title: Inhibition of platelet adhesion by peptidomimetics mimicking the interactive β-hairpin of glycoprotein Ibα.
abstract: β-Hairpin peptidomimetics mimicking the interaction sites of the platelet receptor glycoprotein (GP)Ibα with von Willebrand factor (vWF) were synthesised and evaluated for their ability to increase platelet velocity under high shear conditions and to inhibit shear-induced platelet aggregation. A cyclic and bridged dodecapeptide 2e containing a heterochiral diproline motif was identified as a lead compound for the generation of a novel class of potential antiplatelet agents.
authors.affiliation: Centre for Synthesis & Chemical Biology, Department of Pharmaceutical & Medicinal Chemistry, 123, St. Stephen's Green, Dublin 2, Ireland.
authors.forename: Elise
authors.initials: E
authors.lastname: Bernard
authors.forename: Vivienne
authors.initials: V
authors.lastname: Buckley
authors.forename: Edelmiro
authors.initials: E
authors.lastname: Moman
authors.forename: Lorraine
authors.initials: L
authors.lastname: Coleman
authors.forename: Gerardene
authors.initials: G
authors.lastname: Meade
authors.forename: Dermot
authors.initials: D
authors.lastname: Kenny
authors.forename: Marc
authors.initials: M
authors.lastname: Devocelle
mesh_terms: D001665:Binding Sites; D006801:Humans; D057786:Peptidomimetics / Q000737:chemistry / Q000494:pharmacology*; D010973:Platelet Adhesiveness / Q000187:drug effects*; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry*; D019038:Platelet Glycoprotein GPIb-IX Complex / Q000737:chemistry* / Q000378:metabolism; D011485:Protein Binding; D017433:Protein Structure, Secondary; D014841:von Willebrand Factor / Q000737:chemistry / Q000378:metabolism
chemical_list: D057786:Peptidomimetics; D010975:Platelet Aggregation Inhibitors; D019038:Platelet Glycoprotein GPIb-IX Complex; D014841:von Willebrand Factor