title: Heparinase I acts on a synthetic heparin pentasaccharide corresponding to the antithrombin III binding site.
abstract: A synthetic pentasaccharide, containing an intact antithrombin III (ATIII) binding site that is in clinical studies a specific antifactor Xa agent, serves as a substrate for a heparin lyase (heparinase I, EC 4.2.2.7) from Flavobacterium heparinum. Heparinase I, currently being assessed as a heparin reversal agent, also reverses the antifactor Xa activity of this synthetic pentasaccharide by breaking it down to inactive disaccharide and trisaccharide products.
authors.affiliation: Division of Medicinal and Natural Products Chemistry, University of Iowa, Iowa City, IA 52242, USA.
authors.forename: G
authors.initials: G
authors.lastname: Yu
authors.forename: L
authors.initials: L
authors.lastname: LeBrun
authors.forename: N S
authors.initials: NS
authors.lastname: Gunay
authors.forename: D
authors.initials: D
authors.lastname: Hoppensteadt
authors.forename: J M
authors.initials: JM
authors.lastname: Walenga
authors.forename: J
authors.initials: J
authors.lastname: Fareed
authors.forename: R J
authors.initials: RJ
authors.lastname: Linhardt
mesh_terms: D000990:Antithrombin III / Q000737:chemistry; D001665:Binding Sites; D002240:Carbohydrate Sequence; D004305:Dose-Response Relationship, Drug; D065427:Factor Xa Inhibitors; D005417:Flavobacterium / Q000201:enzymology; D006493:Heparin / Q000737:chemistry / Q000378:metabolism*; D019763:Heparin Lyase / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D008969:Molecular Sequence Data; D009844:Oligosaccharides / Q000737:chemistry / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000737:chemistry
chemical_list: D065427:Factor Xa Inhibitors; D009844:Oligosaccharides; D015842:Serine Proteinase Inhibitors; C049714:IC 831423; D000990:Antithrombin III; D006493:Heparin; D019763:Heparin Lyase