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 HIV mutation literature information.


  The design of 8-hydroxyquinoline tetracyclic lactams as HIV-1 integrase strand transfer inhibitors.
 PMID: 27092410       2016       European journal of medicinal chemistry
Abstract: This manuscript describes a number of 8-hydroxyquinoline tetracyclic lactams with exceptional antiviral activity against HIV-1 and little loss of potency against the IN signature resistance mutations Q148K and G140S/Q148H.


  Effect on HIV-1 viral replication capacity of DTG-resistance mutations in NRTI/NNRTI resistant viruses.
 PMID: 27130466       2016       Retrovirology
Discussion: Most commonly, mutations at N155H and Q148H/R have been observed in combination with M184I/V or less often with K65R.


  Usefulness of Integrase resistance testing in proviral HIV-1 DNA in patients with Raltegravir prior failure.
 PMID: 27177767       2016       BMC infectious diseases
Discussion: Only the accumulation of Q148H/R/K, together with other secondary mutations broadens DTG activity.


  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.
 PMID: 27369381       2016       Nucleic acids research
Abstract: However, these structures give only a partial sense for the limited inhibition of the 3'-processing reaction by INSTIs and how INSTIs can be modified to overcome drug resistance, notably against the G140S-Q148H double mutation.
Abstract: In addition, the G140S-Q148H (SH) mutant integrase, which has a reduced 3'-processing activity, becomes more active and more resistant to inhibition of 3'-processing by RAL and DTG in the absence of the -1 and +
Discussion: Here, we performed biochemical experiments and molecular modeling with the WT and the double-mutant (G140S-Q148H [SH]) that causes significant resistance to RAL and EVG and to a lesser extent to DTG.


  Drug resistant integrase mutants cause aberrant HIV integrations.
 PMID: 27682062       2016       Retrovirology
Abstract: More importantly, we show that at least two of the three clinically relevant drug resistant integrase mutants we tested, N155H and G140S/Q148H, which reduce the enzymatic activity of integrase, can cause the same sorts of aberrant integrations, even in the absence of drugs.
Conclusion: At least two of the three clinically relevant drug resistant integrase mutants we tested, N155H and G140S/Q148H, which reduce the enzymatic activity of integrase, caused aberrant integrations, even in the absence of any added drug.
Introduction: Two of these mutants,


  Prevalence of Integrase Strand Transfer Inhibitors (INSTI) Resistance Mutations in Taiwan.
 PMID: 27779200       2016       Scientific reports
Abstract: Of 30 sequences (47.6%) with INSTI-resistant mutations from raltegravir-experienced patients, 17 harboured Q148H/K/R, 8 N155H, and 6 Y143C/R.
Abstract: Of these 12 sequences, 11 harboured Q148H/K/R, one Y143R, and none N155H.
Result: Among the INSTI-experienced patients, only one (1.6%) had Q148H/R/K along with two or three of G140A/C/S, L74I and E138A/K/T mutations and were predicted to have high-level resistance to dolutegravir.


  Therapy-Emergent Drug Resistance to Integrase Strand Transfer Inhibitors in HIV-1 Patients: A Subgroup Meta-Analysis of Clinical Trials.
 PMID: 27532886       2016       PloS one
Abstract: The ten major integrase mutations
Discussion: Secondary integrase mutations(G140S/G and T97T/A) usually appeared together with Q148H/R and Y143Y/H.
Discussion: The ten major integrase mutations(including N155H, Y143C/R, Q148H/R, Y143Y/H, L74L/M, E92Q, E138E/A, Y143C, Q148Q and Y143S) could reduce the sensitivity of RAL and EVG.


  Development of a phenotypic susceptibility assay for HIV-1 integrase inhibitors.
 PMID: 27737783       2016       Journal of virological methods
Abstract: Solely a Q148H+G140S variant presented reduced susceptibility to dolutegravir.


  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: Based on data from these patient-derived isolates, BIC had an improved resistance profile compared to DTG, EVG, and RAL (with mean fold changes of 2.8, 5.8, >106, and >100, respectively; P = 0.04 for BIC versus DTG) and, most notably, against highly INSTI-resistant isolates encoding multiple mutation combinations, such as E92Q/N155H or G140C/S plus Q148R/H/K with or without additional INSTI mutations (P = 0.037 for the 23 isolates with mutations at positions 140 and 148 and P = 0.031 for the 2 isolates with mutations at positions 92 and 155 for BIC versus DTG).
Figure: Primary INSTI resistance mutations are T66I/A/K, E92Q/G,


  HIV-1 integrase genotyping is reliable and reproducible for routine clinical detection of integrase resistance mutations even in patients with low-level viraemia.
 PMID: 25712318       2015       The Journal of antimicrobial chemotherapy
Abstract: At early genotyping (within 3 months of raltegravir treatment), Q148H/K/R and N155H mutations were detected regardless of the viraemia level, while Y143C/H/R was observed only in samples with viraemia >1000 copies/mL.
Abstract: At viraemia <=500 copies/mL, Q148H/K/R and N155H had the same prevalence (9.1%), while the Y143C/H/R was completely absent.



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