Exploring the drug resistance of V32I and M46L mutant HIV-1 protease to inhibitor TMC114: flap dynamics and binding mechanism.
PMID: 25562662
2015
Journal of molecular graphics & modelling
Introduction: Our previous studies on binding Gibbs free energies for WT, I50V single mutant and I50L/A71V double mutant showed that I50V decreases the binding affinity for TMC114, while the double m
Result: The distance between the flap tips (Ile50Calpha and Ile50'Calpha) and the catalytic aspartates (Asp25Calpha and Asp25'Calpha) for WT-1T, V32I-1T and M46L-1T HIV-1-pr/TMC114 shows that the distances in chain-A for all the three complexes are almost overlapped throughout the simulation with an average distance of 13.89, 14.05 and 14.05 A, respectively, which are slightly shorter than those of double binding for the two mutants.
The Evolving Genotypic Profile of HIV-1 Mutations Related to Antiretroviral Treatment in the North Region of Brazil.
Result: The most prevalent major PI mutations were as follows: M46I (21%), V82A (17%), I54V (16.4%), L90M (13.5%), I50L (8.2%), I84V (5.8%), D30N 22 (5.8%), and M46L (5%) (Figure 1(c)).
HIV Drug Resistance Surveillance in Honduras after a Decade of Widespread Antiretroviral Therapy.
Result: In fact, I50L is associated with increased susceptibility to LPV, DRV and other PIs.
Discussion: I50L and N88S are the most commonly occurring major DRMs in PI-naive individuals receiving ATV/r.
Discussion: Our analysis suggests that the four mutations V82A, L76V, I84V, and I47A would have a sensitivity approaching 90% for detecting intermediate or high-level LPV resistance and that I50L and N88S are the most common major PI-associated DRMs to develop in individuals with VF and intermediate or high-level ATV resistance on an initial ATV/r-associated regimen.
A uniquely prevalent nonnucleoside reverse transcriptase inhibitor resistance mutation in Russian subtype A HIV-1 viruses.
Result: Of the 243 patients who received one or more protease inhibitors, 32 (13%) had a study-defined protease inhibitor-resistance mutation most commonly L10F, K20T, V32I, L33F, M46I/L, I47V/A, I50L, F53L, I54V/L, Q58E, L76V, V82A/C, I84V, L89V, and L90M.
Efficacy, tolerability and virological consequences of long-term use of unboosted atazanavir plus 2 NRTIs in HIV-infected patients.
Abstract: Ten patients with virological failure presented newly selected resistance associated mutations (RAMs) for NRTIs (2/10) or ATV (4/10, one I50L).
2014 Update of the drug resistance mutations in HIV-1.
Discussion: The presence of mutations L24I, I50L/V, F53Y/L/W, I54L, and L76V have been associated with improved virologic response to tipranavir in some studies.
Discussion: Their impacts differ, with I50L, I84V, and N88S having the greatest effect.
Natural polymorphisms and unusual mutations in HIV-1 protease with potential antiretroviral resistance: a bioinformatic analysis.
Result: We modelled the proteins with unusual mutations (L5F, D29V, L63G, L63R, P79L and T91V), natural polymorphisms (L63H andL63S), and drug-resistant mutant PRs with single mutations or patterns of mutations (D30N, V32I, M36I, M46I, I47V, G48V, I50V, I50L, I54M, Q58E, T74P,
Table: I50L
Enhanced stability of monomer fold correlates with extreme drug resistance of HIV-1 protease.
Introduction: These include ANAM-11, which bears 11 mutations including L63P, and mutant I50L/A71V showing Tm increases of 4.8 C and ~2 C, respectively, relative to wild type.
Increasing trends in primary NNRTI resistance among newly HIV-1-diagnosed individuals in Buenos Aires, Argentina.
PMID: 24093951
2013
Journal of the International AIDS Society
Method: Sequences were analyzed to identify mutations associated with reduced susceptibility to protease and RT inhibitors, as reported by the International AIDS Society-USA in 2010: RT-M41L, A62V, K65R, D67N, 69 insert, K70R, L74V,V75I, F77L, L100I, K101P, K103N, V106A, V106M, V108I, Y115F, F116Y,
HIV mutation literature information.
PMID: 
2015
Journal of molecular graphics & modelling
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