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Document Figure 9 Molecular modeling fit of compound 5 in the Factor Xa active site. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_279.html [4/5/2004 5:13:25 PM] Page 279
Document Figure 10 Proposed model of dansyl-Glu-Gly-Arg-chloromethyl ketone in Factor Xa [4,69]. Page 280 Tulinsky and coworkers [4] have proposed a model for the complex of dansyl-Glu-Gly-Argchloromethyl ketone using the thrombin-PPACK crystal structure as a template for the fit to Factor Xa (Figure 10). Using antistasin as a starting point, Ohta et al. [68] have synthesized a series of cyclic peptides <strong>based</strong> on the antistasin sequence. Three of these peptides are shown below and represent the most potent in the series. ATS29-47 NH2-Ser-Gly-Val-Arg-Cys * -Arg-Val-His-Cys * -Pro-His-Gly-Phe-Gln-Arg- Ser-Arg-Tyr-Gly-OH K i (FXa) 0.035 µM ATS29-40 NH2-Ser-Gly-Val-Arg-Cys * -Arg-Val-His-Cys * -Pro-His-Gly-OH 11.8 µM dR-ATS32-38 NH2-dArg-Cys-Arg-Val-His-Cys-Pro-OH 0.96 µM (The Cys * -Cys * are joined in disulfide bonds to form cyclic structures) http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_280.html (1 of 2) [4/5/2004 5:13:29 PM]
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Structure-based Drug Design 14 Stru
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Document Page 33 sustained in many
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Document 8. Kaplan AH, Zack JA, Kni
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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 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 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 63 most of the amino
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Document Page 67 Biochemical data s
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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 45. Majumadar C, Abbotts J
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Document reverse transcriptase inhi
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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 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 Bradykinin Receptor Anta
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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 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 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 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 Page 182 (SAR) model. The
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Document IX. S2' Interactions Page
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Document Figure 6 (a) The pocket of
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Document Figure 1 Reactions catalyz
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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 Page 205 enzyme and of phe
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Document protein kinase core is ess
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Document Figure 4 Surface represent
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Page 311 and 312: Document Cyclotheonamide A (CtA), a
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Page 323 and 324: Document 31. Kettner C, Shaw E. D-P
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Page 329 and 330: Document Table 2 Naturally Occurrin
Page 331 and 332: Document Table 3 Active Site Sequen
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Page 335 and 336: Document Lys in the P1 position is
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Page 345 and 346: Document Figure 12 Modeled fit of S
Page 347 and 348: Document Page 285 number of x-ray s
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Page 363 and 364: Document 12 Polypeptide Modulators
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Document Table 1 Approval Indicatio
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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 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 Phosphoglycerate kinase (P
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Document [Protease targets] serinyl
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