Introduction: In HIV-1-infected patients failing an INI-containing regimen, three distinct resistance pathways involving Y143R, Q148H/R/K or N155 H have been described.
Extended use of raltegravir in the treatment of HIV-1 infection: optimizing therapy.
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: Moreover, the characterization of the phenotypic evolution showed that a switch from N155H to Y143C/R was linked to an increase in resistance to raltegravir.
Discussion: Most of these shifts in raltegravir-resistance profiles
Dynamic patterns of human immunodeficiency virus type 1 integrase gene evolution in patients failing raltegravir-based salvage therapies.
Abstract: RESULTS: : Resistance to RAL appeared initially associated with selection of single variants (Y143R, Q148R N155H) in the majority of patients; however, in three patients, complex patterns of viral mutations were observed.
HIV-1 integrase polymorphisms are associated with prior antiretroviral drug exposure.
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were detected in the virus from one patient, and these reverted to wild type when treatment was withdrawn, although clonal analysis identified maintenance of RAL resistance minority species at this time point.
Effects of HIV type-1 immune selection on susceptability to integrase inhibitor resistance.
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 use of integrase inhibitors in treatment-experienced patients.
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.
HIV mutation literature information.
PMID: 
2010
Biochemistry
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