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Document 27. Tsuda Y, Cygler M, Gibbs BF, Pedyczak A, Fethiere J, Yue SY, Konishi Y. Design of potent bivalent thrombin inhibitors based on hirudin sequence: incorporation of nonsubstrate-type active site inhibitors. Biochemistry 1994; 33:14443–14451. 28. Rehse PH, Steinmetzer T, Li Y, Konishi Y, Cygler M. Crystal structure of a peptidyl pyridinium methyl ketone inhibitor with thrombin. Biochemistry 1995; 34:11537–11544. 29. Gibbs CS, Coutre SE, Tsiang M, Li WX, Jain AK, Dunn KE, Law VS, Tao CT, Matsumura SY, Mejza SJ, Paborsky LR, Leung LLK. Conversion of thrombin into an anticoagulant by protein engineering. Nature 1995; 378:413–416. 30. Greer J. Comparative model-building of the mammalian serine proteinases. J Mol Biol 1981; 153:1027–1042. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_263.html (2 of 2) [4/5/2004 5:11:39 PM]
Document 31. Kettner C, Shaw E. D-PHE-PRO-ARGCH 2Cl-1 selective affinity label for thrombin. Thrombosis Research 1979; 14:969–973. Page 264 32. Brandstetter H, Turk D, Hoeffken W, Grosse D, Sturzebecher J, Martin PD, Edwards BFP, Bode W. X-ray crystal structure of thrombin complexes with the benzamidine- and arginine-base inhibitors NAPAP, 4-TAPAP and MQPA: a starting point for elaborating improved antithrombotics. J Mol Biol 1992; 226:1085–1099. 33. Martin PD, Robertson W, Turke D, Bode W, Edwards BFP. The structure of residues 7–16 of the Aα-chain of human fibrinogen bound to bovine thrombin at 2.3 Å resolution. J Biol Chem 1992; 267:7911–7920. 34. Arni RK, Padmanabhan K, Padmanabhan KP, Wu TP, Tulinsky A. The structure of the non-covalent complex of prothrombin kringle 2 with PPACK-thrombin. Chem Phys Lipids; 1994; 67–68:59–66. 35. Stone SR, Hofsteenge J. Kinetics of the inhibition of thrombin by hirudin. Biochemistry 1986; 25:4622–4628. 36. Witting JI, Bourdon P, Maraganore JM, Fenton JW II. Hirulog-1 and -B2 thrombin specificity. Biochem J 1992; 287:663–664. 37. Bourdon P, Jablonski J, Chao BH, Maraganore JM. Structure-function relationships of hirulog peptide interactions with thrombin. FEBS 1991; 294:163–166. 38. Szewczuk Z, Gibbs BF, Yue SY, Purisima E, Zdanvo A, Cygler M, Konishi Y. Design of a linker for trivalent thrombin inhibitors: interaction of the main chain of the linker with thrombin. Biochemistry 1993; 32:3396–3404. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_264.html [4/5/2004 5:11:41 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 dine (3TC), and 2',3'-dide
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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 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 125 binding site on t
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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 39. Mavunkel BJ, Lu Z, Kyl
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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 Page 176 0.43 Å) as the c
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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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Page 363 and 364: Document 12 Polypeptide Modulators
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Document 17. Szelke M. Chemistry of
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Document Page 359 easily reach the
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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 Figure 13 The identified p
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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 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 33. Szente BE, Johnson HM.
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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 Figure 10 Possible hydroge
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Document conformational transition
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Document Page 518 The differences b
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Document Page 545 protein binding s
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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 Page 603 hydroxymethyl sub
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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 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 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 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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