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Table 6 PAR2 signaling modulators

From: Protease-activated receptors (PARs): mechanisms of action and potential therapeutic modulators in PAR-driven inflammatory diseases

Class Agonist/ Antagonist Name Receptor/Cell/Tissue type Cellular response
Peptide Agonist SLIGRL/−NH2 Human, Rat Induces calcium release [2, 8, 136, 139]
SLIGKV/−NH2 Human Induces calcium release [136]
2f-LIGRLO/−NH2 Human, Rat Induces calcium release [140]
Antagonist FSLLRY-NH2 Human Blocks trypsin, not SLIGRL activation, reduces proinflammatory IL-8 and TNFα [82]
Rat Inhibits neuropathic pain [304]
LSIGRL-NH2 Human Blocks trypsin, not SLIGRL induced calcium release [305]
Peptidomimetic Antagonist K14585, K12940 Human Reduces SLIGKV induced calcium release [306]
Human Inhibits SLIGRL induced NFkB activation [307]
C391a Human, Mouse Blocks calcium release and MAPK activation [308]
Non-peptide small molecule Agonist GB110 Human Induces calcium release [309]
AC-5541, AC-264613 Human Induces calcium release [310]
Rat Induces edema and hyperalgesia [310]
Antagonist ENMD-1068 Human Blocks p.acnes induced calcium release and induction of IL-1a, IL-8 and TNFα [92]
Human Inhibited FVIIa induced cancer cell migration [311]
Mouse Reduces joint inflammation [260]
Mouse Blocks calcium release and reduces liver fibrosis [312]
GB83 Human Inhibits trypsin and PAR2-AP calcium release [313]
GB88 Human Blocks PAR2 induced calcium release [309]
Rat Reduces acute paw edema, inhibits PAR2-AP induced inflammation [309, 314]
AZ8838 AZ3451 Human Blocks PAR2-AP induced calcium release and β-arrestin recruitment [315]
Pepducin Antagonist P2pal-18S Human Blocks PAR2 induced calcium release [316]
Mouse Decreases risk for developing severe biliary pancreatitis [317]
P2pal-14GQ Human Blocks PAR2 induced calcium release [316]
Antibiotic Antagonist Tetracyclines (Tetracycline, Doxycycline, Minocycline) Human Inhibits SLIGRL induced IL-8 release [318]
Mouse Topical application of tetracycline decreases PAR2 induced skin inflammation [319]
Rat Subantimicrobial doses of doxycycline inhibit PAR2 induced inflammation [320]
Antibody   SAM-11 Mouse Reduces joint inflammation [260]
Mouse Prevents allergic inflammation [124]
B5 Mouse Reduces joint inflammation [260]
Mouse Inhibits allergic airway inflammation [124]
MAB3949 Human Blocks trypsin induced PAR2 activation [315]