Abstract: Compound 7d was found to be the most potent one against both wild type (EC50 = 12.1 nM) and E138K mutant strains (EC50 = 0.0270 microM).
HIV-1 Drug Resistance, Distribution of Subtypes, and Drug Resistance-Associated Mutations in Virologic Failure Individuals in Chengdu, Southwest China, 2014-2016.
Result: E138A/G/R/K/Q was found in this case and was predicted to have low/potential resistance to RPV and ETR.
Drug Resistance Mutations Against Protease, Reverse Transcriptase and Integrase Inhibitors in People Living With HIV-1 Receiving Boosted Protease Inhibitors in South Africa.
Discussion: The group receiving AZT plus 3TC or ABC plus 3TC showed the highest rates of NNRTI mutations such as P225H, V106M, E138A/G/K/Q, G190A/S, and Y188L occurred most frequently in patients receiving AZT plus 3TC or ABC plus 3TC.
Pharmaceutical, clinical, and resistance information on doravirine, a novel non-nucleoside reverse transcriptase inhibitor for the treatment of HIV-1 infection.
Introduction: Across those clinical isolates (no subtype information was provided), DOR displayed a good antiviral activity with fold changes in EC50<9 against most single mutant viruses, including A98G, E138A/G/K/Q, G190A, K101E/P, K103N/S, L100I, P236L, V106M, V108I, V197D, V90I, Y181C/V, and Y188H/C.
Introduction: The highest levels of reduction in DOR susceptibility were associated with V106A or Y188L or each of these two
Impact of genotypic diversity on selection of subtype-specific drug resistance profiles during raltegravir-based therapy in individuals infected with B and BF recombinant HIV-1 strains.
PMID: 32125378
2020
The Journal of antimicrobial chemotherapy
Abstract: INI DRMs differed between B and F IN subtypes, with Q148K/R/H, G140S and E138K/A being more prevalent in subtype B (63% versus 0%, P = 0.0021; 50% versus 0%, P = 0.0096; and 50% versus 0%, P = 0.0096, respectively).
Design of Biphenyl-Substituted Diarylpyrimidines with a Cyanomethyl Linker as HIV-1 NNRTIs via a Molecular Hybridization Strategy.
Result: Compounds with 3-F (10c-p) displayed better activity than the marketed drug 3TC on mutant E138K except for 10h and 10i.
Result: In the E138K RT (Figure 4G), the binding mode was similar to the WT RT.
Result: Most compounds showed submicromolar activities against E138K, Y181C, K103N, and L100I variants.
Result: Notably, compound 10p exhibited the best EC50 values of 0.17, 0.87, 0.90, and 1.21 microM against the single mutant strains E138K, Y181C, K103N, and L100I, especially for the mutant strains of E138K,
High prevalence of integrase mutation L74I in West African HIV-1 subtypes prior to integrase inhibitor treatment.
PMID: 32105319
2020
The Journal of antimicrobial chemotherapy
Result: Four had T97A [this was the consensus in three of them and a minority variant in one (who also had L74I)], another participant had an E138K minority variant and another had a G140A minority variant.
Integrase strand transfer inhibitor (INSTI)-resistance mutations for the surveillance of transmitted HIV-1 drug resistance.
PMID: 31617907
2020
The Journal of antimicrobial chemotherapy
Abstract: Among the 29 relatively common INSTI-selected mutations, 24 emerged as candidates for inclusion on a list of INSTI surveillance drug-resistance mutations: T66A/I/K, E92G/Q, G118R, F121Y, E138A/K/T, G140A/C/S, Y143C/H/R/S, S147G, Q148H/R/K, N155H, S230R and R263K.
HIV-1 integrase drug-resistance mutations in Iranian treatment-experienced HIV-1-infected patients.
HIV mutation literature information.
PMID: 
2020
Bioorganic chemistry
Browser Board
Co-occurred Entities
Filtrator
ViMRT