Accurate ensemble molecular dynamics binding free energy ranking of multidrug-resistant HIV-1 proteases.
PMID: 20384328
2010
Journal of chemical information and modeling
Abstract: Multidrug resistance to lopinavir is enthalpically driven and increases through a decrease in the protein-ligand van der Waals interaction, principally due to the V82A/I84V mutation, and an increase in net electrostatic repulsion due to water-mediated disruption of protein-ligand interactions in the catalytic region.
Novel protease inhibitors (PIs) containing macrocyclic components and 3(R),3a(S),6a(R)-bis-tetrahydrofuranylurethane that are potent against multi-PI-resistant HIV-1 variants in vitro.
PMID: 20439612
2010
Antimicrobial agents and chemotherapy
Abstract: At passage 50 with GRL-216 (the HIV isolate selected with GRL-216 at up to 0.16 microM [HIV216-0.16 microM]), HIV-1NL4-3 containing the L10I, L24I, M46L, V82I, and I84V mutations remained relatively sensitive to PIs, including darunavir, with the EC50s being 3- to 8-fold-greater than the EC50 of each drug for HIV-1NL4-3.
Discordant genotypic interpretation and phenotypic role of protease mutations in HIV-1 subtypes B and G.
PMID: 19136678
2009
The Journal of antimicrobial chemotherapy
Abstract: Indinavir-associated mutations M46I/L, I84V and V82A/F/T developed earlier in subtype B across the time of exposure to that drug when compared with subtype G counterparts.
GRL-02031, a novel nonpeptidic protease inhibitor (PI) containing a stereochemically defined fused cyclopentanyltetrahydrofuran potent against multi-PI-resistant human immunodeficiency virus type 1 in vitro.
PMID: 18955518
2009
Antimicrobial agents and chemotherapy
Abstract: GRL-02031 was potent against a variety of HIV-1(NL4-3)-based molecular infectious clones containing a single primary mutation reported previously or a combination of such mutations, although it was slightly less active against HIV-1 variants containing consecutive amino acid substitutions: M46I and I47V or I84V and I85V.
Abstract: Upon selection of HIV-1(NL4-3) in the presence of GRL-02031, mutants carrying L10F, L33F, M46I, I47V, Q58E, V82I, I84V, and I85V in the protease-encoding region and G62R (withi
Gag mutations strongly contribute to HIV-1 resistance to protease inhibitors in highly drug-experienced patients besides compensating for fitness loss.
Introduction: It is, however, seen with significantly higher frequency in resistant viruses carrying the I84V mutation in PR and also specifically seen in resistant viruses carrying the I50V PR mutation, in association with L449F.
Introduction: Mutation L449F is frequently seen in viruses with mutation I84V in PR.
Proteochemometric modeling of drug resistance over the mutational space for multiple HIV protease variants and multiple protease inhibitors.
PMID: 19391634
2009
Journal of chemical information and modeling
Abstract: The model revealed the most deleterious mutations in the protease to be D30N, V32I, G48V, I50V, I54V, V82A, I84V, and L90M.
Darunavir: a review of its use in the management of HIV infection in adults.
Abstract: In a 24-week analysis of pooled data from the POWER 1 and 2 studies in treatment-experienced patients, 11 protease mutations associated with a reduced response to boosted darunavir were identified (V11I, V32I, L33F, I47V, I50V, I54L/M, G73S, L76V, I84V and L89V).
Minority variants associated with transmitted and acquired HIV-1 nonnucleoside reverse transcriptase inhibitor resistance: implications for the use of second-generation nonnucleoside reverse transcriptase inhibitors.
PMID: 19734799
2009
Journal of acquired immune deficiency syndromes (1999)
Result: The sample from PID 30062 - which contained four NRTI-resistance mutations - also had the following minority protease inhibitor (PI) resistance mutations: M46I (0.8%), I84V (0.9%), and L90M (0.9%) (data not shown).
Mutations associated with virological response to darunavir/ritonavir in HIV-1-infected protease inhibitor-experienced patients.
PMID: 19147519
2009
The Journal of antimicrobial chemotherapy
Abstract: CONCLUSIONS: Among the eight mutations with a negative impact on the virological response, I47V, I54M, T74P and I84V were previously described as darunavir resistance-associated mutations.
Abstract: Cochran-Armitage procedure identified eight mutations with a negative impact on the virological response, namely K14R, K20I, E34Q, I47V, I54M, K55R, T74P and I84V; and two mutations (E35D and V82A) with a positive impact.
Emergence of multiclass drug-resistance in HIV-2 in antiretroviral-treated individuals in Senegal: implications for HIV-2 treatment in resouce-limited West Africa.
Result: The contribution of individual HIV-2 PR mutations that confer phenotypic resistance to PIs have not been delineated; however, the emergence of mutations (K7R, G17N, K45R, M46I, V47A, I54M, V62A, I64V, V71I, I82F/L, I84V, L90M, and L99F) in PR in HIV-2 from individuals receiving PI-based therapy have been observed in previous studies.
HIV mutation literature information.
PMID: 
2010
Journal of chemical information and modeling
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