Modulating human proteinase activated receptor 2 with a novel antagonist (GB88) and agonist (GB110)

BACKGROUND AND PURPOSE Many cells express proteinase activated receptor 2 (PAR2) on their plasma membrane. PAR2 is activated by proteolytic enzymes, such as trypsin and tryptase that cleave the receptor N‐terminus, inititating signalling to intracellular G proteins. Studies on PAR2 have relied heavi...

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Veröffentlicht in:	British journal of pharmacology 2012-03, Vol.165 (5), p.1413-1423
Hauptverfasser:	Suen, JY, Barry, GD, Lohman, RJ, Halili, MA, Cotterell, AJ, Le, GT, Fairlie, DP
Format:	Artikel
Sprache:	eng
Schlagworte:	agonist Animals antagonist Anti-Inflammatory Agents - pharmacology anti‐inflammatory Biological and medical sciences Calcium - metabolism Cell Line Dipeptides - pharmacology Edema - metabolism HT29 Cells Humans Inflammation - drug therapy Inflammation - metabolism Isoxazoles - pharmacology Medical sciences Oligopeptides - metabolism Oligopeptides - pharmacology Peptides - metabolism Pharmacology. Drug treatments Piperidines - pharmacology proteinase activated receptor 2 Rats Receptor, PAR-1 - metabolism Receptor, PAR-2 - agonists Receptor, PAR-2 - antagonists & inhibitors Receptor, PAR-2 - metabolism Research Papers Spiro Compounds - pharmacology Trypsin - metabolism
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