Introduction: The latest International AIDS Society (IAS)-USA panel list shows 11 mutations associated with DRV resistance: V11I, V32I, L33F, I47V, I50V, I54M/L, T74P, L76V, I84V, and L89V (Wensing et al.,).
Computational Studies of a Mechanism for Binding and Drug Resistance in the Wild Type and Four Mutations of HIV-1 Protease with a GRL-0519 Inhibitor.
PMID: 27240358
2016
International journal of molecular sciences
Abstract: The stable hydrophobic core, including the side chain of Ile54 in the wild type (WT) complex, became unstable in I54M because the side chain of Met54 is flexible with two alternative conformations.
Abstract: To elucidate the molecular mechanism of drug resistance associated with mutations (D30N, I50V, I54M, and V82A) and inhibitor (GRL-0519) complexes, we have performed five molecular dynamics (MD) simulations and calculated the binding free energies using the molecular mechanics Poisson-Boltzmann surface area (MM-PBSA) method.
Introduction:
Introduction: In this work, we are interested in the drug resistance mechanics about D30N, I50V, I54M, and V82A mutations.
The L33F darunavir resistance mutation acts as a molecular anchor reducing the flexibility of the HIV-1 protease 30s and 80s loops.
PMID: 29124158
2015
Biochemistry and biophysics reports
Introduction: L33F was initially
Introduction: Clinical isolates previously obtained from the Wayne State University Infectious Disease Clinic in Detroit, MI contain major drug resistance mutations L33F, I47V, I50V, I54M, L76V, V82I/F, and I84F as well as nonpolymorphicaccessory mutations L10V/G, V11I, I13V, K20T/R, L33I/M, K43T, F53L, A71L, T74P, and L89V.
Effects of drug-resistant mutations on the dynamic properties of HIV-1 protease and inhibition by Amprenavir and Darunavir.
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.
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.
Result: The patient met VF criteria at week 24, at which time the major viral PI treatment-emergent mutations I50I/V, I54I/M, and V82F/I were detected.
Assessing transmissibility of HIV-1 drug resistance mutations from treated and from drug-naive individuals.
Discussion: We show here that D30N, N88D/S and L90 M also have high transmissibility and that other SDRMs have higher (M41L, T215Rev and K219E/N/Q/R for NRTIs and K101E/P for the NNRTIs) or lower transmissibility (K70E/R, L74I/V, and T215Y/F for NRTIs; Y181C/I/V for NNRTIs and I84 V and I54A/L/M/S/T/V for protease inhibit
HIV Drug Resistance Surveillance in Honduras after a Decade of Widespread Antiretroviral Therapy.
Introduction: The other mutations which were co-occurring with DBM and TPM included major mutations like- M46IL, I54MV, I84V, L90M, N88S, V32I, I47V, V82AS, D30N, G48V; and accompanied by minor mutations like- L10I, I13V, L63P, A71V, L89M, I93L, E35DN, I15V, D60E, L24I etc.
Inhibition Profiling of Retroviral Protease Inhibitors Using an HIV-2 Modular System.
Result: L90M exerts little or no effect on the susceptibility to tipranavir in HIV-1 isolates, while I54M was associated with a reduced susceptibility to the inhibitor.
Result: Further statistical analysis was also performed to complete the linear correlation analysis of data showing non-normal distribution, which revealed that there are no significant differences between the values determined by the different assays (p > 0.05) (wild-type: z = 1.35 and p = 0.22; I54M/L90M mutant: z = 0.51 and p = 0.69).
Result: Introduction of the double mutation I54M and L90M greatly decreased the efficacy of the inhibitors, with the exception of tipranavir, which remained indifferent to the mutations.
Result: The I54M-L90M
HIV-1 Drug Resistance Mutations: Potential Applications for Point-of-Care Genotypic Resistance Testing.
Result: The remaining 8% of viruses with predicted intermediate or high-level LPV resistance had a combination of two or more PI DRMs with lower mutation scores, including V32I, M46I, I54M/L/V, I47V, V82S/T/M and L90M.
HIV mutation literature information.
PMID: 
2016
Frontiers in microbiology
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