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Document 50. Broze Jr GJ. Trends Cardiovasc Med 1994; 2:72. 51. Hofmann KJ, Nutt EM, Dunwiddie CT. Site-directed mutagenesis of the leechderived factor Xa inhibitor antistasin. Biochem J 1992; 287:943. 52. Schreuder H, Arkema A, deBoer B, Kalk K, Dijkema R, Mulders J, Theunissen H, Hol W. Crystallization and preliminary crystallographic analysis of antistasin, a leech-derived inhibitor of blood coagulation factor Xa. J Mol Biol 1993; 231:1137–1138. 53. Broze Jr GJ, Warren LA, Novotny WF, Huguchi DA, Girard JJ, Miletich JP. The lipoproteinassociated coagulation inhibitor that inhibits the factor VII-tissue factor complex also inhibits factor Xa: insight into its possible mechanism of action. Blood 1984; 71:335–343. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_292.html (2 of 2) [4/5/2004 5:16:15 PM]
Document 54. Broze Jr GJ, Girard TJ, Novotny WF. Regulation of coagulation by a multivalent Kunitz-type inhibitor. Biochemistry 1990; 29:7539. Page 293 55. Dunwiddie CT, Vlasuk GP, Nutt EM. The hydrolysis and resynthesis of a single reactive site peptide bond in recombinant antistasin by coagulation factor Xa. Arch Biochem Biophys 1992; 294:647–653. 56. Dunwiddie CT, Neeper MP, Nutt EM, Waxman L, Smith DE, Hoffman KJ, Lumma PK, Garsky VM, Vlasuk GP. Site-directed analysis of the functional domains in the factor Xa inhibitor tick anticoagulant peptide: identification of two distinct regions that constitute the enzyme recognition sites. Biochemistry 1992; 31:12126–12131. 57. Lim-Wilby MSL, Hallenga K, DeMaeyer M, Lasters I, Vlasuk GP, Brunck TK. NMR structure determination of tick anticoagulant peptide (TAP). Protein Sci 1995; 4:178–186. 58. Antuch W, Guntert P, Billeter M, Hawthorne T, Grossenbacher H, Wuthrich K. NMR solution structure of the recombinant tick anticoagulant protein (rTAP), a factor Xa inhibitor from the tick ornithodoros moubata. FEBS Lett 1994; 325:251–257. 59. Rydel TJ, Tulinsky A, Bode W, Huber R. Refined structure of the hirudin-thrombin complex. J Mol Biol 1991;221:583–601. 60. Katakura S-I, Nagahara T, Hara T, Iwamoto M. A novel Factor Xa inhibitor: structure-activity relationships and selectivity between Factor Xa and thrombin. Biochem Biophys Res Comm 1993; 197:965–972. 61. Hara T, Yokoyama A, Ishihara H, Yokoyama Y, Nagahara T, Iwamoto M. DX- 9065a, a new synthetic, potent anticoagulant and selective inhibitor for Factor Xa. Thrombosis and Haemostasis 1994; 71:314–319. 62. Nagahara T, Yokoyama Y, Inamura K, Katakura S-I, Komoriya S, Yamaguchi H, Hara T, Iwamoto M. J Med Chem 1994; 37:1200–1207. 63. Nagahara T, Kanaya N, Inamura K, Yokoyama Y. Aromatic amidine derivatives and salts thereof. Eur Pat App 0-540-051-A1. 64. Lin Z, Johnson ME. Proposed cation-π mediated binding by Factor Xa: a novel enzymatic mechanism for molecular recognition. FEBS Lett 1995; 370:1–5. 65. Banner DW, Hadvary P. Crystallographic analysis of 3.0 Å resolution of the binding to human thrombin of four active-site directed inhibitors. J Biol Chem 1991; 266:20085–20093. 66. Dougherty DA. Cation-π interactions in chemistry and biology: a new view of benzene, Phe, Tyr, and Trp. Science 1996; 271:163–167. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_293.html (1 of 2) [4/5/2004 5:17:35 PM]
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Structure-based Drug Design 14 Stru
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Document 163. Lacey SF, Larder BA.
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Document Page 137 observed for the
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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 Page 176 0.43 Å) as the c
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Page 363 and 364: Document 12 Polypeptide Modulators
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Document 16 Progress in the Design
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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 Page 425 Antinflammatory D
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Document 39. Saurat JH, Schfferli J
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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 13. Stewart HJ, McCann SHE
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Document 33. Szente BE, Johnson HM.
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Document Page 462 strains of influe
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Document Page 464 could not again b
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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 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 64. Ward CW, Elleman TC, A
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Document 80. Suzuki Y, Sato K, Kiso
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Document Page 486 95. Ryan DM, Tice
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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 Page 555 N-acylpyrrolidine
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Document 30. O'Shea EK, Rutkowski R
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Document Acknowledgments Page 620 I
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Document 18. Sawyer TK. In: Peptide
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Document 97; (e) Fujii I, Nakamura
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Document Med Biol 1991; 306:9-21; (
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Document Page 629 ML, Clare M, Decr
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Document Page 630 177. (a) Bode W,
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Document Page 631 197. Musil D, Zuc
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Document son AH, Drummond AH, Huxle
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Document site, 52, 55, 61 triad, 24
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Document factors, 247 Combination t
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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 overview, 103-104, 108-109
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Document [Inhibitors] 2-((3,4-dihyd
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Document antagonistic activity, 416
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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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