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 HIV mutation literature information.


  Molecular dynamics approaches estimate the binding energy of HIV-1 integrase inhibitors and correlate with in vitro activity.
 PMID: 22037850       2012       Antimicrobial agents and chemotherapy
Abstract: Four well-characterized compounds (raltegravir, elvitegravir, MK-0536, and dolutegravir) were used as a training set, and the data for their in vitro activity against the Y143R, N155H, and G140S/Q148H mutants were used in addition to the wild-type (WT) IN data.


  Bicyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors.
 PMID: 22107736       2012       Chemical biology & drug design
Abstract: A representative inhibitor (5e) retained most of its inhibitory potency against the three major raltegravir-resistant IN mutant enzymes, G140S/Q148H, Y143R, and N155H.
Abstract: In antiviral assays employing viral vectors coding these IN mutants, compound 5e was approximately 200- and 20-fold less affected than raltegravir against the G140S/Q148H and Y143R mutations, respectively.
Abstract: Thus, our new compounds represent a novel structural class that may be further developed to overcome resistance to raltegravir, particularly in the case of the G140S/Q148H mutations.


  Genetic barrier to the development of resistance to integrase inhibitors in HIV-1 subtypes CRF01_AE and B.
 PMID: 22456540       2012       Intervirology
Abstract: At six codon positions with different genetic barriers, six mutations (V72I, L101I, A124T, T125K, and G140C/S) displayed a higher genetic barrier and one mutation (V201I) showed a lower genetic barrier in subtype CRF01_AE than subtype B.
Abstract: Nevertheless, different genetic barriers were observed in two mutations described to be associated with DTG resistance (L101I, A124T) and other five RAL and EVG secondary mutations (V72I, T125K, G140C/S, V201I), which could have an impact on the development of resistance to RAL, EVG, and DTG.


  Prevalence of HIV-1 integrase mutations related to resistance to dolutegravir in raltegravir naive and pretreated patients.
 PMID: 22716970       2012       Clinical microbiology and infection
Abstract: RTG-selected double and triple mutants, mostly the G140S/Q148H variant, were detected in only 32 (26.7%) RTG-treated patients.


  The activity of the integrase inhibitor dolutegravir against HIV-1 variants isolated from raltegravir-treated adults.
 PMID: 22878423       2012       Journal of acquired immune deficiency syndromes (1999)
Abstract: The median fold change to dolutegravir for isolates containing changes at G140S + Q148H, G140S + Q148R, T97A + Y143R, and N155H (thus including raltegravir signature resistance codons) were 3.75, 13.3, 1.05, and 1.37, respectively.


  Three main mutational pathways in HIV-2 lead to high-level raltegravir and elvitegravir resistance: implications for emerging HIV-2 treatment regimens.
 PMID: 23028968       2012       PloS one
Abstract: Collectively, our data define three major mutational pathways to high-level raltegravir and elvitegravir resistance: i) E92Q+Y143C or T97A+Y143C, ii) G140S+Q148R, and iii) E92Q+N155H.
Result: Collectively, these data show that raltegravir-resistant mutants of HIV-2 are cross-resistant to elvitegravir and that substitutions T97A+143C, Q148K/R, G140S+Q148R and E92Q+N155H confer high-level elvitegravir resistance in HIV-2.
Result: Dose-response profiles for variants


  "Prolonged and substantial discordance in prevalence of raltegravir-resistant HIV-1 in plasma versus PBMC samples revealed by 454 ""deep"" sequencing."
 PMID: 23049972       2012       PloS one
Result: For example, in Subject 3180 on day 177 post-therapy, 77% of the plasma virus shared identical sequences and contained the G140S/Q148H mutations (Figure 2A, day 177 white shading), but the same sequence could only be found in 1% of the counterpart PBMC population.
Result: In contrast, prevalence of plasma DRMs increased rapidly to 69% (Q148H and G140S) 54 days post-therapy.
Result: Note, however, that in subject 3180, the prevalence of Q148H and


  Monitoring the emergence of resistance mutations in patients infected with HIV-1 under salvage therapy with raltegravir in Rio de Janeiro, Brazil: a follow-up study.
 PMID: 23080489       2012       Journal of medical virology
Abstract: The mutations Q148H + G140S were observed for two patients and for the third patient only mutations to PR/RT inhibitors were detected.


  HIV-1 integrase resistance among antiretroviral treatment naive and experienced patients from Northwestern Poland.
 PMID: 23259737       2012       BMC infectious diseases
Abstract: Among 12 (26.1%) raltegravir treated patients treatment failure was observed; major InI drug resistance mutations (G140S, Q148H and N155H, V151I, E92EQ, V151I, G163R) were noted in four of these cases (8.3% of the total InI-treated patients).
Result: Development of drug resistance mutations followed two patterns: major N155H with or without subsequent accessory V151I, E92EQ, V151I, G163R mutants (three cases) and Q148H accompanied by  PMID: 20946407       2011       Clinical microbiology and infection
Abstract: Major mutation sites in the integrase (E92Q, F121Y, G140A/S, Y143C/R, Q148H/R/K and N155H) were not detected, and only a few minor mutation sites (L74M, V151I, E157Q, V165I, I203M, S230N and D232N) were identified in 21 strains (28%).



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