Agonist-Dependent Plasticity in the TRPC3 Selectivity Filter

Transient receptor potential canonical 3 (TRPC3) forms non-selective cation channels that are opened in response to phospholipase C stimulation. This physiologic mode of activation involves a direct interaction of diacylglycerols with residues within a lateral fenestration of the pore domain behind the selectivity filter. Benzimidazols (GSK1702934A derivatives) activate TRPC3 by a mechanism bypassing the phospholipase cascade. We set out to...