Figure 2.

(A) Schematic illustration of polyamide 1 binding to the VEGF HRE. (B) Uptake of polyamides 1–3 in HeLa cells. Polyamides 1 (left) and 2 (center) localize in the nucleus while polyamide 3 (right) localizes in the nucleus to a limited extent but is largely extracellular. (C) Induction of VEGF mRNA by the hypoxia mimetic deferoxamine (DFO) in the presence of polyamides 1–3 measured by quantitative real-time PCR. Polyamide 1 inhibits the expression of DFO-induced VEGF expression. Polyamides 2 and 3 have a more modest effect. (D) Chromatin immunoprecipitation assays using HeLa cells with anti-HIF1α or mock antibody treatment are consistent with inhibition of HIF-1 binding to the VEGF HRE in the presence of polyamide 1, and, to a more modest degree, 2. Concentrations of polyamides are 1 μM.