Dooku1 is a Yoda1 analogue that antagonizes Yoda1-evoked activation of Piezo1 and aortic relaxation, lacks agonist activity.
Dooku1 inhibits 2 μM Yoda1-induced Ca2+ -entry with IC50 of 1.3 μM (HEK 293 cells) and 1.5 μM (HUVECs) yet failed to inhibit constitutive Piezo1 channel activity.
Dooku1 has no effect on endogenous ATP-evoked Ca2+ elevation or store-operated Ca2+ entry in HEK 293 cells or Ca2+ entry through TRPV4 or TRPC4 channels overexpressed in CHO and HEK 293 cells.
