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Document Page 341 37. Attwood MR, Hassall CH, Krohn A, Lawton G, Redshaw S. The design and synthesis of angiotensin converting enzyme inhibitor cilazapril and related bicyclic compounds. J Chem Soc Perkin 1986; I:1011–1019. 38. Szewczuk Z, Rebholz KL, Rich DH. Synthesis and biological activity of new conformationally restricted analogues of pepstatin. Int J Pept Res 1992; 40:233–242. 39. Wood JM, Fuhrer W, Buhlmayer P, Riniker B, Hofbauer KG. Protection groups increase the in vivo stability of a statine-containing renin inhibitor. In: Kostka V, ed. Aspartic Proteinases and Their Inhibitors. Berlin: Walter de Gruyter, 1985:463–466. 40. Bolis G, Fung AKL, Greer J, Kleinert HD, Marcotte PA, Perun TJ, Plattner JJ, Stein HH. Renin inhibitors. Dipeptide analogues of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond. J Med Chem 1987; 30:1729–1737. 41. Greenlee, WJ Renin inhibitors. Med Res Rev 1990; 10:173. 42. Dhanaraj V, Dealwis C, Frazao C, Badasso M, Sibanda BL, Tickle IJ, Cooper JB, Driessen HPC, Newman M, Aguilar C, Wood SP, Blundell TL, Hobart PM, Geoghegan KF, Ammirati MJ, Danley DE, O'Connor BA, Hoover DJ. X-ray analyses of peptide-inhibitor complexes define the structural basis of specificity for human and mouse renins. Nature 1992; 357:466–472. 43. Dealwis CG, Frazao C, Badasso M, Cooper JB, Tickle IJ, Driessen H, Blundell TL, Murakami K, Miyazaki H, Sueiras-Diaz J, Jones DM, Szelke M. X-ray analysis at 2.0 Å resolution of mouse submaxillary renin complexed with a decapeptide inhibitor CH-66, based on the 4–16 fragment of rat angiotensinogen. J Mol Biol 1994; 236:342–360. 44. Wlodawer A, Miller M, Jaskolski M, Sathyanarayana BK, Baldwin E, Weber IT, Selk LM, Clawson L, Schneider J, Kent S. Conserved folding in retroviral proteinases: crystal structure of synthetic HIV-1 proteinase. Science 1989; 245:616–621. 45. Lapatto R, Blundell TL, Hemmings A, Overington J, Wilderspin A, Wood SP, Merson JR, Whittle PJ, Danley DE, Geoghegan KF, Hawrylik SJ, Lee SE, Scheld KG, Hobart PM. X-ray analysis of HIV-1 proteinase at 2.7 Å resolution confirms structural homology among retroviral enzymes. Nature (Lond) 1989; 342:299–302. 46. Poe M, Wu JK, Lin TY, Hoogsteen K, Bull HG, Slater EE. Renin cleavage of a human-kidney renin substrate analogous to human angiotensinogen that is human renin specific and resistant to cathepsin D. Analyt Biochem 1984; 140:459–467. 47. Cumin F, Lenguyen D, Castro B, Menard J, Corvol P. Comparative enzymatic studies of human renin acting on pure natural or synthetic substrates. Biochim Biophys Acta 1987; 913:10–19. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_341.html (1 of 2) [4/5/2004 5:27:17 PM]
Document 48. Powers JC, Harley AD, Myers DV. Subsite specificity of porcine pepsin. In: Tang J, ed. Acid Proteases-Structure, Function and Biology. New York: Plenum Press, 1977:141–157. 49. Antonov VK. In: Tang J, ed. Acid Proteases-Structure, Function and Biology. New York: Plenum Press, 1977:179. 50. Skeggs LT, Lentz KE, Kahn JR, Hochstrasser H. Kinetics of the reaction of renin with nine synthetic peptide substrates. J. Exp Med 1968; 120:130–34. 51. Holzman TF, Chung CC, Edalji R, Egan DA, Martin M, Gubbins EJ. Krafft GA, Wang GT, Thomas AM, Rosenberg SH, Hutchins C. Characterisation of recombi- http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_341.html (2 of 2) [4/5/2004 5:27:17 PM]
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Structure-based Drug Design 14 Stru
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Document 8. Kaplan AH, Zack JA, Kni
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Document 47. Tummino PJ, Ferguson D
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Document 60. Condra JH, Schleif WA,
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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 dine (3TC), and 2',3'-dide
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Document Figure Continued Page 45 r
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Document monophosphate analogs whic
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Document Analysis of various HIV-1
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Document Page 54 Table 2) [12,54].
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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 ever, once an NNRTI is bou
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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 Page 67 Biochemical data s
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Document Page 69 determining the me
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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 30. Coffin JM. HIV populat
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Document 45. Majumadar C, Abbotts J
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Document reverse transcriptase inhi
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Document 75. Ring CS, Sun E, McKerr
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Document 89. Hughes SH, Arnold E, H
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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 149. Craig JC, Duncan IB,
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Document 163. Lacey SF, Larder BA.
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Document Figure 1 Retroviral lifecy
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Document Figure 2 In vivo reactions
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Document Page 88 transfer (Figure 3
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Document Page 92 The role of the N-
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Document Figure 6 Molscript stereo
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Document Page 96 region in the HIV-
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Document day junction resolving enz
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Document -62° for HIV-1 integrase,
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Document Page 101 crystallized unde
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Document Figure 8 Molscript stereo
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Document proposed mechanisms. For e
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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 4. Vink C, Plasterk RHA. T
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Document Page 115 21. Kulkosky J, J
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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 121 Nearly all cells
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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 16. Martorana PA, Kettenba
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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 IX. S2' Interactions Page
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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 Page 202 269, and valine-2
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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 Cyclotheonamide A (CtA), a
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Document balance its pro- and antic
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Document Lys in the P1 position is
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Document Figure 11 dArg-ATS 32-38 m
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Page 395 and 396: Document 13 Rational Design of Reni
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Page 415 and 416: Document 17. Szelke M. Chemistry of
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Page 421 and 422: Document Page 343 14 Structural Asp
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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 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 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 21. Seckinger P, Lowenthal
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Document 39. Saurat JH, Schfferli J
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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 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 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 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 Figure 7 HRV14 VP1 hydroph
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Document C. Structure-Activity Rela
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Document accommodate a variety of d
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Document Figure 10 Possible hydroge
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Document Page 514 sis. Large number
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Document Page 530 screen. For examp
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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 22 Peptidomimetic and Nonp
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Document Figure 22 Protease 3D stru
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Document Figure 32 PTP and PTB 3D s
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Document Acknowledgments Page 620 I
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Document 18. Sawyer TK. In: Peptide
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Document 78. Rodriguez M, Crosby R,
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Document MA, Welch KM, Hallak H, Ta
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Document Page 626 SJ, Ogden RC, Red
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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 236. (a) Marshall MS. TIBS
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Document 274. (a) Kavanaugh WM, Wil
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Document inhibitor binding, 323, 33
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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 Matrix-metalloproteinase (
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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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