lmmol · Proteins

Proteinase-activated receptor 1

UniProt P25116 Organism Homo sapiens Gene CF2R, F2R, PAR1, TR

Also known as: CF2R, F2R, PAR1, TR

Function

High affinity receptor that binds the activated thrombin, leading to calcium release from intracellular stores. 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. 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.

Classification

Family (Pfam)
PF00001 7tm_1
InterPro
GPCR_Rhodpsn, GPCR_Rhodpsn_7TM, Protea_act_rcpt, Thrmbn_rcpt
Functional cluster
G Protein-Coupled Receptors

Experimental structures · PDB · 13

A predicted model is available from AlphaFold.

Gene Ontology · 56

Drugs targeting this protein · 3

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Literature · 14 cited papers

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