title: Characteristics of a new DNA aptamer, direct inhibitor of thrombin.
abstract: Characteristics of a new antithrombin DNA-aptamer RE31 were studied. This aptamer inhibited thrombin formation in human plasma catalyzed by exogenous (lengthening of thrombin time) and endogenous thrombin (lengthening of partial prothrombin time and activated partial thromboplastin time). In addition, the aptamer completely suppressed thrombin-induced aggregation of human platelets. On the other hand, RE31 did not reduce amidolytic activity of thrombin towards the short peptide substrate, in other words, did not modify the state of enzyme active center. By the capacity to inhibit clotting reactions, RE31 was superior to the previously described highly effective 31-component antithrombin aptamer 31TBA (thrombin binding aptamer, TBA). The effect of RE31 was species-specific: it inhibited human thrombin activity more effectively than activities of rat and rabbit thrombins.
authors.affiliation: Russian Cardiology Research and Production Complex, Federal Agency for High-Technological Medical Care, Moscow, Russia. calab@cardio.ru
authors.forename: A V
authors.initials: AV
authors.lastname: Mazurov
authors.forename: E V
authors.initials: EV
authors.lastname: Titaeva
authors.forename: S G
authors.initials: SG
authors.lastname: Khaspekova
authors.forename: A N
authors.initials: AN
authors.lastname: Storojilova
authors.forename: V A
authors.initials: VA
authors.lastname: Spiridonova
authors.forename: A M
authors.initials: AM
authors.lastname: Kopylov
authors.forename: A B
authors.initials: AB
authors.lastname: Dobrovolsky
mesh_terms: D000818:Animals; D000991:Antithrombins / Q000494:pharmacology*; D052157:Aptamers, Nucleotide / Q000494:pharmacology*; D001777:Blood Coagulation / Q000187:drug effects / Q000502:physiology; D006801:Humans; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D013917:Thrombin / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000991:Antithrombins; D052157:Aptamers, Nucleotide; D010975:Platelet Aggregation Inhibitors; D013917:Thrombin