Transmitted drug resistance of HIV-1 strains among individuals attending voluntary counselling and testing in Taiwan.
PMID: 26404079
2016
The Journal of antimicrobial chemotherapy
Abstract: Among the seven major integrase mutations (T66I, E92Q, G140S, Y143C/H/R, S147G, Q148H/K/R and N155H), only one strain harbouring the Q148R mutation was detected.
Integrase Strand Transfer Inhibitors (INSTIs) Resistance Mutations in HIV-1 Infected Turkish Patients.
Abstract: However, ARV-experienced patients had major resistance mutations associated with raltegravir and elvitegravir; the following results were generated:F121Y, Y143R, Q148R and E157Q (6/91 - 6.6%).
Effect on HIV-1 viral replication capacity of DTG-resistance mutations in NRTI/NNRTI resistant viruses.
Introduction: The absence of compensatory secondary mutations for R263K is also consistent with the observation that many major RAL- and EVG-resistance substitutions such as G140S, Q148R, E92Q, N155H and Y143R are incompatible with the simultaneous presence of R263K in terms of both integrase strand-transfer activity and viral replication capacity.
Selectivity for strand-transfer over 3'-processing and susceptibility to clinical resistance of HIV-1 integrase inhibitors are driven by key enzyme-DNA interactions in the active site.
Introduction: In a previous study, we compared EVG to RAL and showed that EVG retains potency against the RAL-specific mutant Y143R.
Introduction: Using recombinant enzymes and oligonucleotides mimicking the ends of the retroviral DNA, IN mutants have been extensively characterized and RAL resistance can be recapitulated with three primary mutants: Y143R, N155H and G140S-Q148H (SH).
Introduction: While DTG effectively inhibits the Y143R and N155H mutants, the SH double mutant still reduces DTG potency by about 5- to 6-fold.
Result: No correlation was found for the Y143R mutant (Supplementary Figure S4).
Result: The lack of correlation for the
Development of a phenotypic susceptibility assay for HIV-1 integrase inhibitors.
PMID: 27737783
2016
Journal of virological methods
Abstract: While raltegravir resistance profiles presented a high cross-resistance to elvitegravir, dolutegravir maintained in-vitro activity in spite of the Y143R and N155H mutations, confirming the strong activity of dolutegravir against raltegravir-resistant viruses.
Prevalence of Integrase Strand Transfer Inhibitors (INSTI) Resistance Mutations in Taiwan.
Abstract: Of these 12 sequences, 11 harboured Q148H/K/R, one Y143R, and none N155H.
Introduction: With one or two major mutations, such as Q148HKR +- G140SA, N155H +- E92Q or Y143CR +- T97A, a marked reduction of viral susceptibility to raltegravir and elvitegravir has been observed.
Method: The major INSTI mutations, which have been determined having a marked reduction of viral susceptibility to raltegravir and elvitegravir, include Y143C/H/R, Q148H/K/R, and N155H.|m
Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile.
PMID: 27645238
2016
Antimicrobial agents and chemotherapy
Result: The set of tested mutations included E92Q, Y143R, Q148R, N155H, R263K, E138K/Q148K, G140S/Q148R, E92Q/N155H, and Q148R/N155H.
Discussion: The Y143R single mutant in our panel has no effect on susceptibility to BIC or DTG and is mildly resistant to EVG but has a higher resistance to RAL.
Discussion: While Y143R, Q148R, and N155H are primary RAL-associated mutations,
Therapy-Emergent Drug Resistance to Integrase Strand Transfer Inhibitors in HIV-1 Patients: A Subgroup Meta-Analysis of Clinical Trials.
Result: In the VIKING-3 trial, dolutegravir response rates (<50 HIV-1 RNA copies/ml at week 24) declined from 79% (n = 100/126) for patients without Q148 mutations at baseline (including those with N155H, Y143C/H/R, T66A, E92Q, or historical evidence of INSTI resistance), to 58% (21/36) for patients with Q148 plus one additional secondary mutation, to 24% (5/21) for those with Q148 plus two or more secondary mutations.
Resistance against Integrase Strand Transfer Inhibitors and Relevance to HIV Persistence.
Introduction: Resistance mutations that were found in viral isolates from treatment-naive participants who experienced treatment failure during the initial dose-ranging Protocol 004 clinical trial were: L74L/M, V151I, N155H, Y143R and S230R in integrase (IN) and M184M/I/V and K65K/R in RT (Table 1).
HIV mutation literature information.
PMID: 
2016
The Journal of antimicrobial chemotherapy
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