Recombinant Human PAR1/Thrombin Receptor protein (His tag)

Specifications

Form

Lyophilized

General info

Function

High affinity receptor that binds the activated thrombin, leading to calcium release from intracellular stores (PubMed : 1672265, PubMed : 8136362). The thrombin-activated receptor signaling pathway is mediated through PTX-insensitive G proteins, activation of phospholipase C resulting in the production of 1D-myo-inositol 1,4,5-trisphosphate (InsP3) which binds to InsP3 receptors causing calcium release from the stores (By similarity). In astrocytes, the calcium released into the cytosol allows the Ca(2+)-dependent release of L-glutamate into the synaptic cleft through BEST1, that targets the neuronal postsynaptic GRIN2A/NMDAR receptor resulting in the synaptic plasticity regulation (By similarity). May play a role in platelets activation and in vascular development (PubMed : 10079109). Mediates up-regulation of pro-inflammatory cytokines, such as MCP-1/CCL2 and IL6, triggered by coagulation factor Xa (F10) in cardiac fibroblasts and umbilical vein endothelial cells (PubMed : 30568593, PubMed : 34831181).

Sequence similarities

Belongs to the G-protein coupled receptor 1 family.

Post-translational modifications

Proteolytic cleavage by thrombin generates a new N-terminus that functions as a tethered ligand (PubMed:1672265, PubMed:7744748). Also proteolytically cleaved by cathepsin CTSG (PubMed:7744748). Cleavage at 41-Arg-|-Ser-42 by CTSG results in receptor activation while cleavage at 55-Phe-|-Trp-56 results in inhibition of receptor activation (PubMed:7744748).. Phosphorylated in the C-terminal tail; probably mediating desensitization prior to the uncoupling and internalization of the receptor.