Method: Major INSTI resistance mutations (T66I, E92Q, F121Y, Y143CHR, S147G, Q148HKR, N155H) that confer substantial phenotypic resistance to at least one of the currently approved INSTI as well as minor INSTI resistance mutations (T66AK, L74 M, E92G, T97A, E138AK, G140AS, R263K) that increase INSTI resistance and/or viral
Upward trends of acquired drug resistances in Ethiopian HIV-1C isolates: A decade longitudinal study.
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: 28961903
2017
The Journal of antimicrobial chemotherapy
Abstract: CONCLUSIONS: These findings help to alleviate concern that EFdA may not be active against viruses that contain both the M184I/V and E138K substitutions in RT.
Abstract: In other clinical trials that evaluated rilpivirine together with emtricitabine in first-line therapy, the emergence of both the M184I/V and E138K mutations in RT was demonstrated.
Abstract: METHODS: Recombinant viruses containing the M184I/V and/or E138K substitutions were generated by site-directed mutagenesis and evaluated in tissue culture for susceptibility to various nucleoside compounds, including EFdA.
Abstract: Moreover, the E138K substitution was not genera
Week 48 resistance analysis of Elvitegravir/Cobicistat/Emtricitabine/Tenofovir DF versus Atazanavir + Ritonavir + Emtricitabine/Tenofovir DF in HIV-1 infected women (WAVES study GS-US-236-0128).
Abstract: A62V, V90I, K103N, or E138A/G/K/Q; 68-82%) demonstrated virologic suppression at week 48, with no resistance development except for one patient with M184V and pre-existing K103N
Result: Specifically, those participants with A62V, V90I, K103N, or E138A/G/K/Q/R in RT, or M46I/L or L33F in PR, had HIV-1 RNA <50 copies/mL at Week 48 after treatment with EVG/COBI/FTC/TDF or ATV+RTV+FTC/TDF at proportions similar to the overall treated population (Table 5).
Monotherapy with either dolutegravir or raltegravir fails to durably suppress HIV viraemia in humanized mice.
PMID: 28637235
2017
The Journal of antimicrobial chemotherapy
Abstract: The virus from this mouse had mutations E138K, G140S, Q148H, N155H and S230R, was highly resistant to both raltegravir (EC50 of >1000 nM) and dolutegravir (EC50 of 550 nM), and replicated to levels similar to those of control viruses in PBMCs.
High level of HIV-1 drug resistance mutations in patients with unsuppressed viral loads in rural northern South Africa.
Result: E138A/K/Q, a mutation related to the NNRTIs etravirine (ETR) and rilpivirine (RPV) was found in 8.6% of subjects, although these drugs are not currently available and not part of the standard treatment regimen in South Africa.
Result: Excluding E138A/K/Q among
Discussion: In fact, in the Stanford Drug Resistance database, subtype C strains from drug exposed patients have a higher prevalence of the E138A/K/Q mutation compared to other group M strains (8-9.5% vs.
Discussion: Similarly, we speculate that the occurrence of the E138A/K/Q mutation could be due to the codon usage of subtype C RT at this position which is GAA versus GAG in other group M strains.
Antiviral Activity of Bictegravir and Cabotegravir against Integrase Inhibitor-Resistant SIVmac239 and HIV-1.
PMID: 28923862
2017
Antimicrobial agents and chemotherapy
Abstract: In both single and multiple rounds of HIV-1 infections, BIC remained active against the Y143R, N155H, R263K, R263K/M50I, and R263K/E138K mutants (<=4-fold increase in EC50).
Comparison between next-generation and Sanger-based sequencing for the detection of transmitted drug-resistance mutations among recently infected HIV-1 patients in Israel, 2000-2014.
PMID: 28799325
2017
Journal of the International AIDS Society
Result: Some of the low-frequency TDRMs identified are consistent with APOBEC-mediated G-to-A editing: the PI M46L/I and D30N, the NRTI D67N and the NNRTI G190E TDRM, as well as the E138K amino substitution, were all related to APOBEC.
HIV Drug Resistance in Antiretroviral Treatment-Naive Individuals in the Largest Public Hospital in Nicaragua, 2011-2015.
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
HIV mutation literature information.
PMID: 
2017
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