Abstract: Certain Apolipoprotein B Editing Complex 3-related DRMs including reverse transcriptase gene mutations M184I, E138K, M230I, G190E and protease gene mutations M46I, D30N were enriched in hypermutated sequences but not in intact sequences or plasma sequences.
Pre-treatment integrase inhibitor resistance is uncommon in antiretroviral therapy-naive individuals with HIV-1 subtype A1 and D infections in Uganda.
Abstract: Of these, two had E138T (subtype A1), three had E138E/K (subtype D), and one had T66T/I (subtype D).
Increased acquired protease inhibitor drug resistance mutations in minor HIV-1 quasispecies from infected patients suspected of failing on national second-line therapy in South Africa.
Discussion: Previous studies on HIV-1C have shown major INI mutations at baseline in less than 5% of patients from Ethiopia (T66I, E138K, Q148R, and Q148H) and South Africa (Q148H, T66S, E92G, S147G, T66A, Y143YF and Y143H).
Identification of novel potent HIV-1 inhibitors by exploiting the tolerant regions of the NNRTIs binding pocket.
PMID: 33567378
2021
European journal of medicinal chemistry
Abstract: Compounds 16a1 and 16b1 turned out to be the most potent inhibitors against WT and mutant HIV-1 strains (L100I, K103N, and E138K), with EC50 values ranging from 0.007 muM to 0.043 muM.
Analysis and Molecular Determinants of HIV RNase H Cleavage Specificity at the PPT/U3 Junction.
Method: Double mutants E138K/M184I and E138K/M184V were prepared from the single-mutant E138K HIV-1 RT, previously described.
Method: Quadruple mutants E138K/M184I/N348I/T369I and E138K/M184V/N348I/T369I were obtained after introducing mutations E138K and M184I/V in sequential order, using as template the plasmid p66RTB containing the p66-coding sequence of mutant N348I/
Transmitted HIV-1 drug resistance in a large international cohort using next-generation sequencing: results from the Strategic Timing of Antiretroviral Treatment (START) study.
Abstract: TDR was based on the WHO 2009 surveillance definition with the addition of reverse transcriptase (RT) mutations T215N and E138K, and integrase strand transfer inhibitor (INSTI) surveillance mutations (Stanford HIVdb).
Result: K103NS variants were mainly observed (60/77, 78%) in > 80% of the viral quasispecies, E138K mainly (20/34, 59%) in < 5%, and G190ASE displayed a more uniform spread.
Result: The most common NNRTI DRMs - K103NS (3.5%), G190ASE (3.1%), and E138K (1.6%) - sh
"Design, synthesis, and evaluation of ""dual-site""-binding diarylpyrimidines targeting both NNIBP and the NNRTI adjacent site of the HIV-1 reverse transcriptase."
PMID: 33340914
2021
European journal of medicinal chemistry
Abstract: Of note, 14c exhibited potent activity against the single mutant strain E138K (EC50 = 10.6 nM), being comparable with ETR (EC50 = 9.80 nM) and 3.5-fold more potent than that of compound 7 (EC50 = 37.3 nM).
Molecular Network Analysis Reveals Transmission of HIV-1 Drug-Resistant Strains Among Newly Diagnosed HIV-1 Infections in a Moderately HIV Endemic City in China.
Abstract: TDR mutations detected in more than 10 cases were Q58E (n = 51), M46ILV (n = 46), K103N (n = 26), E138AGKQ (n = 25), K103R/V179D (n = 20), and A98G (n = 12).
Result: Transmitted drug resistance mutations detected in more than 10 cases included PI [Q58E (n = 51) and M46ILV (n = 46)] and NNRTI [K103N (n = 26), E138AGKQ (n = 25), K103R/V179D (n = 20), and A98G (n = 12)] m
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,
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).
HIV mutation literature information.
PMID: 
2021
AIDS (London, England)
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