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Document 32. Carson M. Ribbon models of macromolecules. J. Mol. Graphics 1987; 5:103–106. 33. Connolly ML. The molecular surface package J. Mol. Graphics 1993; 11:139–141. 34. Li J, O'Hare MC, Skarzynski T, Lloyd LF, Curry VA, Clark IM, Bigg HF, Hazleman BL, Cawston TE, Blow DM. X-ray structure of a hydroxamate inhibitor complex of stromelysin catalytic domain and its comparison with members of the zinc metalloproteinase superfamily. Structure 1996; 4:375–386. 35. Grams F, Crimmin M, Hinnes L, Huxley P, Pieper M, Tschesche H, Bode W. Structure determination and analysis of human neutrophil collagenase complexed with a hydroxamate inhibitor. Biochemistry 1995; 34:14012–14020. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_188.html (2 of 2) [4/5/2004 5:04:49 PM]
Document Page 189 36. Bode W, Reinemer P, Huber R, Kleine T, Schnierer S, Tschesche H. The X-ray crystal structure of the catalytic domain of human neutrophil collagenase inhibited by a substrate analogue reveals the essentials for catalysis and specificity. EMBO J. 1994; 13:1263–1269. 37. Schwartz MA, Van Wart HE. In: Ellis GP, Luscombe DK, eds. Progress in Medicinal Chemistry, Vol. 29. London: Elsevier Publishers, 1992: Chapter 8. 38. Johnson WH, Roberts NA, Borkakoti N. J. Enzyme Inhibition 1987; 2:1–22. 39. Wahl RC, Dunlop RP, Morgan BA. In: Bristol JA, ed. Annual Reports in Medicinal Chemistry. New York: Academic Press, 1990: Chapter 19. 40. Henderson B, Docherty AJP, Beeley NRA. Drugs of the Future 1990; 15:495–408. 41. Wahl RC, Pulvino TA, Mathiowetz AM, Ghose AK, Johnson JS, Delecki D, Cook ER, Gainer JA, Gowravaram MR, Tomczuk BE. Hydroxamate inhibitors of human gelatinase B (92kDa). Biorg. and Med. Chem. Lett. 1995; 5:349–352. 42. Gowravaram MR, Tomzcuk BE, Johnson JS, Delecki D, Cook ER, Ghose AK, Mathiowetz AM, Spurlino JC, Rubin B, Smith DL, Pulvino T, Wahl RC. Inhibition of matrix metalloproteinases by hydroxamates containing heteroatom-based modifications of the P1' group. J. Med. Chem. 1995; 38:2570–2581. 43. Netzel-Arnett S, Fields G, Birkdal-Hansen H, Avan Wart HE. Sequence specificities of human fibroblast and neutrophil collagenases. J. Biol. Chem. 1991; 206:6747–7855. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_189.html [4/5/2004 5:04:50 PM]
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netLibrary - eBook Summary Universi
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Structure-based Drug Design 14 Stru
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Document Figure 2 Schematic represe
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Document Page 33 sustained in many
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Document 2 Structural Studies of HI
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Document Figure 1 (a) Chemical stru
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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 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 -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 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 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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Page 187 and 188: Document We determined the structur
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Page 195 and 196: Document large solvent channels and
Page 197 and 198: Document IV. Drug Design Progressio
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Page 201 and 202: Document Table 1 Inhibition Data fo
Page 203 and 204: Document Page 166 As predicated, th
Page 205 and 206: Document References 1. Parks RE Jr.
Page 207 and 208: Document 17. Ealick SE, Rule SA, Ca
Page 209 and 210: Document 6 Structural Implications
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Page 215 and 216: Document Page 176 0.43 Å) as the c
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Page 221 and 222: Document Page 182 (SAR) model. The
Page 223 and 224: Document IX. S2' Interactions Page
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Page 227 and 228: Document 5. Willenbrock F, Murphy G
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Page 233 and 234: Document 7 Structure—Function Rel
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Page 251 and 252: Document Page 205 enzyme and of phe
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Page 257 and 258: Document 29. Baker ME. Genealogy of
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Page 263 and 264: Document Page 214 viruses. Specific
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Page 267 and 268: Document Page 218 The catalytic loo
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Page 275 and 276: Document protein kinase core is ess
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Document 9 Structural Studies of Al
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Document 10 Structure-Based Design
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Document Cyclotheonamide A (CtA), a
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Document Page 256 The discovery pro
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Document balance its pro- and antic
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Document 31. Kettner C, Shaw E. D-P
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Document Table 2 Naturally Occurrin
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Document Table 3 Active Site Sequen
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Document Lys in the P1 position is
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Document Page 276 In both cases the
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Document Figure 11 dArg-ATS 32-38 m
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Document 12 Polypeptide Modulators
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Document A. Chemical Modification P
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Document Page 309 site 3 on the sod
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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 17. Szelke M. Chemistry of
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Document Page 343 14 Structural Asp
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Document Figure 8 The catalytic mac
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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 6 Stereoview of NAD
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Document Page 388 nosine proved to
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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 Page 405 strands constitut
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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 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 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 13. Stewart HJ, McCann SHE
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Document 33. Szente BE, Johnson HM.
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Document 47. Igarashi K, Garotta G,
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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 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 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 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 Hydrophobicity Requirement
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Document Figure 9 A solvent-accessi
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Document Figure 10 Possible hydroge
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Document Page 514 sis. Large number
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Document conformational transition
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Document Page 518 The differences b
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Document 20 The Integration of Stru
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Document Page 527 function. Iterati
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Document Figure 3 Generation of com
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Document Page 530 screen. For examp
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Document 21 Structure-Based Combina
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Document Page 545 protein binding s
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Document Page 555 N-acylpyrrolidine
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Document 10. Bobbyer DNA, Goodford
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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 1 Examples of nativ
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Document 12640-0567a.gif Figure 6 C
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Document Figure 22 Protease 3D stru
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Document Page 603 hydroxymethyl sub
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Document Page 617 Val (131) showed
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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 Page 622 Fukuroda T, Fukam
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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 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 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 [Interleukin-1] homology w
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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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