, however, all of them lacked inhibitory activity against the double mutant virus (K103N/Y181C), which is the most prevalent NNRTI resistant-associated double mutant observed in the clinic.
Abstract: The most promising hybrid 5c displayed a significant EC50 value of 0.0096 muM against HIV-1 IIIB and of 0.98 muM against K103N/Y181C.
HIV-1 Epidemiology, Genetic Diversity, and Primary Drug Resistance in the Tyumen Oblast, Russia.
Discussion: Among them, the mutations G190S, K103N, M184V, Y181C, K101E, M41L, and T215F/Y, influencing the HIV resistance to NRTIs and NNRTIs, are observed at a high rate.
Discussion: Mutations K103N, M184I, T215Y, G190S, Y181C, K65R, and V108I with prevalences of 0.3 to 7% depending on the region are most frequently detected in the naive HIV-infected individuals.
From antiretroviral therapy access to provision of third line regimens: evidence of HIV Drug resistance mutations to first and second line regimens among Ugandan adults.
Abstract: The major Non-NRTI (NNRTI) mutations were K103N-19.0%, G190A-7.0% and Y181C-6.0%.
Conclusion: The NNRTI mutations observed included K103N, G190A and Y181C which cause high level resistance to Nevirapine and variable resistance to Efavirenz.
Result: The commonest major NNRTI resistance mutations known to reduce susceptibility or virological response to NNRTIs were: K103N:19.0%, G190A:7.0% and Y181C:6.0%.
Table: Y181C
Molecular dynamics and Monte Carlo simulations for protein-ligand binding and inhibitor design.
Result: 1 might differentially improve potency against the Y181C-bearing variants of HIV-RT.
Result: As was demonstrated in MCPRO simulations of the benzyoxazole inhibitors, the Y181C mutation increases the available space for accommodation of a bulkier R-group.
Result: Experimentally, the R = Et and i-Pr analogues are equally potent and are both sub-10 nM inhibitors of replication of the Y181C viral strain.
Result: Table 2 collects the relative free energies of binding of seven benzyloxazole analogues, for both the wild-type and Y181C mutant, and compares them with previously reported MCPRO (using REST enhanced sampling) and experimental EC50 results.
Result: Turning to the Y181C mutant, the results from Desmond do indic
Two-year outcome of first-line antiretroviral therapy among HIV-1 vertically-infected children in Hanoi, Vietnam.
PMID: 25332224
2015
International journal of STD & AIDS
Abstract: Y181C and M184V/I were the most dominant non-nucleoside and nucleoside RTI-resistance mutations, respectively (13/15, 86.7%).
Archived HIV-1 DNA resistance mutations to rilpivirine and etravirine in successfully treated HIV-1-infected individuals pre-exposed to efavirenz or nevirapine.
PMID: 25344807
2015
The Journal of antimicrobial chemotherapy
Abstract: Rilpivirine RAMs were detected in 41 (32%) individuals, with highest frequency for the mutations Y181C/I/V (18%), K101E/P (7%) and E138A/G/K/Q/R/S (6%) and the association L100I+K103N/S (5%).
Design, Synthesis, and Anti-HIV Evaluation of Novel Triazine Derivatives Targeting the Entrance Channel of the NNRTI Binding Pocket.
PMID: 25358434
2015
Chemical biology & drug design
Abstract: Some compounds displayed submicromolar activity against the K103N/Y181C resistant mutant strain (such as compound DCS-a4, EC50= 0.65 mum).
Impact of drug resistance-associated amino acid changes in HIV-1 subtype C on susceptibility to newer nonnucleoside reverse transcriptase inhibitors.
PMID: 25421485
2015
Antimicrobial agents and chemotherapy
Abstract: Y181C, a major NNRTI resistance-associated amino acid substitution, caused decreased susceptibility to ETR and, to a lesser extent, RPV when combined with other mutations.
In vitro selection of HIV-1 CRF08_BC variants resistant to reverse transcriptase inhibitors.
PMID: 25482475
2015
AIDS research and human retroviruses
Abstract: Phenotypic analyses showed that E138R, Y181C, and G190A contributed high-level resistance to NVP, while L100I and V106L significantly reduced virus susceptibility to EFV.
Abstract: Three different resistance patterns led by initial mutations of Y181C, E138G, and Y188C were detected after the selection with NVP.
Synthesis and biological evaluation of DAPY-DPEs hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Abstract: A series of new DAPY-DPEs hybrids, combined the important pharmacophores of DAPYs and DPEs, has been synthesized and biologically evaluated for their anti-HIV activities against wild-type HIV-1 strain IIIB, double RT mutant (K103N+Y181C) strain RES056 and HIV-2 strain ROD in MT-4 cell cultures.
HIV mutation literature information.
PMID: 
2016
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