Q148N, a Novel Integrase Inhibitor Resistance Mutation Associated with Low-Level Reduction in Elvitegravir Susceptibility.
PMID: 27009474
2016
AIDS research and human retroviruses
Introduction: A baseline genotypic resistance test revealed the nucleoside reverse transcriptase inhibitor-resistance mutations L210W and T215D that were interpreted as causing intermediate resistance to zidovudine and low-level resistance to tenofovir; the non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistance mutations K101P and K103S that were interpreted as causing high-level resistance to each of the NNRTIs; and the protease inhibitor-resistance mutations D30N, L33F, I54V, N88D, and L90M
Binding of Clinical Inhibitors to a Model Precursor of a Rationally Selected Multidrug Resistant HIV-1 Protease Is Significantly Weaker Than That to the Released Mature Enzyme.
Result: I54L (in PR20) and I54V (in PRS17) are major mutations associated with high-level resistance to most PIs, with the possible exception of DRV (for I54V).
Result: Mutations in PRS17 associated with resistance to multiple drugs are M46L, G48V, I54V, V82S and L90M.
Result: Of these, I54V and L90M are major drug resistance mutations.
Result: Only five of the mutations in PR22 are identical with those in PRS17, namely, <
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
Method: The protease inhibitor (PI)-resistant mutant viruses encoding mutations in the HIV-1 protease-coding sequence, L10F/M46I/I50V, I84V/L90M, G48V/I54V/V82S, and G48V/V82A/L90M, were produced in electroporated SupT1 cells via homologous recombination.
Structural Studies of a Rationally Selected Multi-Drug Resistant HIV-1 Protease Reveal Synergistic Effect of Distal Mutations on Flap Dynamics.
Result: I54V mutation of PRS17/DRV retains van der Waals contacts with the 80's loop as observed in PR/DRV, but loses contacts with the side chain of Ile50' in subunit A.|mgd
Result: Conformational changes associated with mutation cluster of M46L, G48V and I54V are illustrated in Fig 4.
Result: Curling of flaps by mutations M46L, G48V and I54V.
Result: Despite the presence of a large number of mutations, PRS17 shares only one mutation (L90M) and a similar substitution (I54L vs I54V) with PR20.
Viral Suppression and Resistance in a Cohort of Perinatally-HIV Infected (PHIV+) Pregnant Women.
PMID: 27338425
2016
International journal of environmental research and public health
Abstract: The most frequent major mutations were K103N, M184V, T215, M41L, D67N at reverse transcriptase gene and M46, I54V and V82A at protease gene.
Result: The most frequent major mutations found among PHIV+ at enrollment were K103N (8/16, 50%) for NNRTIs; M184V (6/16, 38%), T215 (4/16, 25% ), M41L (3/16, 19%), and D67 (3/16, 19%) for NRTIs, and M46 (3/16, 19%), I54V (2/16, 13%) and V82A (2/16, 13%) for PIs.
From antiretroviral therapy access to provision of third line regimens: evidence of HIV Drug resistance mutations to first and second line regimens among Ugandan adults.
Abstract: Seven of the 36 patients on second line ART had major <
Conclusion: The observed PI resistance mutations (V82A, V82F, V82S, M46I, M46L and I54V) are clinically significant because they are associated with highest levels of phenotypic resistance and/or strongest evidence for interfering with successful PI therapy.
Result: The most common major PI-resistance mutations associated with the highest levels of phenotypic resistance were: V82A:7.0% and I54V, M46I, L33I (all 5.0%).
Table: I54V
HIV-1 subtype characteristics of infected persons living in southwestern Greece.
Result: The 22 cases experiencing virologic failure presented with the following DRMs: M46I, F53LY, I54LTV, G73ST, L76V, V82AT, I84V, I185V, N88D, and L90M for PIs; L100I, K103NS, V179F Y181C, G190AS, V106A, K103N, and P225H for NNRTIs; and
Genetic Changes in HIV-1 Gag-Protease Associated with Protease Inhibitor-Based Therapy Failure in Pediatric Patients.
PMID: 25919760
2015
AIDS research and human retroviruses
Abstract: Major protease resistance mutations (M46I, I54V, and V82A) were identified in eight (40%) patients, as well as Gag cleavage site (CS) mutations (at codons 373, 374, 378, 428, 431, 449, 451, and 453) in nine (45%) patients.
Treatment-Emergent Mutations and Resistance in HIV-Infected Children Treated with Fosamprenavir-Containing Antiretroviral Regimens.
Result: At VF, the following major treatment-emergent PI mutations or mutation mixtures were detected: M46M/I, I50I/V, I54I/M/V, and I84I/V, and the virus developed FPV RS.
Effects of drug-resistant mutations on the dynamic properties of HIV-1 protease and inhibition by Amprenavir and Darunavir.
Abstract: Molecular dynamics simulations are performed to investigate the dynamic properties of wild-type HIV-1 protease and its two multi-drug-resistant variants (Flap + (L10I/G48V/I54V/V82A) and Act (V82T/I84V)) as well as
Discussion: The crystal structure comparison of flap variants (I50V, I54V, and I54M) bound with SQV and variants (G48V, I54V, and I54M) bound with DRV suggested that the change in polar interactions between protease and inhibitors have the best correlation with observed resistance mutations.
HIV mutation literature information.
PMID: 
2016
AIDS research and human retroviruses
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