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Document IX. Conclusions Page 289 Factor Xa is clearly an important component of the coagulation process and inhibition of this enzyme can lead to potent anticoagulant effects. Recently, a number of naturally occurring anti-Factor-Xa polypeptides have been isolated from several hematophagous organisms including ticks, leeches, and hook- worms. With the exception of TAP, these molecules appear to bind to Factor Xa by the standard mechanism of inhibition proposed earlier [49]. The sequence information derived from these inhibitors as well as the natural cleavage sites of substrates of Factor Xa can be used along with the conformational constraints imposed by the proposed substrate-like binding to define the pharmacophore requirements of the active site of Factor Xa. The structurally rigid BPTI mutants, which have been found to be potent Factor Xa inhibitors, also provide important conformational information particularly with regard to the specific binding interactions on the P' side of the Factor Xa active site. A number of small molecule inhibitors have also recently been reported which appear to take advantage of a unique cation-π S4-site available in Factor Xa to achieve good selectivity with moderate potency. The availbility of the X-ray structure of native Factor Xa has allowed molecular modeling approaches to suggest possible fits of these inhibitors to the Factor Xa active site. Note Added in Proof After this review was written, the x-ray structure of Factor Xa with DX-9065a was reported [81]. References 1. Proteinase inhibitors. In: Barrett AJ, Salvesen G, eds. Research Monographs in Cell and Tissue Physiology. Vol 12. New York: Elsevier, 1986. Design of Enzyme Inhibitors as Drugs. Sandler M, Smith HJ, eds. New York: Oxford University Press, 1989. 2. Colman RW, Hirsh J, Marder VJ, Salzman EW. Hemostasis and Thrombosis. Basic Principles and Clinical Practice. Second Edition. Philadelphia: J. B. Lippincott Company, 1987. 3. Hathaway, WE, Goodnight, Jr SH. Disorders of Hemostasis and Thrombosis. New York: McGraw- Hill, 1993. 4. Padmanabhan K, Padmanabhan KP, Tulinsky A, Park CH, Bode W, Huber R, Blankenship DT, Cardin AD, Kisiel W. Structure of human Des(1–45) factor Xa at 2.2 Å resolution. J Mol Biol 1993; 232:947–966. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_289.html [4/5/2004 5:15:45 PM]
Document Page 290 5. Kaiser B, Hauptmann J. Factor Xa inhibitors as novel antithrombotic agents: facts and perspectives. Cardiovascular Drug Reviews 1994; 12 (3):225–236. 6. Lynch JJ, Sitko GR, Mellott MJ, Nutt EM, Lehman ED, Friedman PA, Dunwiddie CT, Vlasuk GP. Maintenance of canine coronary artery patency following thrombolysis with front loaded plus low dose maintenance conjunctive therapy. A comparison of factor Xa versus thrombin inhibition. Cardiovasc Res 1994; 28:78–85. 7. Hollenback S, Sinha U, Lin P-H, Needham K, Frey L, Hancock T, Wong A, Wolf D. A comparative study of prothrombinase and thrombin inhibitors in a novel rabbit model of non-occlusive deep vein thrombosis. Thromb Haemost 1994; 71:357–362. 8. Benedict CR, Ryan J, Todd J, Kuwabara K, Tijburg P, Cartwright Jr J, Stern D. Active site-blocked factor Xa prevents thrombus formation in the coronaryvasculature in parallel with inhibition of extravascular coagulation in a canine thrombosis model. Blood 1993; 81:2059–2066. 9. Schaffer LW, Davidson JT, Vlasuk GP, and Siegl PKS. Antithrombotic efficacy of recombinant tick anticoagulant peptide. A potent inhibitor of coagulation factor Xa in a primate model of arterial thrombosis. Circulation 1991; 84:1741– 1748. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_290.html (1 of 2) [4/5/2004 5:16:10 PM]
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Document Table 1 Approval Indicatio
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Document Cyclotheonamide A (CtA), 2
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Document D ddI, 152 tumour necrosis
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Document antistasin peptides, 281 c
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Document fragment-based programs, 5
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Document [Human immunodeficiency vi
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Document Kininogen, 119 high molecu
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Document RT inhibitor, 41, 56 Nonpe
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Document Phosphoglycerate kinase (P
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Document [Protease targets] serinyl
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