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Document KD eds. Peptides: Structure and Function. Rockford:Pierce Chemical Company, 1985:759–762. 22. Rich DH, Sun ETO, Ulm E. Synthesis of analogues of the carboxyl proteinase inhibitor pepstatin. Effect of structure on the inhibition of pepsin and renin. J Med Chem 1980; 23:27–33. Page 340 23. Sali A, Veerapandian B, Cooper JB, Founding SI, Hoover DJ, Blundell TL. High resolution X-ray diffraction study of the complex between endothiapepsin and an oligopeptide inhibitor: the analysis of inhibitor binding and description of the rigid body shifts in the enzyme. EMBO J 1989; 8:2179–2188. 24. Iizuka K, Kamijo T, Kubota T, Akahane K, Umeyama H, Kiso Y. New human renin inhibitors containing an unnatural amino acid, norstatine. J Med Chem 1988; 31:701–704. 25. Dann JG, Stammers DK, Harris, CJ, Arrowsmith RJ, Davies DE, Hardy GW, Morton JA. Human renin: an new class of inhibitors. Biochem Biophys Res Commun 1986; 134:71–77. 26. Cooper JB, Foundling SI, Blundell TL, Arrowsmith RJ, Harris CJ, Champness JN. A rational approach to the design of antihypertensives: X-ray studies of complexes between aspartic proteinases and aminoalcohol inhibitors. In: Leeming PR, ed. Topics in Medicinal Chemistry. London: Royal Society of Chemistry, 1988; 308–313. 27. Lunney EA, Hamilton HW, Hodges JC, Kaltenbrohn JS, Repine JT, Badasso M, Cooper J, Dealwis C, Wallace B, Lowther WT, Dunn BM, Humblet C. Analyses of ligand binding in five endothiapepsin crystal complexes and their use in the design and evaluation of novel renin inhibitors. J Med Chem 1993; 36:3809–3820. 28. Bartlett PA, Kezer WB. Phosphinic acid dipeptide analogues: potent, slowbinding inhibitors of aspartic proteinases. J Amer Chem Soc 1984; 106:4282–4283. 29. Greenlee WJ. Renin inhibitors. Pharm Res 1987; 4(5):364–374. 30. Thaisrivongs S, Pals DT, Harris DW, Kati WM, Turner SR. Design and synthesis of potent and specific renin inhibitors containing difluorostatine, difluorostatone and related analogues. J Med Chem 1986; 29:2088–2093. 31. Veerapandian B, Cooper JB, Sali A, Blundell TL. Direct observation by X-ray analysis of the tetrahedral “intermediate” of aspartic proteinases. Protein Science 1992; 1:322–328. 32. Suguna K, Padlan EA, Smith CW, Carlson WD, Davies DR. Binding of a reduced peptide inhibitor to the aspartic proteinase from Rhizopus chinensis: implications for a mechanism of action. Proc Natl Acad Sci USA 1987; 84:7009–7013. 33. Ptitsyn OB. Pure Appl Chem 1973; 31:227–244. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_340.html (1 of 2) [4/5/2004 5:27:15 PM]
Document 34. Rosenberg SH, Plattner JJ, Woods KW, Stein HH, Marcotte PA, Cohen J, Perun TJ. Novel renin inhibitors containing analogues of statine retro-inverted at the C-termini: specificity of the P 2 histidine site. J Med Chem 1987; 30:1224–1228. 35. Luly JR, Yi N, Soderquist J, Stein H, Cohen J, Perun TJ, Plattner JJ. New inhibitors of human renin that contain novel Leu-Val replacements. J Med Chem 1987; 30:1609–1616. 36. Cooper J, Quail W, Frazao C, Foundling SI, Blundell TL. X-ray crystallographic analysis of inhibition of endothiapepsin by cyclohexyl renin inhibitors. Biochemistry 1992; 31:8142–8150. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_340.html (2 of 2) [4/5/2004 5:27:15 PM]
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Structure-based Drug Design 14 Stru
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Document 74. Reddy RM, Varney MD, K
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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 Page 56 It is also attract
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Document Table 3 HIV-1 RT Amino Aci
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Document 106. Cirino NM, Cameron CE
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Document 122. Marshall WS, Beaton G
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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 when metals are bound. Fin
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Document cubation of phosphotyrosin
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Document Page 141 receptor with int
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Document We determined the structur
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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 References 1. Parks RE Jr.
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Document 6 Structural Implications
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Document Figure 4 Amino acids impor
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Document Page 202 269, and valine-2
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Page 395 and 396: Document 13 Rational Design of Reni
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Page 421 and 422: Document Page 343 14 Structural Asp
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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 5. Dinarello CA. On the Bi
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Document 39. Saurat JH, Schfferli J
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Document 74. Bender PE, Lee JC., ed
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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 Page 462 strains of influe
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Document Figure 3 (a) A MOLSCRIPT [
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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 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 Acknowledgments Page 620 I
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Document 18. Sawyer TK. In: Peptide
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Document MA, Welch KM, Hallak H, Ta
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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 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 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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