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Document 10. Vlasuk GP. Structural and functional characterization of tick anticoagulant peptide (TAP): a potent and selective inhibitor of blood coagulation factor Xa. Thrombosis and Haemostasis 1993; 70:212–216. 11. Scarborough RM. Anticoagulant strategies targeting thrombin and factor Xa. Ann Reports Med Chem 1995; 30:71–80. 12. Wallis RB. Inhibitors of coagulation factor Xa: from macromolecular beginnings to small molecules. Current Opinion in Therapeutic Patents Aug, 1993. 13. Waxman L, Smith DE, Arcuri KE, Vlasuk GP. Tick anticoagulant peptide (TAP) is a novel inhibitor of blood coagulation factor Xa, Science 1990; 248:593. 14. Hauptmann J, Kaiser B, Vowak G, Struzebecher J, Markwardt F. Comparison of the anticoagulant and antithrombotic effects of synthetic thrombin and factor Xa inhibitors. Throm Haemostas 1990; 63:220–223. 15. Jacobs JW, Cupp EW, Sardana M, Friedman PA. Isolation and characterization of a coagulation factor Xa inhibitor from black fly salivary glands. Thromb Haemost (GERMANY) 1990; 64:235–238. 16. Taylor Jr FB, Chang ACK, Peer GT, Mather T, Blick K, Catlett R, Lockhart MS, Esmon CT Blood 1991; 78:364. 17. Sinha U, Hancock T, Lin P-H, Hollenback S, Wolf D. Expression, purification, and characterization of inactive human coagulation factor Xa (Asn322Ala419). Protein Expr Purif 1992;3:518–524. 18. Dunwiddie CT, Waxman L, Vlasuk GP, Friedman PA. Purification and characterization of inhibitors of blood coagulation factor Xa from hematophagous organisms. Methods in Enzymol 1993; 233:291–312. 19. Stanssens P, Bergum PW, Gansemans Y, Jespers L, LaRoche Y, Huang S, Maki S, Messeno J, Lauwereys M, Cappello M, Hotez PJ, Lasters I, Vlasuk GP. Anticoagulant repertoire of the hookworm ancyclostoma caninum. Proc Natl Acad Sci 1996; 93:2149–2154. 20. Nesheim ME, Kettner C, Shaw E, Mann KG. Cofactor dependence of factor Xa incorporation into the prothrombinase complex. J Biol Chem 1981; 256:6537– 6540. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_290.html (2 of 2) [4/5/2004 5:16:10 PM]
Document Page 291 21. Davie EW, Fujikawa K, Kisiel W. The coagulation cascade: interaction, maintenance, and regulation. Biochemistry 1991; 30:10363–10370. 22. Leytus SP, Foster DC, Kurachi K, Davie EW. Gene for human factor X: a blood coagulation factor whose gene organization is Essentially identical with that of factor IX and protein C. Biochemistry 1986; 25:5098–5102. 23. Fung MR, Hay CW, MacGillivray RTA. Characterization of an almost full length cDNA coding for human blood coagulation Factor X. Proc Nat Acad Sci USA 1985; 82:3591–3595. 24. Blanchard RA, Faye KLM, Barrett JM, William B. Isolation and characterization of profactor X from the liver of a steer treated with sodium warfarin. Blood 1985; 66(suppl.1):331a. 25. Vlasuk GP, Ramjit D, Fujita T, Dumwiddie CT, Nutt EM, Smith DE, Shebuski RJ. Comparison of the in vivo anticoagulant properties of standard heparin and the highly selective factor Xa inhibitors antistasin and tick anticoagulant peptide (TAP) in a rabbit model of venous thrombosis. Thromb Haemostas 1991; 65:257– 262. 26. Sitko GR, Ramjit DR, Stabilito II, Lehman D, Lynch JJ, Vlasuk GP. Conjunctive enhancement of enzymatic thrombolysis and prevention of thrombotic reocclusion with the selective factor Xa inhibitor, tick anticoagulant peptide. Comparison to hirudin and heparin in a canine model of acute coronary artery thrombosis. Circulation 1992; 85:805–815. 27. Mellot MJ, Strainieri MT, Sitko GR, Stabilito II, Lynch JJ, Vlasuk GP. Enhancement of recombinant tissue plasminogen activator-induced reperfusion <strong>by</strong> recombinant tick anticoagulant peptide, a selective factor Xa inhibitor, in a canine model of femoral arterial thrombosis. Fibrinolysis 1993; 7:195–202. 28. Mellot JJ, Holahan MA, Lynch JJ, Vlasuk GP, Dunwiddie CT. Acceleration of recombinant tissuetype plasminogen activator-induced reperfusion and prevention of reocclusion <strong>by</strong> recombinant antistasin, a selective factor Xa inhibitor, in a canine model of femoral arterial thrombosis. Circ Res 1992; 70:1152–1160. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_291.html (1 of 2) [4/5/2004 5:16:13 PM]
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Structure-based Drug Design 14 Stru
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Document Page 56 It is also attract
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Document Table 3 HIV-1 RT Amino Aci
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Document Page 61 now clear that the
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Document Page 63 most of the amino
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Document Page 65 cal properties of
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Document dine) and didanosine (dide
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Document 163. Lacey SF, Larder BA.
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Document Page 106 on the same ring
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Document Page 108 mulate during tre
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Document 44. Cushman M, Sherman P.
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Document 65. Gallay P, Swingler S,
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Document 4 Bradykinin Receptor Anta
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Document Page 123 were poorly satis
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Document Page 125 binding site on t
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Document Page 127 The des-Arg 9 for
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Document Page 129 tolerated by the
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Document receptor, it has not yet b
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Document Page 133 This initial stag
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Document Page 135 might be jointly
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Document Page 137 observed for the
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Document Figure 6 Rat and human B2
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Document Page 141 receptor with int
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Document Figure 9 Composition of te
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Document B. Pharmacology Figure 1 T
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Document We determined the structur
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Document Figure 3 Previously known
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Document large solvent channels and
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Document IV. Drug Design Progressio
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Document position eight from formin
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Document Table 1 Inhibition Data fo
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Document Page 166 As predicated, th
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Document References 1. Parks RE Jr.
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Document 17. Ealick SE, Rule SA, Ca
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Document 6 Structural Implications
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Document Figure 1 A ribbon model of
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Document Page 176 0.43 Å) as the c
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Document Page 178 studies show that
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Document Figure 5 (a) A cut away vi
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Document Figure 6 (a) The pocket of
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Document Figure 1 Reactions catalyz
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Document Important for the validity
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Document Figure 4 Amino acids impor
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Document III. Results and Discussio
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Document Figure 6 Structure of α h
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Document Page 205 enzyme and of phe
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Document protein kinase core is ess
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Document 9 Structural Studies of Al
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Document diverse ARIs have been sho
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Document Figure 3 C α trace of the
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Document 18. Wilson DK, Tarle I, Pe
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Document 35. Pailhoux EA, Martinez
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Page 311 and 312: Document Cyclotheonamide A (CtA), a
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Page 335 and 336: Document Lys in the P1 position is
Page 337 and 338: Document Page 276 In both cases the
Page 339 and 340: Document Page 278 The n=3 chain len
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Page 343 and 344: Document Figure 11 dArg-ATS 32-38 m
Page 345 and 346: Document Figure 12 Modeled fit of S
Page 347 and 348: Document Page 285 number of x-ray s
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Page 363 and 364: Document 12 Polypeptide Modulators
Page 365 and 366: Document Page 297 whereas, calcium
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Page 369 and 370: Document Page 301 domains contribut
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Page 373 and 374: Document A. Chemical Modification P
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Page 383 and 384: Document Page 314 anemone toxins an
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Page 395 and 396: Document 13 Rational Design of Reni
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Document C. Specificity Figure 4 Th
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Document Figure 5 The S 3 specifici
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Document IV. Rational Drug Design F
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Document 2. Blundell TL, Cooper J,
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Document 17. Szelke M. Chemistry of
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Document 34. Rosenberg SH, Plattner
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Document Figure 8 The catalytic mac
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Document Figure 10 Structures of so
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Document Figure 14 The energy profi
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Document Page 359 easily reach the
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Document Figure 1 Available drugs f
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Document Table 1 Trypanosomal Targe
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Document Table 2 Three-Dimensional
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Document Figure 2 Glycolysis in blo
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Document II. Three Glycolytic Enzym
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Document Figure 4 Stereoview of sup
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Document Figure 6 Stereoview of NAD
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Document 5-Methoxytryptamine 19.0 9
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Document Figure 12 Predicted bindin
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Document Page 388 nosine proved to
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Document 15. Carter NS, Fairlamb AH
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Document 30. Kim H, Feil I, Verlind
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Document 65. João HC, Williams RJP
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Document 84. Verlinde CLMJ, Hol WGJ
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Document 16 Progress in the Design
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Document Table 1 Known Three-Dimens
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Document Page 398 with growth hormo
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Document All effects of the IL-1 fa
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Document Figure 2 Structural alignm
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Document Page 405 strands constitut
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Document Figure 4 (a) Stereo diagra
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Document Figure 6 (a) Stereo diagra
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Document Figure 7 (a) Superposition
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Document Page 412 ture is unlike ot
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Document Page 416 positions of the
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Document Figure 11 Functional resid
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Document Figure 13 The identified p
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Document B. Interleukin-1 Receptor
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Document Page 423 American Home Pro
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Document Page 425 Antinflammatory D
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Document Page 427 These aromatic di
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Document 5. Dinarello CA. On the Bi
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Document 21. Seckinger P, Lowenthal
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Document 39. Saurat JH, Schfferli J
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Document receptor antagonist into a
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Document 74. Bender PE, Lee JC., ed
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Document 102. Machin PJ, Osbond JM,
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Document 17 Structure and Functiona
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Document Table 1 Approval Indicatio
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Document Page 438 proteins. One pot
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Document II. Type IFNs A great deal
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Document Page 441 sequence of the m
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Document Page 443 that allowed for
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Document Figure 4 Stereo view of IF
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Document Figure 5 Velcro-key model
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Document Figure 6 Proposed receptor
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Document Page 451 with the cytoplas
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Document for directed subcellular t
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Document Figure 1 A schematic diagr
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Document Page 462 strains of influe
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Document Figure 3 (a) A MOLSCRIPT [
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Document B. Protein Structure Page
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Document Figure 5 (a) Stereo image
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Document Page 471 molecules in the
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Document hydroxy, and 6 Neu5Ac2en -
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Document Figure 8 Stereo image of t
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Document Page 476 nM, respectively.
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Document Page 478 lished—was asso
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Document VI. Conclusion Page 480 It
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Document 21. Both GW, Sleigh MJ, Co
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Document 40. Drzenick R, Frank H, R
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Document 45. Varghese JN, Laver WG,
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Document 80. Suzuki Y, Sato K, Kiso
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Document Page 488 against most of t
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Document A. The Canyon Page 491 The
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Document Subsequent studies have sh
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Document Page 495 of the RNA and pr
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Document Figure 4 A ribbon diagram
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Document Figure 5 Some compounds wh
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Document Figure 7 HRV14 VP1 hydroph
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Document C. Structure-Activity Rela
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Document B. Peptidomimetic Drugs: C
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Document Acknowledgments Page 620 I
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Document 18. Sawyer TK. In: Peptide
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Document Med Biol 1991; 306:9-21; (
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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 [Human immunodeficiency vi
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Document Kininogen, 119 high molecu
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