Teleocidin A2 inhibits human proteinase-activated receptor 2 signaling in tumor cells.

ABSTRACT: Enhanced expression of the proteinase-activated receptor 2 (PAR2) is linked to cell proliferation and migration in many cancer cell types. The role of PAR2 in cancer progression strongly illustrates the need for PAR2-inhibiting compounds. However, to date, potent and selective PAR2 antagonists have not been reported. The natural product teleocidin A2 was characterized against PAR2-activating peptide SLIGKV-NH ₂, and trypsin-induced PAR2-dependent intracellular Ca²⁺ mobilization in tumor and in primary endothelial or epithelial cells. Further biochemical and cell-based studies were conducted to evaluate teleocidin specificity. The antagonizing effect of teleocidin A2 was confirmed in PAR2-dependent cell migration and rearrangement of actin cytoskeleton of human breast

SUBMITTER: Stahn S 

PROVIDER: S-EPMC5242168 | biostudies-literature | 2016 Aug

REPOSITORIES: biostudies-literature