[HTML][HTML] Mechanisms of desensitization and resensitization of proteinase-activated receptor-2
SK Bühm, LM Khitin, EF Grady, G Aponte… - Journal of Biological …, 1996 - ASBMB
Proteinase-activated receptor-2 (PAR-2) is a G-protein-coupled receptor that is expressed
by intestinal epithelial cells, which are episodically exposed to pancreatic trypsin in the
intestinal lumen. Trypsin cleaves PAR-2 to expose a tethered ligand, which irreversibly
activates the receptor. Thus, PAR-2 may desensitize and resensitize by novel mechanisms.
We examined these mechanisms in kidney epithelial cells, stably expressing human PAR-2,
and intestinal epithelial cells, which naturally express PAR-2. Trypsin stimulated a prompt …
by intestinal epithelial cells, which are episodically exposed to pancreatic trypsin in the
intestinal lumen. Trypsin cleaves PAR-2 to expose a tethered ligand, which irreversibly
activates the receptor. Thus, PAR-2 may desensitize and resensitize by novel mechanisms.
We examined these mechanisms in kidney epithelial cells, stably expressing human PAR-2,
and intestinal epithelial cells, which naturally express PAR-2. Trypsin stimulated a prompt …