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Document 160. Gu Z, Gao Q, Li X, Parniak MA, Wainberg MA. Novel mutation in the human immunodeficiency virus type 1 reverse transcriptase gene that encodes cross-resistance to 2',3'-dideoxyinosine and 2',3'dideoxycytidine. J Virol 1992; 66:7128–7135. 161. Tisdale M, Kemp SD, Parry NR, Larder BA. Rapid in vitro selection of human immunodeficiency virus type 1 resistant to 3'-thiacytidine inhibitors due to a mutation in the YMDD region of reverse transcriptase. Proc Natl Acad Sci USA 1993; 90:5653–5656. 162. Larder BA, Coates KE, Kemp SD. Zidovudine-resistant human immunodeficiency virus selected <strong>by</strong> passage in cell culture. J Virol 1991; 65:5232–5236. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_81.html (2 of 2) [4/5/2004 4:53:26 PM]
Document 163. Lacey SF, Larder BA. A novel mutation (V75T) in the HIV-1 reverse transcriptase confers resistance to 2',3'-didehydro-2',3'-dideoxythymidine (D4T) in cell culture. Antimicrob Agents Chemother 1994; 38:1428–1432. 164. Byrnes VW, Sardana VV, Schleif WA, Condra JH, Waterbury JA, Wolfgang JA, et al. Comprehensive mutant enzyme and viral variant assessment of human immunodeficiency virus type 1 reverse transcriptase resistance to nonnucleoside inhibitors. Antimicrob Agents Chemother 1993; 37:1576–1579. Page 82 165. Vasudevachari MB, Battista C, Lane HC, Psallidopoulos MC, Zhao B, Cook J, et al. Prevention of the spread of HIV-1 infection with nonnucleoside reverse transcriptase inhibitors. Virology 1992; 190:269–277. 166. Balzarini J, Karlsson A, Perez-Perez M-J, Vrang L, Walbers J, Zhang H, et al. HIV-1-specific reverse transcriptase inhibitors show differential activity against mutant strains containing different amino acid substitutions in the reverse transcriptase. Virology 1993; 192:246–253. 167. Balzarini J, Velazquez S, San-Felix A, Karlsson A, Perez-Perez M-J, Camarasa M-J, et al. Human immunodeficiency virus type 1-specific [2',5'-bis-O-[tert-butyldimethylsilyl] - β - D - ribofuranosyl] -3' - spiro-5'' -(4'' -amino - 1",2" - oxathiole-2", 2'-dioxide)-purine analogues show a resistance spectrum that is different from that of the human immunodeficiency virus type-1-specific nonnucleoside analogues. Mol Pharmacol 1993; 43:109–114. 168. Bacolla A, Shih C-K, Rose JM, Piras G, Warren TC, Grygon CA, et al. Amino acid substitutions in HIV-1 reverse transcriptase with corresponding residues from HIV-2. J Biol Chem 1993; 268:16571–16577. 169. Demeter L, Resnick L, Nawaz T, Timpone JG Jr., Batts D, Reichman RC. Phenotypic and genotypic analysis of ateviridine (ATV) susceptibility of HIV-1 isolates obtained from patients receiving ATV monotherapy in a phase I clinical trial (ACTG 187): comparison to patients receiving combination therapy with ATV and zidovudine. In: Third Workshop on Viral Resistance. Gaithersburg, Maryland, 1993. 170. Tisdale M, Parry NR, Cousens D, St. Clair MH and Boone LR. Anti-HIV activity of (lS-4R)-4-[2amino-6-cyclopropylamino-9H-purin-9-yl]-2-cyclopentene-1-methanol (1592U89). In: Abstracts of the 34th Interscience Conference on Antimicrobial Agents and Chemotherapy. Orlando, Florida, 1994:92. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_82.html [4/5/2004 4:53:28 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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Page 63 and 64: Document monophosphate analogs whic
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Page 67 and 68: Document Page 54 Table 2) [12,54].
Page 69 and 70: Document Page 56 It is also attract
Page 71 and 72: Document Table 3 HIV-1 RT Amino Aci
Page 73 and 74: Document ever, once an NNRTI is bou
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Page 79 and 80: Document Page 65 cal properties of
Page 81 and 82: Document Page 67 Biochemical data s
Page 83 and 84: Document Page 69 determining the me
Page 85 and 86: Document Chris Tantillo. The work i
Page 87 and 88: Document Page 72 16. Goldman ME, Nu
Page 89 and 90: Document 30. Coffin JM. HIV populat
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Page 93 and 94: Document reverse transcriptase inhi
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Page 101 and 102: Document 122. Marshall WS, Beaton G
Page 103 and 104: Document dine) and didanosine (dide
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Page 109 and 110: Document Figure 1 Retroviral lifecy
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Page 113 and 114: Document Page 88 transfer (Figure 3
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Page 117 and 118: Document Page 92 The role of the N-
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Page 121 and 122: Document Page 96 region in the HIV-
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Page 127 and 128: Document Page 101 crystallized unde
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Page 133 and 134: Document Page 106 on the same ring
Page 135 and 136: Document Page 108 mulate during tre
Page 137 and 138: Document when metals are bound. Fin
Page 139 and 140: Document cubation of phosphotyrosin
Page 141 and 142: Document 4. Vink C, Plasterk RHA. T
Page 143 and 144: Document Page 115 21. Kulkosky J, J
Page 145 and 146: Document 44. Cushman M, Sherman P.
Page 147 and 148: Document 65. Gallay P, Swingler S,
Page 149 and 150: Document 4 Bradykinin Receptor Anta
Page 151 and 152: Document Page 121 Nearly all cells
Page 153 and 154: Document Page 123 were poorly satis
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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 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 39. Mavunkel BJ, Lu Z, Kyl
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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 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 7 Structure—Function Rel
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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 Page 207 sure and the acti
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Document 29. Baker ME. Genealogy of
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Document Page 214 viruses. Specific
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Document protein kinase core is ess
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Document 31. Kettner C, Shaw E. D-P
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Document 12 Polypeptide Modulators
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Document A. Chemical Modification P
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Document Page 323 been suggested th
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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 2. Blundell TL, Cooper J,
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Document 17. Szelke M. Chemistry of
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Document 34. Rosenberg SH, Plattner
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Document Page 359 easily reach the
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Document Table 1 Trypanosomal Targe
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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 4 (a) Stereo diagra
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Document Figure 6 (a) Stereo diagra
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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 423 American Home Pro
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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 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 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 conformational transition
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Document Page 518 The differences b
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Document 10. Mast EE, Harmon MW, Gr
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Document 25. Arnold E, Rossmann MG.
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Document 44. Argos P, Rossmann MG,
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Document Page 527 function. Iterati
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Document 17. Zuckermann RN, Martin
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Document 21 Structure-Based Combina
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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 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 Page 622 Fukuroda T, Fukam
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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 274. (a) Kavanaugh WM, Wil
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Document site, 52, 55, 61 triad, 24
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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 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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