Figure 2.
Biological evaluation of HPMA-based heterobifunctional inhibitors of Stx1. Panel A: inhibition of Stx1 binding to Gb3 analog-coated microtiter plates; Panel B: inhibition of intoxication of Vero cells with Stx1 (LD100 25 ng/mL); Panel C: protection of from intoxication with Stx1 at LD100. Survival plot demonstrating the efficacy of HPMA-n2 compared with the original PolyBAIT in preventing Stx1-mediated lethality in human SAP-transgenic mice. Mice received a single anterior dorsal injection of a lethal dose of Stx1 (LD100 20 ng/g of body weight) that was premixed with a heterobifunctional inhibitor.