Receptor binding and agonist efficacy: new insights from mutants of the thrombin protease-activated receptor-1 (PAR-1). 2000

M D Hollenberg
Department of Pharmacology and Therapeutics and Department of Medicine, University of Calgary, Faculty of Medicine, Calgary, Alberta, Canada. mhollenb@ucalgary.ca

UI MeSH Term Description Entries
D008024 Ligands A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed) Ligand
D009154 Mutation Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations. Mutations
D010446 Peptide Fragments Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques. Peptide Fragment,Fragment, Peptide,Fragments, Peptide
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D013917 Thrombin An enzyme formed from PROTHROMBIN that converts FIBRINOGEN to FIBRIN. Thrombase,Thrombin JMI,Thrombin-JMI,Thrombinar,Thrombostat,alpha-Thrombin,beta,gamma-Thrombin,beta-Thrombin,gamma-Thrombin,JMI, Thrombin
D044463 Receptor, PAR-1 A thrombin receptor subtype that couples to HETEROTRIMERIC GTP-BINDING PROTEINS resulting in the activation of a variety of signaling mechanisms including decreased intracellular CYCLIC AMP, increased TYPE C PHOSPHOLIPASES and increased PHOSPHOLIPASE A2. PAR-1 Receptor,Protease-Activated Receptor 1,PAR1 Receptor,Proteinase-Activated Receptor 1,PAR 1 Receptor,Protease Activated Receptor 1,Proteinase Activated Receptor 1,Receptor, PAR 1,Receptor, PAR1
D018179 Receptors, Thrombin A family of proteinase-activated receptors that are specific for THROMBIN. They are found primarily on PLATELETS and on ENDOTHELIAL CELLS. Activation of thrombin receptors occurs through the proteolytic action of THROMBIN, which cleaves the N-terminal peptide from the receptor to reveal a new N-terminal peptide that is a cryptic ligand for the receptor. The receptors signal through HETEROTRIMERIC GTP-BINDING PROTEINS. Small synthetic peptides that contain the unmasked N-terminal peptide sequence can also activate the receptor in the absence of proteolytic activity. Thrombin Receptors,TRAP Peptide,Thrombin Receptor,Thrombin Receptor Activating Peptide Ligand,Thrombin Receptor Activating Peptides,Thrombin Receptor Activator Peptide,Peptide, TRAP,Receptor, Thrombin

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