literature

HIV mutation literature information.

Biochemical and pharmacological analyses of HIV-1 integrase flexible loop mutants resistant to raltegravir.

PMID: 20334344 2010 Biochemistry

Abstract: Resistance to raltegravir (RAL), the first HIV-1 integrase (IN) inhibitor approved by the FDA, involves three genetic pathways: IN mutations N155H, Q148H/R/K, and Y143H/R/C.

Natural polymorphisms of integrase among HIV type 1-infected South African patients.

PMID: 20377427 2010 AIDS research and human retroviruses

Abstract: Amino acid sequence analysis revealed there were no primary mutations (Y143R/C/H, Q148H/R/K, and N155H/S) associated with reduced susceptibility to the integrase inhibitors raltegravir and elvitegravir.

HIV-1 resistance patterns to integrase inhibitors in antiretroviral-experienced patients with virological failure on raltegravir-containing regimens.

PMID: 20388636 2010 The Journal of antimicrobial chemotherapy

Abstract: Four different patterns of IN mutations were observed: (i) emergence of Q148H/R with secondary mutations (n=5 patients); (ii) emergence of N155H, then replaced by a pattern including Y143C/H/R (n=3); (iii) selection of S230N (n=1); and (iv) no evidence of selection of IN mutations (n=2).

Abstract: The median plasma raltegravir Cmin was lower in patients with selection of the N155H mutation followed by Y143C/H/R compared with patients with Q148H/R and with patients without emerging mutations or without VF.

Abstract: The median raltegravir and elvitegravir fold changes (FCs) were 244 (154-647) and 793 (339-892), respectively,

Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy.

PMID: 21694899 2010 Infection and drug resistance

Abstract: The development of resistance to raltegravir mainly involved three resistance mutations in integrase gene: Q148H/K/R, N155H, and Y143C/H/R.

Discussion: A recent crystal structure study enabled to describe the interactions between HIV-1 integrase residue Tyr 143 and the methyloxadiazole group of raltegravir, which could explain the role of the Y143C/H/R mutations in the development of resistance to raltegravir.

Discussion: Three major raltegravir resistance-associated mutations are characterized and frequently detected in vivo in case of virological failure on a raltegravir-containing regimen: Q148H/K/R, N155H, and

PMID: 19959414 2009 European journal of medical research

Abstract: Tolerance was remarkably good and virological failure was often associated with selection of integrase gene resistance mutations following the Y143C/H/R, Q148H/K/R o less frequently the NI55H paths.

Introduction: Overall, by week 96 resistance tests were available for 112 raltegravir treated patients of whom 73% had integrase mutations at one of the three positions (Y143C/H/R, Q148H/K/R N155H) almost always in combination with at least one other mutation.

Effects of HIV type-1 immune selection on susceptability to integrase inhibitor resistance.

PMID: 19918099 2009 Antiviral therapy

Result: Of the 38 major and minor integrase inhibitor resistance associated codons, 44, 61, 66, 92, 121, 140, 143, 147, 148, 155, 226 and 263 were the only positions absolutely conserved across all 342 sequences and these included six primary resistance-associated mutations for raltegravir and elvitegravir (T66I, E92Q, G140S, Y143C/H/R Q148H/R/K and N155S/H).

Discussion: In this population-based review of all sites associated with integrase inhibitor resistance in 342 natural isolates of HIV-1 obtained from two geographically distinct cohorts in Switzerland and Australia, we observed that the primary raltegravir and elvitegravir resistance mutations T66

The dynamics of appearance and disappearance of HIV-1 integrase mutations during and after withdrawal of raltegravir therapy.

PMID: 19571721 2009 AIDS (London, England)

Abstract: Mutations Q148R (2 months) followed by G140A/Q148R and then G140A/Y143CHR/Q148R/G163R were detected in the virus from one patient, and these reverted to wild type when treatment was withdrawn, although clonal analysis identified maintenance of RAL resistance minority species at this time point.

Characterization and structural analysis of HIV-1 integrase conservation.

PMID: 19290031 2009 AIDS reviews

Abstract: All primary signature mutations emerging in patients failing raltegravir (Y143R, Q148H/K/R, N155H) or elvitegravir (T66I, E92Q, S147G, Q148H/K/R, N155H), as well as secondary mutations (H51Y, T66A/K, E138K, G140S/A/C, Y143C/H, K160N, R166S, E170A, S230R, D232N, R263K) were complete

Natural variation of HIV-1 group M integrase: implications for a new class of antiretroviral inhibitors.

PMID: 18687142 2008 Retrovirology

Result: Y143H was present in three subtype C isolates and one subtype D isolate.

Result: Among the CCD mutations shown to directly reduce raltegravir or elvitegravir susceptibility - H51Y, T66I, E92Q, F121Y, G140S, Y143C/H/R, Q146P, S147G, Q148H/R/K, S153Y, N155H/S, and E157Q - only positions 153 and 157 are polymorphic (prevalence >= 0.5%) with S153A and E157Q each present in 1% of sequences (Figures 1).

Discussion: Nearly all

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