Introduction: However, the landscape of antiretrovirals is changing continuously and new mutations such as E138A/G/K/Q/R (that confers resistance to the NNRTI rilpivirine (RPV), approved in 2011) are therefore not covered by this list.
Result: Mutations E138A/G/K/R were found in 99 of 186 viruses (52.9%) showing RPV resistance, which account for 40% of all NNRTI-resistant viruses.
Result: The NNRTI mutations at position E138 (
Result: The most common TDRMs found in baseline samples were the T215 revertants, followed by E138A/G/K/Q/R, K103NS, V179DE and M41L (S1 Table).
Exploiting the Tolerant Region I of the Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI) Binding Pocket: Discovery of Potent Diarylpyrimidine-Typed HIV-1 NNRTIs against Wild-Type and E138K Mutant Virus with Significantly Improved Water Solubility and Favorable Safety Profiles.
PMID: 30721060
2019
Journal of medicinal chemistry
Abstract: Diarylpyrimidine derivatives (DAPYs) exhibit robust anti-HIV-1 potency, although they have been compromised by E138K variant and severe side-effects and been suffering from poor water solubility.
Abstract: The anti-HIV-1 activities of 11c (EC50(WT) = 0.0035 muM, EC50(E138K) = 0.0075 muM) were the same as and 2-fold better than that of the lead etravirine against the wild-type and E138K mutant HIV-1, respectively, with a relative low cytotoxicity (CC50 >= 173 muM).
High predictive efficacy of integrase strand transfer inhibitors in perinatally HIV-1-infected African children in therapeutic failure of first- and second-line antiretroviral drug regimens recommended by the WHO.
PMID: 30891603
2019
The Journal of antimicrobial chemotherapy
Abstract: Two (2/18; 11.1%) viruses from children treated with a first-line regimen had INSTI DRMs at codon 138 (E138K and E138T), which is known to harbour major resistance mutations, and also had the accessory mutations L74I, G140K, G140R and G163R.
Result: In addition, the HIV-1 strain harbouring the E138K DRM also displayed accessory mutations G140K, G163R (Table 2) and APOBEC-related mutations not associated with resistance, including G82E, E85K, G106K, D116N, D167N
Delayed linkage to HIV care among asylum seekers in Quebec, Canada.
Result: One newly diagnosed patient, who was unknowingly prescribed functional monotherapy, developed full integrase inhibitor resistance (N155H, Q148R, S147G, E138K, and E92Q mutations).
Raltegravir-Induced Adaptations of the HIV-1 Integrase: Analysis of Structure, Variability, and Mutation Co-occurrence.
Abstract: The network and the structure analysis also support the hypothesis that the resistance-related E138K mutation may be a mechanism to compensate for mutations in neighbor lysine residues to maintain DNA binding.
Result: E138K co-occurs with three mutations of lysine residues, one of them in K156 (K156N).
Result: By the observed co-occurrence, E138K could also be compensating for K156N.
Result: It is also possible to see that except for Y143R and E138K, all the mutations on VG3 positions are in cluster A (Figure 6), which means they either co-occur or share co-occurring partners.
Result: Other mutations that co-occur with E138K are K215N and
Discovery of novel indolylarylsulfones as potent HIV-1 NNRTIs via structure-guided scaffold morphing.
PMID: 31434039
2019
European journal of medicinal chemistry
Abstract: Furthermore, some compounds maintained excellent activity against various single HIV-1 mutants (L100I, K103 N, E138K, Y181C) as well as one double mutant (F227L/V106A) with EC50 values in low-micromolar concentration ranges.
Abstract: Notably, 34 displayed outstanding potency against F227L/V106A (EC50 = 0.094 muM), and also showed exceptional activity against E138K (EC50 = 0.014 muM), L100I (EC50 = 0.011 muM) and K103 N (EC50 = 0.025 muM).
Switching to bictegravir/emtricitabine/tenofovir alafenamide maintained HIV-1 RNA suppression in participants with archived antiretroviral resistance including M184V/I.
PMID: 31430369
2019
The Journal of antimicrobial chemotherapy
Method: Primary NNRTI-R substitutions were L100I
Result: NNRTI-R substitutions were observed in 23% (124/543) of participants; the most frequently detected substitutions were K103N/S in 12% (64/543) and rilpivirine-associated resistance substitutions (L100I, K101E/P, E138A/G/K/Q/R, V179L, Y181C/I/V, Y188L, H221Y, F227C or M320I/L) in 10% (53/543) (Table 3).
Table: E138A/K
Table: E138K
Trends in HIV-1 Drug Resistance Mutations from a U.S. Reference Laboratory from 2006 to 2017.
PMID: 31169022
2019
AIDS research and human retroviruses
Abstract: Rilpivirine and etravirine DRMs E138A/Q/R and E138K increased from 4.9% and 0.4% to 9.7% and 1.7%, respectively.
HIV Drug Resistance Mutations in Patients with HIV and HIV-TB Coinfection After Failure of First-Line Therapy: A Prevalence Study in a Resource-Limited Setting.
PMID: 31117863
2019
Journal of the International Association of Providers of AIDS Care
HIV mutation literature information.
PMID: 
2019
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