literature

HIV mutation literature information.

HIV Drug Resistance Mutations Detection by Next-Generation Sequencing during Antiretroviral Therapy Interruption in China.

PMID: 33668946 2021 Pathogens (Basel, Switzerland)

Result: The most common drug resistance mutation was K103N (13.2%), followed by V179D (6.3%) and E138AGK (3.5%).

Discussion: The minority mutations detected by NGS may have resulted from apolipoprotein B mRNA editing catalytic polypeptide (APOBEC)-mediated G-to-A hypermutation such as E138K, M184I and G190E in RT or spontaneous mutation during viral replication, or from PCR error, which was introduced by error-prone reverse transcriptase or PCR enzymes.

Low Frequency of Integrase Inhibitor Resistance Mutations Among Therapy-Naive HIV Patients in Southeast China.

PMID: 33679129 2021 Drug design, development and therapy

Abstract: INSTIs TDRM was rare, with only one primary integrase mutation E138K observed in one sample and one secondary mutation E157Q detected in another sample.

Conclusion: However, TDRM associated with INSTIs-treatment resistance, including E138K and E517Q were also detected in therapy- naive HIV patients in Southeast China.

Result: Only one major INSTIs-resistance mutation (E138K) was detected in one sample.

Integrase Strand Transfer Inhibitor Resistance in Integrase Strand Transfer Inhibitor-Naive Persons.

PMID: 33683148 2021 AIDS research and human retroviruses

Abstract: Two surveillance DRMs, E138K and R263K occurred in 0.15% and 0.10% of naive sequences, respectively.

HIV-1 Subtype C Drug Resistance Mutations in Heavily Treated Patients Failing Integrase Strand Transfer Inhibitor-Based Regimens in Botswana.

PMID: 33807382 2021 Viruses

Introduction: INSTI-naive highly treatme

Result: Amongst the individuals previously exposed to RAL ART (seven out of eleven), DRMs selected whilst failing their current DTG based regimens were E138K, G140A, Q148R; and N155H Figure 3.

Result: The four individuals failing DTG cART but with no documented prior exposure to RAL, their selected DRMs were E138K, G140A, Q148K, A128T; G118R, E138K; N155ND and T66A, G118R, E138EAKT Figure 3.

Chemical space exploration of novel naphthyl-carboxamide-diarylpyrimidine derivatives with potent anti-HIV-1 activity.

PMID: 33895602 2021 Bioorganic chemistry

Abstract: Compound a1 showed exceptionally inhibitory effects with an EC50 value of 3.7 nM against HIV-1 wt strain, and an EC50 of 11 nM targeting mutant E138K.

Abstract: They displayed up to single-digit nanomolar activity against wild-type (WT) and rilpivirine-associated resistant mutant E138K viruses, as well as potent inhibitory ability toward the RT enzyme.

Design, synthesis, and antiviral evaluation of novel piperidine-substituted arylpyrimidines as HIV-1 NNRTIs by exploring the hydrophobic channel of NNIBP.

PMID: 34536931 2021 Bioorganic chemistry

Abstract: In addition, most of the compounds displayed micromolar activity against K103N and E138K mutant strains, while FT1 (EC50(K103N) = 50 nM, EC50(E138K) = 0.19 microM) still has the most effective activity.

Phylogenetic and Drug-Resistance Analysis of HIV-1 Sequences From an Extensive Paediatric HIV-1 Outbreak in Larkana, Pakistan.

PMID: 34484134 2021 Frontiers in microbiology

Table: E138K

Structure-Based Design and Discovery of Pyridyl-Bearing Fused Bicyclic HIV-1 Inhibitors: Synthesis, Biological Characterization, and Molecular Modeling Studies.

PMID: 34496571 2021 Journal of medicinal chemistry

Abstract: Furthermore, molecular modeling studies elucidated the binding modes of compounds 6, 15, 21, and 30 in the binding pocket of WT, E138K, K103N, or Y181C HIV-1 RTs.

High-level resistance to bictegravir and cabotegravir in subtype A- and D-infected HIV-1 patients failing raltegravir with multiple resistance mutations.

PMID: 34453542 2021 The Journal of antimicrobial chemotherapy

Abstract: However, combinations of primary INSTI-resistance mutations such as E138A/G140A/G163R/Q148R or E138K/G140A/S147G/Q148K led to decreased susceptibility to both cabotegravir (fold change in EC50 values from 429 to 1000x) and bictegravir (60 to 100x), exhibiting a high degree of cross-resistance.

Dolutegravir-based dual maintenance regimens combined with lamivudine/emtricitabine or rilpivirine: risk of virological failure in a real-life setting.

PMID: 34651192 2021 The Journal of antimicrobial chemotherapy

Abstract: Among subjects receiving dolutegravir/rilpivirine, two genotypes harboured emerging RAMs at VF: E138K on NNRTI (n = 1); and E138K+K101E on NNRTI and N155H on INSTI (n = 1).

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