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Fig. 1 | Retrovirology

Fig. 1

From: Altered Env conformational dynamics as a mechanism of resistance to peptide-triazole HIV-1 inactivators

Fig. 1

Generating resistance to peptide triazole inhibitors of HIV-1 entry. A Structures of macrocyclic PT AAR029b and linear PT thiol KR13. The two PTs share the same pharmacophore, I-X-W, where X represents an azidoproline with a ferrocene group. B PT inhibitory titrations against replicating HIV-1NL4-3. Viruses were added to CEM-GFP cells in the presence or absence of inhibitor, and the viral content in each culture was measured six days later by p24 ELISA. Data represent the mean and standard deviation of three independent experiments. C Dose-escalation profiles of KR13 (red), AAR029b (black) and C37 (blue) used during virus passaging. Inhibitor concentration was initiated at half of the IC50 value and increased when the p24 levels in culture supernatant were comparable to the p24 levels of cultures propagated in the absence of inhibitor. The data are expressed as the ratio of inhibitor concentration in culture at a given week to the initial inhibitor concentration at week zero. C37 is a gp41-targeted fusion inhibitor with a well-defined escape profile for HIV-1NL4-3 and served as a positive control for these assays. Data represent mean and standard deviation from three independent cultures for each inhibitor

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