Kibirev V K, Gershkovich A A
Institute of Bioorganic Chemistry and Petrolchemistry, Ukrainian National Academy of Sciences, Kyiv.
Ukr Biokhim Zh (1999). 1999 Jan-Feb;71(1):5-15.
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.
综述了主要生理性（肝素、抗凝血酶III、肝素辅因子II）和非生理性（水蛭素、凝血酶结合适体、环丝氨酸酰胺）天然凝血酶抑制剂及其片段和合成类似物（水蛭肽、水蛭素类似物、水蛭素规范物、五糖、大环α-酮酰胺）的结构与性质。讨论了这些化合物与凝血酶相互作用的分子机制及其在临床前和临床试验中的抗凝血活性。对天然凝血酶抑制剂及其合成片段和类似物的研究对于不同血栓栓塞性疾病的预防和治疗具有前景。
