Thrombin (PAR)

Proteinase-activated receptors (PAR1 and PAR2), a family of four seven-transmembrane G protein-coupled receptors (GPCR-A15), act as targets for signaling by various proteolytic enzymes. PARs are characterized by a unique activation mechanism involving the proteolytic unmasking of a tethered ligand that stimulates the receptor. Given the broad spectrum of roles that PARs have in normal and pathological tissue function, these receptors are emerging as potential therapeutic targets for several diseases including arthritis, colitis, asthma, neurodegenerative conditions, tumor invasion and cardiovascular diseases. The proteolytic mechanisms that regulate PAR activity are more complex than initially anticipated. Thus, via a proteinase, a PAR can be: activated by a tethered ligand mechanism; disarmed for further activation by an activating proteinase; or activated via a non-canonical mechanism involving cleavage at a site distinct from the one that reveals the canonical tethered ligand sequence[1].


[1] Targeting proteinase-activated receptors: therapeutic potential and challenges. R. Ramachandran, F. Noorbakhsh, K. DeFea, M.D. Hollenberg. Nat. Rev. Drug Disc. 2012, 11, 69-86.

6 Item(s)

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Axon ID Name Description From price
2030 E 5555 hydrobromide Potent and orally active PAR1 antagonist €115.00
1622 GB 83 PAR2 antagonist €110.00
1928 ML 161 Allosteric inhibitor of PAR1 €90.00
2055 Q94 hydrochloride Negative allosteric modulator of PAR1 (Gαq linkage) €80.00
1755 SCH 530348 PAR1 antagonist €145.00
1275 SCH 79797 dihydrochloride PAR1 antagonist €95.00

6 Item(s)

per page
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