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 HIV mutation literature information.


  Bicyclic 1-hydroxy-2-oxo-1,2-dihydropyridine-3-carboxamide-containing HIV-1 integrase inhibitors having high antiviral potency against cells harboring raltegravir-resistant integrase mutants.
 PMID: 24471816       2014       Journal of medicinal chemistry
Abstract: Importantly, some of these new inhibitors retain greater antiviral efficacy compared to that of RAL when tested against a panel of IN mutants that included Y143R, N155H, G140S/Q148H, G118R, and E138K/Q148K.
Method: The following sense with cognate antisense (not shown) oligonucleotides (Integrated DNA Technologies, Coralville, IA) was used in the mutagenesis: G118R, 5'-GTACATACAGACAATCGCAGCAATTTCACCAGTAC-3'; E138K, 5'-GGCGGGGATCAAGCAGAAATTTGGCATTCCCTA-3'; G140A, 5'-GGGGATCAAGCAGGAATTTGCCATTCCCTACAATC-3'; G140S, 5'-GGGGATCAAGCAGGAATTTAGCATTCCCTACAATC-3';


  Resistance mutations against dolutegravir in HIV integrase impair the emergence of resistance against reverse transcriptase inhibitors.
 PMID: 24463394       2014       AIDS (London, England)
Abstract: DESIGN AND METHODS: We tested the ability of DTG-resistant viruses containing either the R263K or G118R and/or H51Y mutations to develop further resistance against several reverse transcriptase inhibitors during in-vitro selection experiments.
Abstract: We have previously selected mutations at position R263K, G118R, H51Y, and E138K as being associated with low-level resistance to DTG.


  Development of a G118R mutation in HIV-1 integrase following a switch to dolutegravir monotherapy leading to cross-resistance to integrase inhibitors.
 PMID: 24080645       2013       Antimicrobial agents and chemotherapy
Abstract: Homology modeling provided insight into the mechanism of resistance conferred by G118R as well as the effects of H51Y or E138K on enzyme activity.
Abstract: Now, we have characterized the impact of the G118R substitution, alone or in combination with either H51Y or E138K, on 3' processing and integrase strand transfer activity.
Abstract: The addition of H51Y and E138K to G118R partially restored strand trans


  Viral fitness cost prevents HIV-1 from evading dolutegravir drug pressure.
 PMID: 23432922       2013       Retrovirology
Discussion: In vitro selection experiments with both DTG and another second-generation compound termed MK-2048 have identified several mutations within the integrase coding region, including G118R, S153Y, and R263K that confer low-level resistance to these drugs .


  HIV Drug Resistance and the Advent of Integrase Inhibitors.
 PMID: 23180144       2013       Current infectious disease reports
Abstract: Here, we provide new information about the most recent mutations identified and other mutations that confer resistance to several integrase inhibitors, such as new resistance mutations-for example, G118R, R263K, and S153Y-that have been identified through in vitro selection studies with second-generation integrase strand transfer inhibitors (INSTIs).


  The development of novel HIV integrase inhibitors and the problem of drug resistance.
 PMID: 22989757       2012       Current opinion in virology
Abstract: Several newly identified resistance mutations, such as G118R, R263K and S153Y, have been identified through tissue culture selection studies with second-generation integrase strand-transfer inhibitors (INSTIs).


  Resistance to HIV integrase inhibitors.
 PMID: 22789986       2012       Current opinion in HIV and AIDS
Abstract: RECENT FINDINGS: New resistance mutations, such as G118R, R263K and S153Y, have been recently identified through in-vitro selection studies with second-generation integrase strand-transfer inhibitors (INSTIs).


  Risk factors for raltegravir resistance development in clinical practice.
 PMID: 22763565       2012       The Journal of antimicrobial chemotherapy
Abstract: Among patients without main resistance mutations, two patients showed raltegravir phenotypic resistance, one naturally with F121Y at baseline and the other acquiring G118R at failure.


  Development of a G118R mutation in HIV-1 integrase following a switch to dolutegravir monotherapy leading to cross-resistance to integrase inhibitors.
 PMID: 21933786       2011       The Journal of antimicrobial chemotherapy
Abstract: For this patient, the phenotypic analysis showed that addition of only the G118R mutation conferred a high level of resistance to raltegravir (fold change = 25.5) and elvitegravir (fold change = 9.2).


  MK-0536 inhibits HIV-1 integrases resistant to raltegravir.
 PMID: 21876054       2011       Antimicrobial agents and chemotherapy
Abstract: It is also effective against INs that carry the three main RAL resistance mutations (Y143R, N155H, and to a lesser extent G140S-Q148H) and against the G118R mutant.



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