literature

HIV mutation literature information.

Primary resistance to integrase strand transfer inhibitors in Spain using ultrasensitive HIV-1 genotyping.

PMID: 32929472 2020 The Journal of antimicrobial chemotherapy

Abstract: Only three (1.7%) subjects had INSTI TDR (R263K, E138K and G163R), while minority variants with integrase TDR were detected in 9.6% of subjects.

Review of Doravirine Resistance Patterns Identified in Participants During Clinical Development.

PMID: 32925358 2020 Journal of acquired immune deficiency syndromes (1999)

Introduction: Although RT E138K was observed as with the other subtypes, it was followed by RT K101E to yield the unique double substitution RT E138K/K101E instead of E138K/L100I.

Introduction: By contrast, under the same conditions, RT substitutions L100I and K103N were the major substitutions associated with EFV, and E138K and K101P substitutions were the 2 most common resistance pathways in selection studies with RPV.

Introduction: No viral breakthrough was observed with DOR

Accumulation of integrase strand transfer inhibitor resistance mutations confers high-level resistance to dolutegravir in non-B subtype HIV-1 strains from patients failing raltegravir in Uganda.

PMID: 32853364 2020 The Journal of antimicrobial chemotherapy

Abstract: Two patients, one with E138A/G140A/Q148R/G163R and one with E138K/G140A/S147G/Q148K, displayed the highest reported resistance to raltegravir, elvitegravir and even dolutegravir.

First case of Dolutegravir and Darunavir/r multi drug-resistant HIV-1 in Cameroon following exposure to Raltegravir: lessons and implications in the era of transition to Dolutegravir-based regimens.

PMID: 32843050 2020 Antimicrobial resistance and infection control

Conclusion: Another GRT, covering HIV-1 integrase (IN) region, performed on the sample plasma aliquot, revealed major RAMs, L74I, E138KQ, G140A, Q148R, and E157Q, to integrase strand transfer inhibitors (INSTI) including raltegravir, dolutegravir, bictegravir and elvitegravir.

Discussion: Specifically, previous exposure to RAL (a drug with a low-genetic barrier to resistance) in a context of poor adherence contributed to selecting mutations (E138KQ, G140A, Q148R) conferring cross-resistance to DTG.

Occurrence of the S230R integrase strand inhibitor mutation in a treatment-naive individual case report.

PMID: 32629687 2020 Medicine

Discussion: Common INSTI RAMS include R263K, Q148H/R/K, G118R, G140A/S/C, E138A/K/T, N155H, and Y143C/R.

Molecular dynamic simulations to investigate the structural impact of known drug resistance mutations on HIV-1C Integrase-Dolutegravir binding.

PMID: 32379830 2020 PloS one

Introduction: Genetic resistance pathways including primary mutations at codons Y143C/H/R, Q148H/K/R or N155H together with one or more additional associated secondary mutations at L74M, E92Q, T97A, E138E/A/K or G140S/A, has been reported to result in higher levels of resistance with RAL treatment.

Table: E138K

Discussion: Furthermore, Xue and team found that the cross-resistance mutation E138K/Q148K resulted in a reduction in the chelation ability of oxygen atoms in INSTIs to Mg2+ in the active site of the mutated intaso

Virologic failure after 48 weeks of raltegravir-based regimen in low HIV-1 incidence setting.

PMID: 32434393 2020 Antiviral chemistry & chemotherapy

Abstract: Primary mutations (Y143C, N155H, T66I, G118R, E138K) conferring high level resistance to raltegravir were detected in only three patients.

Result: Among patients with M184V mutation, two had mutations at position 138 of reverse transcriptase that is associated with low-level resistance to the NNRTI, rilpivirine, and three had major mutations (Y143C, N155H, T66I, G118R, E138K) conferring high level resistance to RAL (Table 2).

Table: E138K

Pretreatment resistance mutations and treatment outcomes in adults living with HIV-1: a cohort study in urban Malawi.

PMID: 32434561 2020 AIDS research and therapy

Table: E138K

Susceptibility to HIV-1 integrase strand transfer inhibitors (INSTIs) in highly treatment-experienced patients who failed an INSTI-based regimen.

PMID: 32450199 2020 International journal of antimicrobial agents

Abstract: The primary INSTI resistance substitutions E138A/K, G140S, Y143C/H/R, Q148H and N155H were detected in 14 of 22 samples and were associated with resistance to one or more INSTIs, with G140S+Q148H present in 11 of 22 samples.

Abstract: Two isolates contained L74M, E138K, G140S and Q148H, or L74M, T97A, S119T, E138K, G140S,

Exploring the hydrophobic channel of NNIBP leads to the discovery of novel piperidine-substituted thiophene[3,2-d]pyrimidine derivatives as potent HIV-1 NNRTIs.

PMID: 32528834 2020 Acta pharmaceutica Sinica. B

Abstract: Especially, compound 26 exhibited the most potent activity against wild-type and a panel of single mutations (L100I, K103N, Y181C, Y188L and E138K) with an EC50 ranging from 6.02 to 23.9 nmol/L, which were comparable to those of etravirine (ETR).

Result: All the compounds were further evaluated against a panel of clinically relevant NNRTIs-resistant single-mutant strains (L100I, K103N, Y181C, Y188L, E138K) and double-mutant strains F227L + V106A, RES056.

Result: Compound 26 demonstrated the most active potency towa

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