title: Rational design of anticoagulant drugs using oligosaccharide chemistry.
abstract: For a long time, heparin and low molecular weight heparins have been the drugs of choice for the management of thrombosis. Discovery of the antithrombin binding domain in heparin, a critical element in the anticoagulant activity of this polysaccharide, allowed a rational approach based on medicinal carbohydrate chemistry in the design of new anticoagulants. The fully synthetic pentasaccharide fondaparinux that selectively targets blood coagulation factor Xa was first to be developed as a drug. Fondaparinux was followed by various heparin mimicking oligosaccharides prepared with a view to replace polydisperse heparin and low molecular weight heparins by structurally-defined anticoagulants with no unwanted side-effects.
authors.affiliation: Endotis Pharma, Parc Biocitech, 102 Avenue Gaston Roussel 93230, Romainville, France.
authors.forename: Ahmed
authors.initials: A
authors.lastname: El Hadri
authors.forename: Maurice
authors.initials: M
authors.lastname: Petitou
mesh_terms: D000925:Anticoagulants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001777:Blood Coagulation / Q000187:drug effects*; D002240:Carbohydrate Sequence; D015195:Drug Design; D065427:Factor Xa Inhibitors; D008969:Molecular Sequence Data; D008970:Molecular Weight; D009844:Oligosaccharides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000925:Anticoagulants; D065427:Factor Xa Inhibitors; D009844:Oligosaccharides