发明名称 |
MODIFIED DNA APTAMERS INHIBITING THROMBIN ACTIVITY |
摘要 |
FIELD: chemistry; biochemistry. ^ SUBSTANCE: invention relates to biotechnology and medicine and specifically to direct thrombin inhibitors. The invention discloses a modified aptamer oligodeoxyribonucleotide of general formula d R-GTGACGTANGGTTGGTGTGGTTGGGGCGTCAC-R where d is deoxyribose (oligonucleotide contains deoxyribose in all positions), R denotes chemical substitutes. The substitute used is aminohexanol (NH2 group), which esterifies the phosphate group on the 5' or 3' end and PEG which is bonded on the 5' and/or 3' end. At least one of the substitutes bonded on the 5' or 3' end is polyethylene glycol (PEG). The disclosed modified DNA aptamer inhibits thrombin activity in human blood plasma by prolonging thrombin clotting time, prothrombin time and activated partial thromboplastin time and inhibits thrombin-stimulated aggregation of thrombocytes. During intravenous administration to an experimental animal, the modified DNA aptamer circulates in the blood longer than the basic aptamer RE31. ^ EFFECT: said DNA aptamer can serve as the base for antithrombotic medicinal agents. ^ 6 dwg, 3 ex |
申请公布号 |
RU2410432(C1) |
申请公布日期 |
2011.01.27 |
申请号 |
RU20090142862 |
申请日期 |
2009.11.23 |
申请人 |
GOSUDARSTVENNOE UCHREZHDENIE NAUCHNO-ISSLEDOVATEL'SKIJ INSTITUT FIZIKO-KHIMICHESKOJ BIOLOGII IMENI A.N. BELOZERSKOGO MOSKOVSKOGO GOSUDARSTVENNOGO UNIVERSITETA IMENI M.V. LOMONOSOVA;FEDERAL'NOE GOSUDARSTVENNOE UCHREZHDENIE "ROSSIJSKIJ KARDIOLOGICHESKIJ NAUCHNO-PROIZVODSTVENNYJ KOMPLEKS FEDERAL'NOGO AGENTSTVA PO VYSOKOTEKHNOLOGICHNOJ MEDITSINSKOJ POMOSHCHI" |
发明人 |
SPIRIDONOVA VERA ALEKSEEVNA;GOLOVIN ANDREJ VIKTOROVICH;KOPYLOV ALEKSEJ MIKHAJLOVICH;DOBROVOL'SKIJ ANATOLIJ BORISOVICH;MAZUROV ALEKSEJ VLADIMIROVICH |
分类号 |
A61K31/712;C12N15/115;C12N15/15 |
主分类号 |
A61K31/712 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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