Daphnane Diterpenoids from Trigonostemon lii and Inhibition Activities Against HIV-1.
PMID: 32048186
2020
Natural products and bioprospecting
Introduction: More important, these compounds still displayed significant inhibitions against T20-resistant HIV-1 strains, pNL4-3gp41(36G)V38E, N42S and pNL4-3gp41(36G)V38A, N42T.
Result: It not only inhibited replication of HIV-1 laboratory strains (HIV-1IIIB), but also inhibited T20-resistant strains (pNL4-3gp41(36G)V38E,N42S and pNL4-3gp41(36G)V38A,N42T) that those compounds showed strong inhibitory activities against all T20-resistant strains with EC50 values about 10 ng/mL.
Result: Thus, the inhibition assay of microtiter syncytium formation of the two T20-resistant HIV-1 strains, pNL4-3gp41(36G)V38E,N42S and pNL4-3gp41(36G
Genetic analysis and natural polymorphisms in HIV-1 gp41 isolates from Maputo City, Mozambique.
PMID: 24188582
2014
AIDS research and human retroviruses
Abstract: The major polymorphisms in the HR1 were N42S, L54M, A67T, and V72I.
Characterization of Gp41 polymorphisms in the fusion peptide domain and T-20 (Enfuvirtide) resistance-associated regions in Korean HIV-1 isolates.
PMID: 24616600
2014
Journal of Korean medical science
Introduction: T-20 can restrict HIV-1 replication in an efficient manner, but several T-20 resistance mutations have been reported in HR1 as follows: G36D/S, I37V, V38A/M/E, Q39R, Q40H, N42S/T/D/E, N43D/K/S, L44M, L45M, G36S/L44M, G36S/V38M, V38A/N42D, V38A/N42T, V38E/N42S, N42T
Molecular dynamics studies of the inhibitor C34 binding to the wild-type and mutant HIV-1 gp41: inhibitory and drug resistant mechanism.
Introduction: Now, many mutations are identified, single mutations like G36D/S, V38A/M, Q40H, N42S/T/D/E, N43D/K/S, L44M and L45M have been generally showed to reduce the sensitivity of ENF.
Naturally occurring resistance mutations to HIV-1 entry inhibitors in subtypes B, C, and CRF31_BC.
Result: All the pre-treatment viral env clones from patient B carried the N42S polymorphism (Table S1).
Result: Early resistance mutations (G36D and N42S+N43D) conferred high level resistance (>100-fold) and persisted throughout treatment.
Discussion: Furthermore, the HR1-HR2 recombinant viruses from this patient were less susceptible to enfuvirtide than the HR1-HR2 recombinants from the other patients despite the N42S polymorphism, which has been associated with increased enfuvirtide susceptibility and a slightly improved virological outcome.
Genotypic analysis of the gp41 HR1 region from HIV-1 isolates from enfuvirtide-treated and untreated patients.
PMID: 21857318
2011
Journal of acquired immune deficiency syndromes (1999)
Abstract: Overall, 17% of all isolates showed the N42S polymorphism related to ENF hypersusceptibility.
High prevalence of primary Enfuvirtide (ENF) resistance-associated mutations in HIV-1-infected patients in Hong Kong.
Abstract: RESULTS: Mutations in a 10 amino acid motif, such as N42S and N42R, and those outside this motif, such as L33M, R46S, A50V, Q52H and L54M, were found in the 27 isolates.