Table 6 PAR2 signaling modulators
Class | Agonist/ Antagonist | Name | Receptor/Cell/Tissue type | Cellular response |
|---|---|---|---|---|
Peptide | Agonist | SLIGRL/−NH2 | Human, Rat | |
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 | Â | 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] |