title: [Natural and synthetic inhibitors of thrombin. I. Natural inhibitors].
abstract: Structures and properties of main physiological (heparin, antithrombin III, heparin cofactor II) and nonphysiological (hirudin, thrombin-binding aptamers, cyclotheonamides) natural thrombin inhibitors and its fragments and synthetic analogs (hirugen, hirulogs, hirunorms, pentasaccharides, macrocyclic alpha-keto amides) were reviewed. The molecular mechanisms of interaction of these compounds with thrombin and their anticoagulant activity at preclinical and clinical trials are discussed. The examined of natural thrombin inhibitors and their synthetic fragments and analogs are perspective for prophylaxis and treatment of different thrombo-embolic diseases.
authors.affiliation: Institute of Bioorganic Chemistry and Petrolchemistry, Ukrainian National Academy of Sciences, Kyiv.
authors.forename: V K
authors.initials: VK
authors.lastname: Kibirev
authors.forename: A A
authors.initials: AA
authors.lastname: Gershkovich
mesh_terms: D000990:Antithrombin III / Q000502:physiology; D000991:Antithrombins / Q000494:pharmacology / Q000502:physiology*; D002240:Carbohydrate Sequence; D005343:Fibrinolytic Agents / Q000494:pharmacology*; D006493:Heparin / Q000502:physiology; D015844:Heparin Cofactor II / Q000502:physiology; D006629:Hirudins / Q000031:analogs & derivatives / Q000494:pharmacology; D006801:Humans; D008969:Molecular Sequence Data; D009844:Oligosaccharides / Q000494:pharmacology
chemical_list: D000991:Antithrombins; D005343:Fibrinolytic Agents; D006629:Hirudins; D009844:Oligosaccharides; D015844:Heparin Cofactor II; D000990:Antithrombin III; D006493:Heparin