Synthesis and Anti-HIV-1 Activity of a Novel Series of Aminoimidazole Analogs.
PMID: 20535242
2010
Letters in drug design & discovery
Introduction: Mutations associated with resistance to NNRTIs include L100I, K101E, K103N, V106A, V108I, V179D, Y181C, Y188C/L/H, G190A/E/S, M230L, P236L and Y318F.
Connection domain mutations in treatment-experienced patients in the OPTIMA trial.
PMID: 20130473
2010
Journal of acquired immune deficiency syndromes (1999)
Abstract: Frequencies of E312Q, Y318F, G333D, G333E, G335C, G335D, N348I, A360I, A360V, V365I, A371V, A376S, and E399G were compared with a treatment-naive population.
Etravirine: a second-generation NNRTI for treatment-experienced adults with resistant HIV-1 infection.
Introduction: In vitro studies suggest that etravirine selects for L100I, V179F/I, Y181C, G190E, M230L and Y318F, which may contribute to etravirine resistance (FC >10).
Connection domain mutations N348I and A360V in HIV-1 reverse transcriptase enhance resistance to 3'-azido-3'-deoxythymidine through both RNase H-dependent and -independent mechanisms.
PMID: 18547911
2008
The Journal of biological chemistry
Introduction: The rare G333D/E polymorphisms have been associated with dual resistance to AZT and other NRTIs, and few connection mutations, including Y318F and N348I, have been linked to decreased susceptibility to NNRTIs.
Impact of residues in the nonnucleoside reverse transcriptase inhibitor binding pocket on HIV-1 reverse transcriptase heterodimer stability.
Abstract: We found that the mutations K101A, P225H, Y318F and Y318W decreased RT heterodimer stability whereas K103N, V108I, V108W, Y181C, Y188L, G190A, G190E, G190W and P225W increased RT heterodimer stability.
N348I in the connection domain of HIV-1 reverse transcriptase confers zidovudine and nevirapine resistance.
Introduction: These include the G333D/E polymorphism that facilitates dual AZT/3TC resistance in viruses that contain both thymidine analogue mutations (TAMs) and M184V and the Y318F mutation that confers NNRTI resistance.
Resistance mutational analysis of HIV type 1 subtype C among rural South African drug-naive patients prior to large-scale availability of antiretrovirals.
PMID: 17209775
2006
AIDS research and human retroviruses
Abstract: Most of the RT sequences were wild-type, although V118I (8.5%) and Y318F (5.7%) associated with resistance to lamivudine and nevirapine, respectively, were observed.
Subtype-specific patterns in HIV Type 1 reverse transcriptase and protease in Oyo State, Nigeria: implications for drug resistance and host response.
PMID: 16910833
2006
AIDS research and human retroviruses
Abstract: Six of 35 (17%) individuals harbored primary mutations for RT inhibitors, including M41L, V118I, Y188H, P236L, and Y318F, and curiously three of the six were infected with CRF06_cpx.
TMC125 displays a high genetic barrier to the development of resistance: evidence from in vitro selection experiments.
Abstract: The selection experiments identified mutations selected by TMC125 that included known NNRTI-associated mutations L100I, Y181C, G190E, M230L, and Y318F and the novel mutations V179I and V179F.
A mutation in the 3' region of the human immunodeficiency virus type 1 reverse transcriptase (Y318F) associated with nonnucleoside reverse transcriptase inhibitor resistance.
Abstract: Combinations of Y318F with K103N, Y181C, or both resulted in decreased efavirenz susceptibility of 43-, 3.3-, and 84-fold, respectively, as well as >100- and >60-fold decreases in delavirdine and nevirapine susceptibility, respectively.
Abstract: The Y318F substitution in the 3' region of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) has been linked to nonnucleoside RT inhibitor (NNRTI) resistance in vitro.
Abstract: There was a significant association between Y318F and use of delavirdine (P = 10(-11)) and nevirapine (P = 10(-6)) but not efavirenz (P = 0.3).
Abstract: These results indicate the importance of the