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Document 12. Tantillo C, Ding J, Jacobo-Molina A, Nanni RG, Boyer PL, Hughes SH, et al. Locations of anti- AIDS drug binding sites and resistance mutations in the three-dimensional structure of HIV-1 reverse transcriptase: implications for mechanisms of drug inhibition and resistance. J Mol Biol 1994; 243:369–387. 13. Miyasaka T, Tanaka H, Baba M, Hayakawa H, Walker RT, Balzarini J, et al. A novel lead for specific anti-HIV-1 agents: 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine. J Med Chem 1989; 32:2507–2509. 14. Pauwels R, Andries K, Desmyter J, Schols D, Kukla MJ, Breslin HJ, et al. Potent and selective inhibition of HIV-1 replication in vitro by a novel series of TIBO derivatives. Nature 1990; 343:470–474. 15. Merluzzi VJ, Hargrave KD, Labadia M, Grozinger K, Skoog M, Wu JC, et al. Inhibition of HIV-1 replication by a nonnucleoside reverse transcriptase inhibitor. Science 1990; 250:1411–1413. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_71.html (2 of 2) [4/5/2004 4:50:53 PM]
Document Page 72 16. Goldman ME, Nunberg JH, O'Brien JA, Quintero JC, Schleif WA, Freund KF, et al. Pyridinone derivatives: specific human immunodeficiency virus type 1 reverse transcriptase inhibitors with antiviral activity. Proc Natl Acad Sci USA 1991; 88:6863–6867. 17. Romero DL, Busso M, Tan C-K, Reusser F, Palmer JR, Poppe SM, et al. Nonnucleoside reverse transcriptase inhibitors that potently and specifically block human immunodeficiency virus type 1 replication. Proc Natl Acad Sci USA 1991; 88:8806–8810. 18. Chimirri A, Grasso S, Monforte A-M, Monforte P, Zappala M. Anti-HIV agents. I. Synthesis and in vitro anti-HIV evaluation of novel 1H,3H-thiazolo[3,4-a]benzimidazoles. Farmaco 1991; 46:817–823. 19. Chimirri A, Grasso S, Monforte A-M, Monforte P, Zappala M. Anti-HIV agents. II. Synthesis and in vitro anti-HIV activity of novel 1H3H-thiazolo[3,4-a]benzimidazoles. Farmaco 1991; 46:925–933. 20. Balzarini J, Perez-Perez M-J, San-Felix A, Schols D, Perno C–F, Vandamme A–M, et al. 2',5'-bis-O- (tert-butyldimethylsilyl)-3'-spiro-5''-(4''-amino-1",2"-oxathiole-2",2"-dioxide)pyrimidine (TSAO) nucleoside analogues: highly selective inhibitors of human immunodeficiency virus type 1 that are targeted at the viral reverse transcriptase. Proc Natl Acad Sci USA 1992; 89:4392–4396. 21. Pauwels R, Andries K, Debyser Z, Van Dable P, Schols D, Stoffels P, et al. Potent and highly selective human immunodeficiency virus type 1 (HIV-1) inhibition by a series of αanilinophenylacetamide derivatives targeted at HIV-1 reverse transcriptase. Proc Natl Acad Sci USA 1993; 90:1711–1715. 22. Kleim J–P, Bender R, Billhardt U-M, Meichsner C, Riess G, Roesner M, et al. Activity of a novel quinoxaline derivative against human immunodeficiency virus type 1 reverse transcriptase and viral replication. Antimicrob Agents Chemother 1993; 37:1659–1664. 23. Kleim J-P, Roesner M, Winkler I, Paessens A, Kirsch R, Hsiou Y, et al. Selective pressure of a quinoxaline class nonnucleoside inhibitor of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase (RT) on HIV-1 replication results in the emergence of nucleoside RT inhibitor specific (RT L74->V/I, V75->L/I) HIV-1 mutants. Proc Natl Acad Sci USA 1996; 93:34–38. 24. Nunberg JH, Schleif WA, Boots EJ, O'Brien JA, Quintero JC, Hoffman JM, et al. Viral resistance to human immunodeficiency virus type 1-specific pyridinone reverse transcriptase inhibitors. J Virol 1991; 65:4887–4892. 25. Mellors JW, Dutschman GE, Im G-J, Tramontano E, Winkler SR, Cheng Y-C. Rapid emergence of HIV-1 resistant to non-nucleoside inhibitors of reverse transcriptase. Antiviral Research 1992; 17 S1:48. 26. Larder BA. Interactions between drug resistance mutations in human immunodeficiency virus type 1 reverse transcriptase. J Gen Virol 1994; 75:951–957. http://legacy.netlibrary.com/nlreader/nlReader.dll?bookid=12640&filename=Page_72.html (1 of 2) [4/5/2004 4:50:55 PM]
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Structure-based Drug Design 14 Stru
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Page 103 and 104: Document dine) and didanosine (dide
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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 B. Protein Structure Page
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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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