Agreement between an in‐house replication competent and a reference replication defective recombinant virus assay for measuring phenotypic resistance to <scp>HIV</scp>‐1 protease, reverse transcriptase, and integrase inhibitors

Saladini, Francesco; Giannini, Alessia; Boccuto, Adele; Vicenti, Ilaria; Zazzi, Maurizio

doi:10.1002/jcla.22206

Cited by 22 publications

(25 citation statements)

References 26 publications

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“…The interassay coefficient of variation (CV) of our HIV-1 inhibition assay, as determined for HIV Ba-L infectivity in DMEM-50, is 17%. This value is in a range similar to that previously reported for HIV-1 assays in TZM-bl cells ( 65 ).…”

Section: Methodssupporting

confidence: 89%

Anti-HIV-1 Activity of Lactic Acid in Human Cervicovaginal Fluid

Tyssen

Wang

Hayward

et al. 2018

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The Lactobacillus-dominated vaginal microbiota is associated with a reduced risk of acquiring and transmitting HIV and other sexually transmitted infections (STIs). Lactic acid is a major organic acid metabolite produced by lactobacilli that acidifies the vagina and has been reported to have inhibitory activity in vitro against bacterial, protozoan, and viral STIs, including HIV infections. However, the anti-HIV properties of lactic acid in native vaginal lumen fluids of women colonized with Lactobacillus spp. have not yet been established. Our study, using native cervicovaginal fluid from women, found that potent and irreversible anti-HIV-1 activity is significantly associated with the concentration of the protonated (acidic, uncharged) form of lactic acid. This work advances our understanding of the mechanisms by which vaginal microbiota modulate HIV susceptibility and could lead to novel strategies to prevent women from acquiring HIV or transmitting the virus during vaginal intercourse and vaginal birth.

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Section: Methodssupporting

confidence: 89%

Anti-HIV-1 Activity of Lactic Acid in Human Cervicovaginal Fluid

Tyssen

Wang

Hayward

et al. 2018

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“…Two complementary assays were employed to assess the effects of ligands during a single or two cycles of cell infection (i.e., Monocycle and BiCycle assay, respectively) [44]. In the former, TZM-bl cells were seeded in a 96-well plate at a concentration of 30,000/well.…”

Section: Evaluation Of Antiviral Activitymentioning

confidence: 99%

Identification of novel 2-benzoxazolinone derivatives with specific inhibitory activity against the HIV-1 nucleocapsid protein

Gamba

Mori

Kovalenko

et al. 2018

European Journal of Medicinal Chemistry

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In this report, we present a new benzoxazole derivative endowed with inhibitory activity against the HIV-1 nucleocapsid protein (NC). NC is a 55-residue basic protein with nucleic acid chaperone properties, which has emerged as a novel and potential pharmacological target against HIV-1. In the pursuit of novel NC-inhibitor chemotypes, we performed virtual screening and in vitro biological evaluation of a large library of chemical entities. We found that compounds sharing a benzoxazolinone moiety displayed putative inhibitory properties, which we further investigated by considering a series of chemical analogues. This approach provided valuable information on the structure-activity relationships of these compounds and, in the process, demonstrated that their anti-NC activity could be finely tuned by the addition of specific substituents to the initial benzoxazolinone scaffold. This study represents the starting point for the possible development of a new class of antiretroviral agents targeting the HIV-1 NC protein.

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“…Susceptibility to DTG, BIC, and CAB was assessed through a TZM-bl cell line-based phenotypic assay, shown to correlate well with the de facto reference PhenoSense assay by Monogram Biosciences and expressed as fold change (FC) with respect to the reference wild type NL4-3 virus (2). Differences in FC values among groups were tested by Friedman's ANOVA, and multiple comparisons were performed by the Dunn's test when appropriate.…”

mentioning

confidence: 99%

Comparable In Vitro Activities of Second-Generation HIV-1 Integrase Strand Transfer Inhibitors (INSTIs) on HIV-1 Clinical Isolates with INSTI Resistance Mutations

Saladini

Giannini

Boccuto

et al. 2019

Antimicrob Agents Chemother

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Second-generation HIV-1 integrase strand transfer inhibitors (INSTIs) dolutegravir (DTG), bictegravir (BIC), and cabotegravir (CAB) showed a high genetic barrier to resistance and limited cross-resistance with first-generation INSTIs raltegravir (RAL) and elvitegravir (EVG). In this study, DTG, BIC, and CAB demonstrated a comparable activity on a panel of INSTI-resistant strains isolated from patients exposed to RAL, EVG, and/or DTG, with a significantly reduced susceptibility only with the pathway Q148H/K/R plus one to two additional INSTI mutations.

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Agreement between an in‐house replication competent and a reference replication defective recombinant virus assay for measuring phenotypic resistance to HIV‐1 protease, reverse transcriptase, and integrase inhibitors

Abstract: The described phenotypic assay can be adopted to evaluate the antiviral activity of licensed and investigational HIV-1 drugs targeting any of the three HIV-1 enzymes.

Cited by 22 publications

References 26 publications

Anti-HIV-1 Activity of Lactic Acid in Human Cervicovaginal Fluid

Anti-HIV-1 Activity of Lactic Acid in Human Cervicovaginal Fluid

Identification of novel 2-benzoxazolinone derivatives with specific inhibitory activity against the HIV-1 nucleocapsid protein

Comparable In Vitro Activities of Second-Generation HIV-1 Integrase Strand Transfer Inhibitors (INSTIs) on HIV-1 Clinical Isolates with INSTI Resistance Mutations

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