Proteinases and signalling: pathophysiological and therapeutic implications via PARs and more.

@article{Ramachandran2008ProteinasesAS,
  title={Proteinases and signalling: pathophysiological and therapeutic implications via PARs and more.},
  author={Rithwik Ramachandran and Morley D Hollenberg},
  journal={British journal of pharmacology},
  year={2008},
  volume={153 Suppl 1},
  pages={S263-82}
}
Proteinases like thrombin, trypsin and tissue kallikreins are now known to regulate cell signaling by cleaving and activating a novel family of G-protein-coupled proteinase-activated receptors (PARs 1-4) via exposure of a tethered receptor-triggering ligand. On their own, short synthetic PAR-selective PAR-activating peptides (PAR-APs) mimicking the tethered ligand sequences can activate PARs 1, 2 and 4 and cause physiological responses both in vitro and in vivo. Using the PAR-APs as sentinel… CONTINUE READING