literature

HIV mutation literature information.

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.

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

Result: None of these pre-treatment integrase sequences contained primary integrase mutations most often associated with emergent EVG (T66I, E92Q, S147G, Q148R/H/K, and N155H) or RAL (Y143C/R/H, Q148H/K/R, and N155H) resistance.

Drug resistance mutations in HIV-2 patients failing raltegravir and influence on dolutegravir response.

PMID: 28369593 2017 The Journal of antimicrobial chemotherapy

Abstract: Although dolutegravir may allow successful rescue in most HIV-2 raltegravir failures, we report and characterize three cases of dolutegravir resistance in HIV-2 patients, emerging variants Q148K and Q148R and a novel change G118R.

Abstract: In two of them N155H was replaced by Q148K/R and in another by G118R.

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).

PMID: 28891788 2017 HIV clinical trials

Method: Primary INSTI-R substitutions assessed were T66A/I/K, E92G/Q, T97A, Y143C/H/R, S147G, Q148H/K/R, and N155H/S in IN.

Probing Resistance Mutations in Retroviral Integrases by Direct Measurement of Dolutegravir Fluorescence.

PMID: 29070877 2017 Scientific reports

Abstra

Introduction: Our findings define a new approach to study the binding properties of DTG to IN and reach deeper insight into the mechanisms of drug resistance mutations such as G187R, F190Y and S217K (equivalent to G118R, F121Y and G140S/Q148K mutations, respectively, in INHIV).

Result: DTG binding to analogous G187R and F190Y INPFV was then investigated using fluorescence-based DTG-binding assays and compared to results obtained with the S217K INPFV mutant (equivalent to the RAL/DTG resistant G140S/Q148K INHIV double mutant.

Molecular evolution of HIV-1 integrase during the 20 years prior to the first approval of integrase inhibitors.

PMID: 29137637 2017 Virology journal

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

The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors.

PMID: 27092410 2016 European journal of medicinal chemistry

Abstract: This manuscript describes a number of 8-hydroxyquinoline tetracyclic lactams with exceptional antiviral activity against HIV-1 and little loss of potency against the IN signature resistance mutations Q148K and G140S/Q148H.

Transmitted drug resistance of HIV-1 strains among individuals attending voluntary counselling and testing in Taiwan.

PMID: 26404079 2016 The Journal of antimicrobial chemotherapy

Abstract: Among the seven major integrase mutations (T66I, E92Q, G140S, Y143C/H/R, S147G, Q148H/K/R and N155H), only one strain harbouring the Q148R mutation was detected.

Q148N, a Novel Integrase Inhibitor Resistance Mutation Associated with Low-Level Reduction in Elvitegravir Susceptibility.

PMID: 27009474 2016 AIDS research and human retroviruses

Discussion: Q148N is also the only mutation other than Q148H/R/K that has been shown to have strand transfer activity in biochemical assays.

Discussion: Of 1,120 integrase sequences from patients receiving raltegravir in GenBank as of June 2015, 23%, 8%, and 1% had the previously characterized INSTI-resistance mutations Q148H, Q148R, and Q148K, respectively.

Discussion: The rarity of Q148N and its weaker association with INSTI resistance suggest that it may be a revertant mutation arising from single nucleotide substitutions in viruses that once harbored Q148H (CAC or CAT) or Q148K

Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile.

PMID: 27645238 2016 Antimicrobial agents and chemotherapy

Figure: Primary INSTI resistance mutations are T66I/A/K, E92Q/G, T97A, Y143C/H/R, S147G, Q148H/K/R, and N155H, and other INSTI resistance mutations are H51Y, L68I/V, V72A/N/T, L74M, Q95K/R, F121C/Y, A128T, E138A/K, G140A/C/S, P145S,

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