Thrombin inhibitors based on single-stranded DNA aptamers

Blood Coagulation and Fibrinolysis

Volumn 25, Issue 1, 2014, Pages 39-45

  Gribkova, Irina V ^a,c   Spiridonova, Vera A ^b   Gorbatenko, Alexander S ^a   Denisov, Stepan S ^b   Ataullakhanov, Fazoil I ^a,c   Sinauridze, Elena I ^a,c  

^a N N BLOKHIN NATIONAL MEDICAL RESEARCH CENTER OF ONCOLOGY   (Russian Federation)

^b MOSCOW STATE UNIVERSITY   (Russian Federation)

^c CENTER FOR THEORETICAL PROBLEMS OF PHYSICOCHEMICAL PHARMACOLOGY   (Russian Federation)

Author keywords

aptamers; coagulation; fibrin polymerization; thrombin inhibitor; thrombodynamics

Indexed keywords

ANTICOAGULANT AGENT; APTAMER; EXONUCLEASE; FIBRINOGEN; SINGLE STRANDED DNA; THROMBIN BINDING APTAMER 15; THROMBIN BINDING APTAMER 31; THROMBIN INHIBITOR; UNCLASSIFIED DRUG;

ANTICOAGULATION; ARTICLE; BLOOD; BLOOD CLOTTING; DRUG ACTIVITY; FIBRIN POLYMERIZATION; FUNCTIONAL ASSESSMENT; GROWTH RATE; HEMODYNAMIC PARAMETERS; HUMAN; HUMAN EXPERIMENT; IN VITRO STUDY; IN VIVO STUDY; NORMAL HUMAN; PARTIAL THROMBOPLASTIN TIME; PLASMA; PRIORITY JOURNAL;

ANTICOAGULANTS; APTAMERS, NUCLEOTIDE; BLOOD COAGULATION; DNA, SINGLE-STRANDED; DRUG STABILITY; FIBRIN; FIBRINOGEN; HUMANS; THROMBIN;

EID: 84893711534     PISSN: 09575235     EISSN: 14735733     Source Type: Journal    
DOI: 10.1097/MBC.0b013e32836577f3     Document Type: Article

References (52)

1. Crawley JT, Zanardelli S, Chion CK, Lane DA. The central role of thrombin in hemostasis. J Thromb Haemost 2007; 5 (SUPPL.1):95-101.
2. Lane DA, Philippou H, Huntington JA. Directing thrombin. Blood 2005; 106:2605-2612.
3. Guillin MC, Bezeaud A, Bouton MC, Jandrot-Perrus M. Thrombin specificity. Thromb Haemost 1995; 74:129-133.
4. Chobi SH, Smith SA, Matsushita T, Kojima T. Historical perspective and future direction of coagulation research. J Thromb Haemost 2011; 9 (SUPPL.1):352-363.
5. Hauptmann J, Sturzebecher J. Synthetic inhibitors of thrombin and factor Xa: from bench to bedside. Thromb Res 1999; 93:203-241.
6. Vacca JP. New advances in the discovery of thrombin and factor Xa inhibitors. Curr Opin Chem Biol 2000; 4:394-400.
7. Bauer KA. New anticoagulants: anti IIa vs anti Xa - is one better? J Thromb Thrombolysis 2006; 21:67-72.
8. Straub A, Roehrig S, Hillisch A. Oral, direct thrombin and factor Xa inhibitors: the replacement for warfarin, leeches, and pig intestines? Angew Chem Int Ed 2011; 50:4574-4590.
9. Bauer KA. Recent progress in anticoagulant therapy: oral direct inhibitors of thrombin and factor Xa. J Thromb Haemost 2011; 9 (SUPPL.1):12-19.
10. Okamoto S, Hijikata A, Kikumoto R, Tonomura S, Hara H, Ninomiya K, et al. Potent inhibition of thrombin by the newly synthesized arginine derivative No.805. The importance of stereo-structure of its hydrophobic carboxamide portion. Biochem Biophys Res Commun 1981; 101:440- 446.
11. Stangier J, Rathgen K, Stahle H, Gansser D, Roth W. The pharmacokinetics, pharmacodynamics and tolerability of dabigatran etexilate, a new oral direct thrombin inhibitor, in healthy male subjects. Br J Clin Pharmacol 2007; 64:292-303.
12. Lee JF, Stovall GM, Ellington AD. Aptamers therapeutics advance. Curr Opin Chem Biol 2006; 10:282-289.
13. Tuerk C, Gold L. Systematic evolution of ligands by exponential enrichment RNA ligands to bacteriophage T4 DNA polymerase. Science 1990; 249:505-510.
14. Ellington AD, Szoztak JW. In vitro selection of RNA molecules that bind specific ligands. Nature 1990; 346:818-822.
15. Wilson DS, Szostak JW. In vitro selection of functional nucleic acids. Annu Rev Biochem 1999; 68:611-647.
16. Famulok M, Hartig JS, Mayer G. Functional aptamers and aptazymes in biotechnology, diagnostics, and therapy. Chem Rev 2007; 107:3715- 3743.
17. Gold L, Polisky B, Uhlenbeck O, Yarus M. Diversity of oligonucleotide functions. Annu Rev Biochem 1995; 64:763-797.
18. Nimjee SM, Rusconi CP, Harriington RA, Sullenger BA. The potential of aptamers as anticoagulants. Trends Cardiovasc Med 2005; 15:41-45.
19. Brody EN, Gold L. Aptamers as therapeutic and diagnostic agents. J Biotechnol 2000; 74:5-13.
20. Proske D, Blank M, Buhmann R, Resch A. Aptamers-basic research, drug development, and clinical applications. Appl Microbiol Biotechnol 2005; 69:367-374.
21. Shamah SM, Healy JM, Cload ST. Complex target SELEX. Acc Chem Res 2008; 41:130-138.
22. Kopylov AM, Spiridonova VA. Application of aptamers for medical diagnostics and therapy. Mol Biol (Moscow) 2000; 34:1097-1113; (in Russian; abstract in English).
23. Kul'bachinskyi AV. Methods of aptamer selection for protein targets. Uspekhi Biol Chem (Moscow) 2006; 46:193-224; (in Russian; abstract in English).
24. Rad'ko SP, Rakhmetova SYu, Bodoev NV, Archakov AI. Aptamers as prospective affine reagents for clinical proteomics. Biomed Chem (Moscow) 2007; 53:5-24; (in Russian, abstract in English).
25. Spiridonova VA. Molecular recognizing elements: DNA/RNA-aptamers to proteins. Biomed Chem (Moscow) 2010; 56:639-656; (in Russian, abstract in English).
26. Bock LC, Griffin LC, Latham JA, Vermaas EH, Toole JJ. Selection of singlestranded DNA molecules that bind and inhibit human thrombin. Nature 1992; 355:564-566.
27. Ikebukuro K, Okumura Y, Sumikura K, Karube I. A novel method of screening thrombin-inhibiting DNA aptamers using an evolution-mimicking algorithm. Nucl Acid Res 2005; 33:e108; (doi:10.1093/nar/gni108) (Accessed 12 July 2012).
28. Wu Q, Tsiang M, Sadler JE. Localization of the single-stranded DNA binding site in the thrombin anion-binding exosite. J Biol Chem 1992; 267:24408-24412.
29. Paborsky LR, McCurdy SN, Griffin LC, Toole JJ, Leung LL. The singlestranded DNA aptamer-binding site of human thrombin. J Biol Chem 1993; 268:20808-20811.
30. Wang KY, McCurdy S, Shea RG, Swaminathan S, Bolton PH. A DNA aptamer which binds to and inhibits thrombin exhibits a new structural motif for DNA. Biochemistry 1993; 32:1899-1904.
31. Macaya RF, Waldron JA, Beutel BA, Gao H, Joesten ME, Yang M, et al. Structural and functional characterization of potent antithrombotic oligonucleotides possessing both quadruplex and duplex motifs. Biochemistry 1995; 34:4478-4492.
32. Tasset DM, Kubik MF, Steiner W. Oligonucleotide inhibitors of human thrombin that bind distinct epitopes. J Mol Biol 1997; 272:688-698.
33. Schultze P, Macaya RF, Feigon J. Three-dimensional solution structure of the thrombin-binding DNA aptamer d(GGTTGGTGTGGTTGG). J Mol Biol 1994; 235:1532-1547.
34. Macaya RF, Schultze P, Smith FW, Roe JA, Feigon J. Thrombin-binding DNA aptamer forms a unimolecular quadruplex stricture in solution. Proc Natl Acad Sci USA 1993; 90:3745-3749.
35. Padmanabhan K, Padmanabhan KP, Ferrara JD, Sadier JE, Tulinsky A. The structure of alpha-thrombin inhibited by a 15-mer single-stranded DNA aptamer. J Biol Chem 1993; 268:17651-17654.
36. Shaw J-P, Fishback JA, Cundy KC, Lee WA. A novel oligodeoxynucleotide inhibitor of thrombin. I. In vitro metabolic stability in plasma and serum. Pharmaceut Res 1995; 12:1937-1942.
37. Eder PS, De Vine RJ, Dagle JM, Walder JA. Substrate specificity and kinetics of degradation of antisense oligonucleotides by a 3' exonuclease in plasma. Antisense Res Dev 1991; 1:141-151.
38. Sinauridze EI, Volkova RI, Krasotkina YV, Sarbash VI, Ataullakhanov FI. Dynamics of clot growth induced by thrombin diffusing into nonstirred citrate human plasma. Biochim Biophys Acta 1998; 1425:607-616.
39. Ovanesov MV, Lopatina EG, Saenko EL, Ananyeva NM, Ul'yanova LI, Plyushch OP, et al. Effect of factor VIII on tissue factor-initiated spatial clot growth. Thromb Haemost 2003; 89:235-242.
40. Ovanesov MV, Krasotkina JV, Ul'yanova LI, Abushinova KV, Plyushch OP, Domogatskii SP, et al. Hemophilia A and B are associated with abnormal spatial dynamics of clot growth. Biochim Biophys Acta 2002; 1572: 45-57.
41. Parunov LA, Fadeeva OA, Balandina AN, Soshitova NP, Kopylov KG, Kumskova MA, et al. Improvement of spatial fibrin formation by the anti-TFPI aptamer BAX499: changing clot size by targeting extrinsic pathway initiation. J Thromb Haemost 2011; 9:1825-1834.
42. Fadeeva OA, Panteleev MA, Karamzin SS, Balandina AN, Smirnov IV, Ataullakhanov FI. Thromboplastin immobilized on polystyrene surface exhibits kinetic characteristics close to those for the native protein and activates in vitro blood coagulation similarly to thromboplastin on fibroblasts. Biochemistry (Mosc) 2010; 75:734-743.
43. Dobrovolsky AB, Titaeva EV, Khaspekova SG, Spiridonova VA, Kopylov AM, Mazurov AV. Inhibition of thrombin activity with DNAaptamers. Bull Exp Biol Med 2009; 148:33-36.
44. Griffin LC, Tidmarsh GF, Bock LC, Toole JJ, Leung LLK. In vivo anticoagulant properties of a novel nucleotide-based thrombin inhibitor and demonstration of regional anticoagulation in extracorporeal circuits. Blood 1993; 81:3271-3276.
45. Lee WA, Fishback JA, Shaw JP, Bock LC, Griffin LC, Cundy KC. A novel oligodeoxynucleotide inhibitor of thrombin. II. Pharmacokinetics in the cynomolgus monkey. Pharmaceut Res 1995; 12:1943-1947.
46. Reyderman L, Stavchansky S. Pharmacokinetics and biodistribution of a nucleotide-based thrombin inhibitor in rats. Pharm Res 1998; 15:904- 910.
47. Li WX, Kaplan AV, Grant GW, Toole JJ, Leung LLK. A novel nucleotidebased thrombin inhibitor inhibits clot-bound thrombin and reduces arterial platelet thrombus formation. Blood 1994; 83:677-682.
48. Ikebukuro K, Okumura Y, Sumikura K, Karube I. Novel strategy for DNA aptamers inhibiting enzymatic activity using algorithm mimicking evolution. Nucl Acid Res 2003; 3 (Suppl 3):205-207.
49. Pratt KP, Cô té CF, Chung DW, Stenkamp RE, Davie EW. The primary fibrin polymerization pocket: three-dimensional structure of a 30-kDa C-terminal (chain fragment complexed with the peptide Gly-Pro-Arg-Pro. Proc Natl Acad Sci USA 1997; 94:7176-7181.
50. Elmen W, Mannik M. Kinetics and mechanisms for removal of circulating single-stranded DNA in mice. J Exp Med 1978; 147:684-699.
51. Floege J, Ostendorf T, Janssen U, Burg M, Radeke HH, Vargeese C, et al. Novel approach to specific growth factor inhibition in vivo: antagonism of platelet-derived growth factor in glomerulonephritis by aptamers. Am J Pathol 1999; 154:169-179.
52. Tucker CE, Chen LS, Judkins MB, Farmer JA, Gill SC, Drolet DW. Detection and plasma pharmacokinetics of an antivascular endothelial growth factor oligonucleotide-aptamer (NX1838) in rhesus monkeys. J Chromatogr B Biomed Sci Appl 1999; 732:203-212.