Molecular Hybridization-Inspired Optimization of Diarylbenzopyrimidines as HIV-1 Nonnucleoside Reverse Transcriptase Inhibitors with Improved Activity against K103N and E138K Mutants and Pharmacokinetic Profiles.
PMID: 27330069
2016
The Journal of antimicrobial chemotherapy
Abstract: E138K emerged in three patients while other rilpivirine resistance mutations emerged in the other three patients.
Abstract: E138K in HIV-1 reverse trans
Abstract: An unidentified mechanism could amplify resistance to rilpivirine conferred by E138K.
Abstract: Analysis of recombinant HIV-1 variants indicated that E138K conferred low-level rilpivirine resistance and that coexistence of I135T/L with E138K amplified the resistance.
Abstract: CONCLUSIONS: I135T/L, escape mutations from HLA-B*51/52-restricted cytotoxic T lymphocytes, which are prevalent in Japan, may predispose HIV-1 to harbour E138K upon failure of rilpivirine-containing ART.
Discovery, characterization, and lead optimization of 7-azaindole non-nucleoside HIV-1 reverse transcriptase inhibitors.
Introduction: Both drugs selected for mutations on RT, as the V108I mutant emerged after 69 weeks of treatment with 8 and E138K arose after 39 weeks of treatment with 9 (Supp.
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 V108I mutant is associated with resistance to first generation 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.
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
Figure: Primary INSTI resistance mutations are T66I/A/K, E92Q/G, T97A, Y143C/H/R, S147G, Q148H/K/R, and N155H, and other INSTI resistance mutations are H51Y, L68I/V, V72A/N/T, L74M, Q95K/R, F121C/Y, A128T, E138A/K, G140A/C/S, P145S, PMID: 27736898
2016
PloS one
Discussion: Using NGS, a total of 13 patients presented the E138A mutation over the 20% threshold and 10 additional patients presented E138 mutants as low-abundance variants <20%, including E138A, E138K and E138G.
Prevalence of Integrase Strand Transfer Inhibitors (INSTI) Resistance Mutations in Taiwan.
Discussion: Besides the Q148 mutation combined with one or more of G140A/C/S, L74I and E138A/K/T was identified to reduce viral susceptibility to dolutegravir, two amino acid mutations, G118R and R263K, have been reported to confer low-level resistance to dolutegravir.
Discussion: However, some of the mutations are significantly associated with raltegravir exposure, such as L74M, T97A, E138K, V151I and G163R.
Discussion: In patients experiencing virological failure to the first generation of INSTIs, raltegravir and elvitegravir, three genotypic mutation pathways have been de
Evolution of a novel pathway leading to dolutegravir resistance in a patient harbouring N155H and multiclass drug resistance.
PMID: 25281399
2015
The Journal of antimicrobial chemotherapy
Abstract: RESULTS: Five mutations (A49P, L68FL, T97A, E138K and L234V) were implicated in emergent dolutegravir resistance, with a concomitant severe compromise in viral replicative capacity.
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%).
In vitro resistance selection with doravirine (MK-1439), a novel nonnucleoside reverse transcriptase inhibitor with distinct mutation development pathways.
PMID: 25385110
2015
Antimicrobial agents and chemotherapy
Abstract: Mutations that are commonly associated with RPV and EFV in clinical settings were also identified in subtype B viruses such as the E138K and K103N mutants, respectively, in this in vitro resistance selection study.
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: The low-level resistance to RPV and ETR conferred by E138K was not significantly enhanced in the presence of M184V/I, unlike for EFV and NVP.
HIV mutation literature information.
PMID: 
2016
The Journal of antimicrobial chemotherapy
Browser Board
Co-occurred Entities
Filtrator
ViMRT