Figure 1

Inhibition of IN-LEDGF interaction, correlation with ARV activity and LEDGF competition for IN binding. (A) IN-CCD/LEDGF-IBD interaction inhibition dose–response curves of the compounds listed in Table 1. Data represent the means of six independent experiments with standard deviations shown as error bars. (B) Log-log correlation plot between IC₅₀ of CCD-IBD interaction inhibition and EC₅₀ of ARV activity for MT4 cells infected by HxB2 HIV-1. A subset of 51 Mut101 series compounds was studied (R² = 0.77). (C) IN-LEDGF/p75 interaction inhibition dose–response curves. Data represent the means of three independent experiments with standard deviations shown as error bars. (D) Log-log correlation plot between IC₅₀ of IN-LEDGF/p75 interaction inhibition and EC₅₀ of ARV activity as in (B) (R² = 0.88). (E) IN-LEDGF/p75 interaction inhibition dose–response curves for Mut101 at various LEDGF/p75 competing concentrations ranging from 7.5 nM to 480 nM. Data represent the means of two independent experiments done in quadruplicate with standard deviations shown as error bars. (F) Correlation plot between LEDGF/p75 concentration and IC₅₀ of Mut101 IN-LEDGF interaction (R² = 0.94).