literature

HIV mutation literature information.

Etravirine combined with antiretrovirals other than darunavir/ritonavir for HIV-1-infected, treatment-experienced adults: Week 48 results of a phase IV trial.

PMID: 28382208 2017 SAGE open medicine

Result: Other etravirine RAMs that each emerged in <5 VFs were V90I, E138G, E138K, and E138Q.

Discovery of uracil-bearing DAPYs derivatives as novel HIV-1 NNRTIs via crystallographic overlay-based molecular hybridization.

PMID: 28254696 2017 European journal of medicinal chemistry

Abstract: Activity against the clinic prevalent mutant strains was also tested, suggesting that 16d was sensitive to E138K (EC50 = 34.2 nM).

Recent trends and patterns in HIV-1 transmitted drug resistance in the United Kingdom.

PMID: 27476929 2017 HIV medicine

Method: In this report, the term 'transmitted drug resistance mutations' (TDRMs) is used to describe (a) for pol, the presence of one or more mutations from the World Health Organisation (WHO) 2009 surveillance list 19 with the addition of E138K, a mutation known to cause resistance to the second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) rilpivirine, and all changes at codon T215 as they are likely to be ancestrally related to T215F or Y mutations 20; (b) for integrase, the presence of mutations from the IAS-USA 2013 list or accessory mutations reported by the Stanford HIVdb algorithm v7.0 (HIV Drug Resistance Database, Stanford University, Stanford, CA).

Prevalence of integrase inhibitor resistance mutations in Austrian patients recently diagnosed with HIV from 2008 to 2013.

PMID: 27530391 2017 Infection

Abstract: Two patients carried the accessory mutations E138K and G140A, respectively, where both lie on the Q148 pathway.

Lack of impact of pre-existing T97A HIV-1 integrase mutation on integrase strand transfer inhibitor resistance and treatment outcome.

PMID: 28212411 2017 PloS one

Method: Primary INSTI RAMs against EVG and/or RAL were based on IAS-USA Guidelines of RAMs with some modifications to remove secondary INSTI RAMs (i.e., L74M, F121Y, E138A/K, and G140A/S) (Fig 1).

HIV-1 drug-resistant mutations and related risk factors among HIV-1-positive individuals experiencing treatment failure in Hebei Province, China.

PMID: 28114955 2017 AIDS research and therapy

Table: E138K

Performance of Celera RUO integrase resistance assay across multiple HIV-1 subtypes.

PMID: 27993614 2017 Journal of virological methods

Abstract: Mutations associated with integrase resistance were observed in seven of the 106 (7%) clinical samples [one sample: Q148K; E138K; G140A; two samples: T97A and four samples: L74I].

Result: The following mutations were observed: Q148K; E138K; G140A in one sample; T97A in two samples; and L74I in four samples.

Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement.

PMID: 27750153 2017 European journal of medicinal chemistry

Abstract: Especially, 8 displayed outstanding potency against L100I (EC50 = 17 nM with a 2.8-fold resistance ratio) and 18 was relatively more potent to E138K mutant (EC50 = 43 nM with a 4.7-fold resistance ratio).

Abstract: Furthermore, most compounds maintained high activity agaist various single HIV-1 mutants (L100I, K103N, E138K, Y181C) as well as one double mutant (F227L/V106A) with EC50 values in low-micromolar to double-digit nanomolar concentration ranges.

HIV Drug Resistance in Antiretroviral Treatment-Naive Individuals in the Largest Public Hospital in Nicaragua, 2011-2015.

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.

Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus.

PMID: 27070547 2016 Journal of medicinal chemistry

Abstract: Compounds 6a, 14c, and 14d showed high potency against the 1b-resistant E138K mutated viral strain as well as good balance between anti-HIV-1 activity and desirable druglike properties.

Abstract: From the perspective of optimizing future NNRTI compounds as clinical trial candidates, computational modeling results provided valuable information about how the R(1) group might provide greater efficacy against the E138K mutant.

Abstract: Three series (6, 13, and 14) of new diarylaniline (DAAN) analogues were designed, synthesized, and evaluated for anti-HIV potency, especially against the E138K viral strain with a major mutation conferring resistance to the new-generation non-nucleoside reverse transcriptase inhibitor drug rilpivirine (1b).

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