Figure 10.
Cartoon summary of 3NB and 3PP gating effects. 3NB acts as a pure catalyst for the C1↔O1 transition (blue arrow), thereby increasing channel opening rate and nonhydrolytic closing rate. 3PP acts to inhibit the ATP hydrolysis step (red line). Both effects independently stimulate Po for WT CFTR, but neither effect changes Po for a nonhydrolytic mutant. NPPB exerts both effects at the same time, resulting in extremely efficacious stimulation of Po for WT (and ΔF508) CFTR (Csanády and Töröcsik, 2014).