DNA aptamers for human thrombin with high anticoagulant activity demonstrate target-and species-specificity

Current Medicinal Chemistry

Volumn 19, Issue 30, 2012, Pages 5232-5237

  Zavyalova, E ^a,b   Golovin, A ^a,b   Timoshenko, T ^b,c   Babiy, A ^b   Pavlova, G ^b,c   Kopylov, A ^a,b  

^a MOSCOW STATE UNIVERSITY   (Russian Federation)

^b LTD 'APTO PHARM ^*  (Russian Federation)

^c RUSSIAN ACADEMY OF SCIENCES   (Russian Federation)

Author keywords

Anticoagulant; DNA aptamer; Hemostasis; Species specificity; Specificity; Target specificity; Thrombin; Thrombin inhibitor

Indexed keywords

ANTICOAGULANT AGENT; APTAMER; BLOOD CLOTTING FACTOR 10; BLOOD CLOTTING FACTOR 5; BLOOD CLOTTING FACTOR 7; DNA; FIBRINOGEN; PROTHROMBIN; RA 36; THROMBIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANTICOAGULATION; ARTICLE; BLOOD CLOTTING TEST; BLOOD SAMPLING; ENZYME INHIBITION; HUMAN; HYDROLYSIS; NONHUMAN; PROTEIN STRUCTURE; PROTHROMBIN DEFICIENCY; SPECIES DIFFERENCE; TURBIDIMETRY;

ANIMALS; ANTICOAGULANTS; APTAMERS, NUCLEOTIDE; BLOOD COAGULATION; CATTLE; FIBRINOGEN; HAPLORHINI; HUMANS; MICE; RABBITS; RATS; SPECIES SPECIFICITY; THROMBIN;

EID: 84870420969     PISSN: 09298673     EISSN: 1875533X     Source Type: Journal    
DOI: 10.2174/092986712803530575     Document Type: Article

References (25)

1. De Souza, E.B.; Cload, S.T.; Pendergrast, P.S.; Sah, D.W.Y. Novel therapeutic modalities to address nondrugable protein interaction targets. Neuropsychopharmacology, 2009, 34, 142-158.
2. Pendergrast, P.S.; Marsh, H.N.; Grate, D.; Healy, J.M.; Stanton, M. Nucleic acid aptamers for target validation and therapeutic applications. J. Biomol. Tech., 2005, 16, 224-234.
3. Bock, L.C., Griffin, L.C., Latham, J.A., Vermaas, E.H., and Toole, J.J. Selection of single-stranded DNA molecules that bind and inhibit human thrombin. Nature, 1992, 355, 564-566.
4. Padmanabhan, K.; Padmanabhan, K.P.; Ferrara, J.D.; Sadler, J.E.; Tulinsky, A. The structure of α-thrombin inhibited by a 15-mer single-stranded DNA aptamer. J. Biol. Chem., 1993, 268(24), 17651-17654.
5. Padmanabhan, K.; Tulinsky, A. An ambiguous structure of a DNA 15-mer thrombin complex. Acta Crystallogr D Biol Crystallogr., 1996, 52, 272-282.
6. Pagano, B.; Martino, L.; Randazzo, A.; Giancola, A. Stability and binding properties of a modified thrombin binding aptamer. Biophys. J., 2008, 94(2), 562-569.
7. Diener, J. L.; Wagner-Whyte, J.; Fontana, D. Aptamers that bind thrombin with high affinity. U.S. Patent 60/711,768, August 26, 2005.
8. Ikebukuro, K.; Okumura, Y.; Sumikura, K.; Karube, I. A novel method of screening thrombin-inhibiting DNA aptamers using an evolution-mimicking algorithm. Nucleic Acids Res., 2005, 33(12), e108.
9. Zavyalova, E.; Golovin, A.; Reshetnikov, R.; Mudrik, N.; Panteleyev, D.; Pavlova, G.; Kopylov, A. Novel modular DNA aptamer for human thrombin with high anticoagulant activity. Curr. Med. Chem., 2011, 18, 3343-3350.
10. Golovin, A.V.; Kopylov, A.M.; Reshetnikov, R.V.; Zavyalova, E.G.; Pavlova, G.V.; Babiy, V.E. Antithrombin aptamers and a method of their structure stabilization. The patent pending according to Patent Collaboration Treaty WO 2011/075004 A1, December 13, 2010, published on June 23, 2011.
11. Web-site of Archemix company http://www.archemix.com (Accessed March 15, 2011).
12. Golovin, A.V., Kopylov, A.M.; Zavyalova, E.G.; Pavlova, G.V.; Mudrik, N.N.; Babiy, V.E. A method for thrombin activity determination. Russian Patent 2429488, May 18, 2010.
13. Zavyalova, E.G.; Protopopova, A.D., Yaminsky, I.V.; Kopylov, A.M. Kinetic characterization of inhibition of human thrombin with DNA aptamers by turbidimetric assay. Anal. Biochem., 2012, 421, 234-239.
14. Van Den Besselaar, A.M.H.P.; Barrowcliffe, T.W.; Houbouyan-Reveillard, L.L.; Jespersen, J.; Johnston, M.; Poller, L.;Tripodi, A. Guidelines on preparation, certification, and use of certified plasmas for ISI calibration and INR determination. J. Thromb. Haemost., 2004, 2, 1946-1953.
15. Kretz, C.A.; Stafford, A.R.; Fredenburgh, J.C.; Weitz, J.I. HD1, a thrombindirected aptamer, binds exosite 1 on prothrombin with high affinity and inhibits its activation by prothrombinase. J. Biol. Chem., 2006, 281, 37477-37485.
16. Tasset, D.M.; Kubik, M.F.; Steiner, W. Oligonucleotide inhibitors of human thrombin that bind distinct epitopes. J. Mol. Biol., 1997, 272, 688-698.
17. UniProtKB DataBase http://www.uniprot.org (Accessed December 19, 2011).
18. Muller, J.; Freitag, D.; Mayer, G; Potzsch B. Anticoagulant characteristics of HD1-22, a bivalent aptamer that specifically inhibits thrombin and prothrombinase. J. Thromb. Haemost., 2008, 6 (12), 2105-2112.
19. Mendelboum Raviv, S.; Horvath, A.; Aradi, J.; Bagoly, Z.; Fazakas, F.; Batta, Z.; Muszbek, L.; Harsfalvi, J. 4-thio-deoxyuridylate-modified thrombin aptamer and its inhibitory effect on fibrin clot formation, platelet aggregation and thrombus growth on subendothelial matrix. J. Thromb. Haemost., 2008, 6 (10), 1764-1771.
20. Boncler, M.A.; Koziolkiewicz, M.; Watala C. Aptamer inhibits degradation of platelet proteolytically activatable receptor, PAR-1, by thrombin. Thromb. Res., 2001, 104 (3), 215-222.
21. Nowak, G. The ecarin clotting time, a universal method to quantify direct thrombin inhibitors. Pathophysiol. Haemost. Thromb., 2003, 33, 173-183.
22. Anderson, P.J.; Bock, P.E. Role of prothrombin fragment 1 in the pathway of regulatory exosite I formation during conversion of human prothrombin to thrombin. J. Biol. Chem., 2003, 278(45), 44489-44495.
23. th ed.; Lippincott Williams & Wilkins: Philadelphia, 2010.
24. Paborsky, L.R.; McCurdy, S.N.; Griffin, L.C.; Toole, J.J.; Leung, L.L.K. The single-stranded DNA aptamer-binding site of human thrombin. J. Biol. Chem., 1993, 288(28), 20808-20811.
25. Kretz, C.A.; Stafford, A.R.; Fredenburgh, J.C.; Weitz, J.I. HD1, a Thrombindirected aptamer, binds exosite 1 on prothrombin with high affinity and inhibits its activation by prothrombinase. J. Biol. Chem., 2006, 281(49), 37477-37485.