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Document 29. Neeper MP, Waxman L, Smith DE, Schulman CA, Sardana M, Ellis RE, Schaffer LW, Siegel PKS, Valsuk GP. Characterization of recombinant tick anticoagulant peptide. A highly selective inhibitor of blood coagulation factor Xa. J Biol Chem 1990; 265:17746–17752. 30. Dunwiddie CT, Nutt EM, Vlasuk GP, Siegel PDS, Schaffer LW. Anticoagulant efficacy and immunogenicity of the selective factor Xa inhibitor antistasin following subcutaneous administration in the rhesus monkey. Thromb Haemostas 1992; 67:371–376. 31. Schaffer LW, Davidson JT, Vlasuk GP, Dunwiddie CT, Siegel PKS. Selective factor Xa inhibition by recombinant antistasin prevents vascular graft thrombosis in baboons. Arteriosclerosis and Thromb 1992; 12:879–885. 32. Kelly AP, Hanson SR, Dunwiddie CT, Harker LA. Circulation 1992; 86:411. 33. Suttie JW. Vitamin K-dependent carboxylase. Annu Rev Biochem 1985; 54:459– 477. 34. Fernlund P, Stenflo J. β-Hydroxy-aspartic acid in vitamin K-dependent proteins. J Biol Chem 1983; 258:12509–12512. 35. DiScipio RG, Hermodson MA, Davie EW. Activation of human factor X (Stuart factor) by a protease from Russell's viper venom. Biochemistry 1977; 16:5253– 5260. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_291.html (2 of 2) [4/5/2004 5:16:13 PM]
Document 36. Leytus SP, Chung DW, Kisiel W, Kurachi K, Davie EW. Characterization of a cDNA coding for human factor X. Proc Nat Acad Sci USA 1984; 81:3699–3702. Page 292 37. Skogen WF, Esmon CT, Cox AC. Comparison of coagulation factor Xa and des(1–44) factor Xa in the assembly of prothrombinase. J Biol Chem 1984; 259:2306–2310. 38. Hertzberg MS, Ben-Tal O, Furie BC. Construction, expression, and characterization of a chimera of Factor IX and Factor X: the role of the second epidermal growth factor domain and serine protease domain in factor Xa binding. J Biol Chem 1992; 267:14759–14766. 39. Sigler PB, Blow DM, Matthews BW, Henderson R. Structure of crystalline α- chymotrypsin. II. A preliminary report including a hypothesis for the activation mechanism. J Mol Biol 1968; 35:143–164. 40. Bode W, Turk D, Karshikov A. The refined 1.9 Å X-ray crystal structure of D- Phe-Pro-Arg chloromethylketone-inhibited human α-thrombin. Structure analysis, overall structure, electrostatic properties, detailed active site geometry, structure function relationships. Protein Sci 1992; 1:426–471. 41. Mann KG, Nesheim ME, Church WR, Haley P, Krishnaswamy S. Surface-dependent reactions of the vitamin K-dependent enzyme complexes. Blood 1990; 76:1– 16. 42. Girard TJ, Warren LA, Novotny WF, Likert KM, Brown SG, Miletich JP, Broze Jr GJ. Functional significance of the Kunitz-type inhibitory domains of lipoprotein- associated coagulation inhibitor. Nature 1989; 338:518–520. 43. Nutt E, Gasic T, Rodkey J, Gasic G, Jacobs J, Friedman P, Simpson E. The amino acid sequence of antistasin. J Biol Chem 1988; 263:10162–10167. 44. Lauwereys M, Stanssens P, Lambier AM, Messens J, Dempsey E, Vlasuk GP. Ecotin as a potent factor Xa inhibitor. Thromb Haemostasis 1993; 69:864. 45. Seymour JL, Lindquist RN, Dennis MA, Moffat B, Yansura D, Reilly D, Wessinger ME, Lazurus RA. Ecotin is a potent anticoagulant and reversible tightbinding inhibitor of factor Xa. Biochemistry 1994; 33:3949–3958. 46. McGrath ME, Gillmor SA, Fletterick RJ. Ecotin: lessons on survival in a proteasefilled world. Protein Sci 1995;4:141–148. 47. Laskowski M, Kato I. Protein inhibitors of proteinases. Annu Rev Biochem 1980; 49:593–626. 48. Schechter I, Berger A. On the size of the active site in proteases. I. Papain. Biochem Biophys Res Commun 1967; 27:157–162. 49. Peterson LC. Progress in vascular biology, haemostasis and thrombosis. Abstracts, 1992 Zimmerman Conference. San Diego, California, Feb. 27–29, 1993. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_292.html (1 of 2) [4/5/2004 5:16:15 PM]
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Structure-based Drug Design 14 Stru
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Document 2 Structural Studies of HI
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Document Analysis of various HIV-1
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Document Table 3 HIV-1 RT Amino Aci
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Document ever, once an NNRTI is bou
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Document Chris Tantillo. The work i
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Document Page 72 16. Goldman ME, Nu
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Document 45. Majumadar C, Abbotts J
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Document 106. Cirino NM, Cameron CE
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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 108 mulate during tre
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Document cubation of phosphotyrosin
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Document 4 Bradykinin Receptor Anta
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Document Page 121 Nearly all cells
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Document Page 123 were poorly satis
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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 Figure 6 Rat and human B2
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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 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 4 Amino acids impor
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Page 343 and 344: Document Figure 11 dArg-ATS 32-38 m
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Page 363 and 364: Document 12 Polypeptide Modulators
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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 Page 359 easily reach the
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Document 65. João HC, Williams RJP
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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 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 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 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 Figure 4 Stereo view of IF
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Document Figure 5 Velcro-key model
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Document B. Protein Structure Page
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Document Page 471 molecules in the
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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 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 Figure 4 A ribbon diagram
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Document D ddI, 152 tumour necrosis
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Document antistasin peptides, 281 c
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Document [Protease targets] serinyl
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