title: Structure-activity studies of the thrombin receptor activating peptide.
abstract: Cleavage of the human platelet thrombin receptor by thrombin exposes a new N-terminal which acts as a putative tethered ligand. A synthetic peptide--"SFLL" (SFLLRNPNDKYEPF), corresponding to the new N-terminal region, activates and induces platelet aggregation and serotonin secretion. We have found that the pentapeptide--SFLLR is the minimal peptide length which retains full activity in inducing [14C]serotonin secretion. Structure-activity relationship studies were performed on this pentameric peptide. Systematic replacement of all amino acids with L-Ala indicated the importance of F-2, L-3 and R-5 for activity. Further studies demonstrated that the positive charge at the N-terminus, but not at the C-terminus of the pentapeptide, is crucial for activity.
authors.affiliation: Israel Institute for Biological Research, Ness-Ziona.
authors.forename: T
authors.initials: T
authors.lastname: Sabo
authors.forename: D
authors.initials: D
authors.lastname: Gurwitz
authors.forename: L
authors.initials: L
authors.lastname: Motola
authors.forename: P
authors.initials: P
authors.lastname: Brodt
authors.forename: R
authors.initials: R
authors.lastname: Barak
authors.forename: E
authors.initials: E
authors.lastname: Elhanaty
mesh_terms: D000595:Amino Acid Sequence; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism*; D006801:Humans; D008969:Molecular Sequence Data; D009842:Oligopeptides / Q000138:chemical synthesis / Q000494:pharmacology*; D010974:Platelet Aggregation / Q000187:drug effects*; D011956:Receptors, Cell Surface / Q000378:metabolism*; D018179:Receptors, Thrombin; D012701:Serotonin / Q000097:blood; D013329:Structure-Activity Relationship; D013917:Thrombin / Q000378:metabolism*
chemical_list: D009842:Oligopeptides; D011956:Receptors, Cell Surface; D018179:Receptors, Thrombin; D012701:Serotonin; D013917:Thrombin