Protease-Activated Receptors
Cambridge Bioscience, through our collaboration with ChanTest, offers access to GPCR screening and profiling services to the following protease-activated receptor targets:
PAR1
Synonym: F2R
Validated Assay/Platform: Calcium
Description: Protease-activated receptor-1 (PAR1) belongs to a four-member family of GPCRs that are activated by proteases (see Ossovskaya et al for review). These proteases cleave a specific extracellular amino-terminal domain of the receptor to reveal a tethered ligand, which in turn activates the receptor which couples via Gq to release intracellular calcium (Nystedt, S. et al., 1995). PAR1 is expressed in platelets, vasculature, GI tract, CNS, lung, kidney, liver and heart. PAR1 is a relevant target for coronary thrombosis, inflammatory bowel disease and cancer.
PAR2
Synonym: F2RL1, coagulation factor II (thrombin) receptor-like 1
Validated Assay/Platform: Binding & Calcium
Description: Protease-activated receptor-2 (PAR2) belongs to a four-member family of GPCRs that are activated by proteases (see Ossovskaya et al for review). These proteases cleave a specific extracellular amino-terminal domain of the receptor to reveal a tethered ligand, which in turn activates the receptor which couples via Gq to release intracellular calcium (Nystedt, S. et al., 1995). PAR2 is expressed in the vasculature, GI tract, CNS, lung, kidney, liver, and heart. PAR2 is a relevant target for arthritis, inflammation, bowel disease, and cancer.
PAR4
Synonym: F2RL3, coagulation factor II (thrombin) receptor-like 3
Validated Assay/Platform: Calcium
Description: Protease-activated receptor-4 (PAR4) belongs to a four-member family of GPCRs that are activated by proteases (see Ossovskaya et al for review). These proteases cleave a specific extracellular amino-terminal domain of the receptor to reveal a tethered ligand, which in turn activates the receptor which couples via Gq to release intracellular calcium (Nystedt, S. et al., 1995). PAR4 is expressed in the vasculature, GI tract, leukocytes, lung, and heart. PAR4 is a relevant target for coronary thromboses, inflammatory bowel disease and cancer.
Platforms Available
Cambridge Bioscience, through our collaboration with ChanTest, offers access to both FLIPRTETRA® and FlexStation® 3 allowing you to select the right balance of speed, throughput and data quality to suit your needs.
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