Tubeimoside I Antagonizes Yoda1-Evoked Piezo1 Channel Activation.

ABSTRACT: Piezo1, a mechanosensitive Ca²⁺-permeable non-selective cationic ion channel protein, is involved in a wide range of biological processes and plays crucial roles in vascular development. However, the pharmacology of this protein is in its infancy. Yoda1, the first specific chemical activator of Piezo1 channels, can activate Piezo1 in absence of mechanical stimulation. Hence, we sought to identify inhibitors of Yoda1 from Traditional Chinese Medicine (TCM). Intracellular Ca²⁺ measurements were conducted in human umbilical vein endothelial cells (HUVECs), HEK 293T cells overexpressing TRPC5 and TRPM2 channels, as well as in CHO K1 cells overexpressing TRPV4 channels. We identified tubeimoside I (TBMS1) as a strong inhibitor of the Yoda1 response and demonstrated its sel

SUBMITTER: Liu S 

PROVIDER: S-EPMC7261832 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature