Prevalence of M184V and K65R in proviral DNA from PBMCs in HIV-infected youths with lamivudine/emtricitabine exposure.
PMID: 16989618
2006
AIDS research and human retroviruses
Abstract: In testing longitudinal plasma specimens from four SIV-infected macaques that received an active daily regimen of 30 mg/kg of tenofovir subcutaneously, the assay was able to detect K65R-positive viruses in all animals within 1-7 weeks after treatment began.
Abstract: To have this capability, we developed a real-time PCR-based assay for the detection of the SIV K65R reverse transcriptase mutation, a key marker for reduced susceptibility to tenofovir.
Abstract: We propose the SIV K65R real-time PCR assay provides improved sensitivity and simplicity in studying tenofovir resistance in macaque models.
Prevalence of M184V and K65R in proviral DNA from PBMCs in HIV-infected youths with lamivudine/emtricitabine exposure.
PMID: 17005757
2006
Journal of clinical microbiology
Abstract: We report a real-time PCR assay capable of detecting drug-resistant human immunodeficiency virus type 1 reverse transcriptase K65R mutant virus at a level of 0.5% in polymorphic patient plasma specimens.
Tenofovir disoproxil fumarate-emtricitabine coformulation for once-daily dual NRTI backbone.
PMID: 17009933
2006
Expert review of anti-infective therapy
Abstract: Resistance mutation K65R is selected for by tenofovir and confers a two- to fourfold reduced susceptibility to this drug.
Abstract: The incidence of K65R is low (3%) and has not been observed in clinical trials with the concomitant use of tenofovir and FTC.
Prevalence of M184V and K65R in proviral DNA from PBMCs in HIV-infected youths with lamivudine/emtricitabine exposure.
PMID: 17015626
2006
Antimicrobial agents and chemotherapy
Abstract: The K65R mutation was selected either alone or together with the Q151M, S68G, or F116Y substitution in viruses from seven such individuals.
Abstract: The results of in vitro passage experiments were consistent with an apparent increased propensity of subtype C viruses to develop the K65R substitution.
Indolopyridones inhibit human immunodeficiency virus reverse transcriptase with a novel mechanism of action.
Abstract: While INDOPY-1 susceptibility is unaffected by mutations associated with NNRTI or multidrug NRTI resistance, mutations M184V and Y115F are associated with decreased susceptibility, and mutation K65R confers hypersusceptibility to INDOPY-1.
Tenofovir disoproxil fumarate, emtricitabine, and efavirenz versus fixed-dose zidovudine/lamivudine and efavirenz in antiretroviral-naive patients: virologic, immunologic, and morphologic changes--a 96-week analysis.
PMID: 17057609
2006
Journal of acquired immune deficiency syndromes (1999)
Abstract: No patient developed the K65R mutation.
Virologic response of zidovudine, lamivudine, and tenofovir disoproxil fumarate combination in antiretroviral-naive HIV-1-infected patients.
PMID: 17057610
2006
Journal of acquired immune deficiency syndromes (1999)
Abstract: Six viral failures occurred, including 2 with K65R mutations (alone or associated with Y115F and M184V).
Differential impact of thymidine analogue mutations on emtricitabine and lamivudine susceptibility.
PMID: 17075395
2006
Journal of acquired immune deficiency syndromes (1999)
Abstract: For samples with K65R, L74I/V, or Q151M mutations, the phenotypic impact was similar, as the mean fold-change was not significantly different between drugs.
Rate of virologic failure and selection of drug resistance mutations using different triple nucleos(t)ide analogue combinations in HIV-infected patients.
PMID: 17209764
2006
AIDS research and human retroviruses
Abstract: M184V was the most frequent resistance mutation (75.4%), followed by T215Y (52.5%) and K65R (14.8%).
Abstract: Conversely, subjects who developed K65R did not accumulate TAMs.
Abstract: Of note, K65R did not develop in patients taking AZT nor in those with prior thymidine-associated mutations (TAMs).
Abstract: The presence of TAMs precluded the selection of K65R in patients treated with TDF.
Mechanistic insights into the suppression of drug resistance by human immunodeficiency virus type 1 reverse transcriptase using alpha-boranophosphate nucleoside analogs.
PMID: 15550379
2005
The Journal of biological chemistry
Abstract: Likewise, resistance to 3TCTP by M184V RT (30-fold) and K65R/M184V RT (180-fold) is suppressed using BH3-3TCTP because of a 160-fold acceleration of the catalytic constant kpol.
Abstract: We have shown previously that alpha-boranophosphate nucleoside analogs suppress RT-mediated resistance when the catalytic rate is responsible for drug resistance such as in the case of K65R and dideoxy (dd)NTPs, and Q151M toward AZTTP and ddNTPs.