Article
Molecular basis for activation and biased signaling at the thrombin-activated GPCR proteinase activated receptor-4 (PAR4).
The Journal of biological chemistry - 21 Feb 2020
Thibeault Pierre E, LeSarge Jordan C, Arends D'Arcy, Fernandes Michaela, Chidiac Peter, Stathopulos Peter B, Luyt Leonard G, Ramachandran Rithwik
Abstract excerpt
Proteinase-activated receptor (PAR)-4 is a member of the proteolytically-activated PAR family of G-protein-coupled receptors (GPCR) that represents an important target in the development of anti-platelet therapeutics. PARs are activated by proteolytic cleavage of their receptor N terminus by enzymes such as thrombin, trypsin, and cathepsin-G. This reveals the receptor-activating motif, termed the tethered ligand...
Topics
- Alanine
- Amino Acid Substitution
- Calcium
- Calcium Signaling
- GTP-Binding Protein alpha Subunits, Gq-G11
- HEK293 Cells
- Humans
- Isomerism
- MAP Kinase Signaling System
- Methylation