title: [New antithrombotic oligosaccharides].
abstract: In the early eighties, following breakthroughs in oligosaccharide chemistry, the total chemical synthesis of pentasaccharides has been achieved, representing the antithrombin binding domain of heparin (the active site). The selective inhibitors of coagulation factor Xa thus obtained represent a new type of antithrombotic drugs. In a further step, based on the knowledge of the mechanism of antithrombin activation by heparin, oligosaccharides (pentadeca- to eicosasaccharides), comprising an antithrombin binding domain prolonged by a thrombin binding domain, were designed and synthesised in the Sanofi group. These compounds inhibit both factor Xa and thrombin, in the presence of antithrombin. Endowed with the full anticoagulant activity of heparin but devoid of undesired non-specific interactions, particularly with platelet factor 4 (PF4), they might represent "the ideal heparin-like antithrombotic".
authors.affiliation: Sanofi Recherche, Ligne Hémobiologie, Toulouse.
authors.forename: M
authors.initials: M
authors.lastname: Petitou
authors.forename: J P
authors.initials: JP
authors.lastname: Hérault
authors.forename: A
authors.initials: A
authors.lastname: Bernat
authors.forename: P A
authors.initials: PA
authors.lastname: Driguez
authors.forename: P
authors.initials: P
authors.lastname: Duchaussoy
authors.forename: J C
authors.initials: JC
authors.lastname: Lormeau
authors.forename: J M
authors.initials: JM
authors.lastname: Herbert
mesh_terms: D000818:Animals; D002240:Carbohydrate Sequence; D065427:Factor Xa Inhibitors; D005343:Fibrinolytic Agents / Q000138:chemical synthesis*; D006801:Humans; D008969:Molecular Sequence Data; D009844:Oligosaccharides / Q000737:chemistry*; D013917:Thrombin / Q000037:antagonists & inhibitors*
chemical_list: D065427:Factor Xa Inhibitors; D005343:Fibrinolytic Agents; D009844:Oligosaccharides; D013917:Thrombin
vernacular_title: Nouveaux oligosaccharides antithrombotiques.