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An Historical Overview of Drug Discovery

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Ligand-Macromolecular Interactions in Drug Discovery

Part of the book series: Methods in Molecular Biology ((MIMB,volume 572))

Summary

Drug Discovery in modern times straddles three main periods. The first notable period can be traced to the nineteenth century where the basis of drug discovery relied on the serendipity of the medicinal chemists. The second period commenced around the early twentieth century when new drug structures were found, which contributed for a new era of antibiotics discovery. Based on these known structures, and with the development of powerful new techniques such as molecular modelling, combinatorial chemistry, and automated high-throughput screening, rapid advances occurred in drug discovery towards the end of the century. The period also was revolutionized by the emergence of recombinant DNA technology, where it became possible to develop potential drugs target candidates. With all the expansion of new technologies and the onset of the “Omics” revolution in the twenty-first century, the third period has kick-started with an increase in biopharmaceutical drugs approved by FDA/EMEA for therapeutic use.

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References

  1. Drews, J. (2000). Drug discovery: a historical perspective. Science 287, 1960–1964

    Article  PubMed  CAS  Google Scholar 

  2. Thomas, G. (2000). Medicinal Chemistry – An Introduction. Wiley, England

    Google Scholar 

  3. Chin, Y., Balunas, M.J., Chai, H.B., and Kinghorn, A.D. (2006). Drug discovery from natural sources.AAPS J 2, E239–E253

    Google Scholar 

  4. Zhang, M. and Wilkinson, B. (2007). Drug discovery beyond the “rule-of-five”. Curr Opin Biotechnol 18, 478–488

    Article  PubMed  CAS  Google Scholar 

  5. Lombardino, J.G. and Lowe, J.A. III. (2004). The role of the medicinal chemist in drug discovery – then and now. Nat Rev Drug Discov 3, 853–862

    Article  PubMed  CAS  Google Scholar 

  6. Niwayama, S. (2006). Proteomics in medicinal chemistry. Mini Rev Med Chem 6, 241–246

    Article  PubMed  CAS  Google Scholar 

  7. Sleno, L. and Emili, A. (2008). Proteomic methods for drug target discovery. Curr Opin Chem Biol 12, 1–9

    Article  Google Scholar 

  8. Ahn, N.G. and Wang, A.H.-J. (2008). Proteomics and genomics: perspectives on drug and target discovery. Curr Opin Chem Biol 12, 1–3

    Article  PubMed  CAS  Google Scholar 

  9. Veenstra, T.D. (2006). Proteomic approaches in the drug discovery. Drug Discov Today Tech 3, 193–195

    Article  Google Scholar 

  10. Kopec, K.K., Bozyczko-Coyne, D., and Williams, M. (2005). Target identification and validation in drug discovery: the role of proteomics. Biochem Pharmacol 69, 1133–1139

    Article  PubMed  CAS  Google Scholar 

  11. Katayama, H. and Oda, Y. (2007). Chemical proteomics for drug discovery based on compound-immobilized affinity chromatography. J Chromatogr B 855, 21–27

    Article  CAS  Google Scholar 

  12. Gershell, L.J. and Atkins, J.H. (2003). A brief history of novel drug discovery technologies. Nat Rev Drug Discov 2, 321–327

    Article  PubMed  CAS  Google Scholar 

  13. Gupta, P. and Lee, K.H. (2007). Genomics and proteomics in process development: opportunities and challenges. Trends Biotechnol 25, 324–330

    Article  PubMed  CAS  Google Scholar 

  14. Bleicher, K.H., Böhm, H., Müller, K., and Alanine, A.I. (2003). Hit and lead generation: beyond high-throughput screening. Nat Rev Drug Discov 2, 369–378

    Article  PubMed  CAS  Google Scholar 

  15. Kerns, E.H. and Di, L. (2003). Pharmaceutical profiling in drug discovery. Drug Discov Today 8, 316–323

    Article  PubMed  CAS  Google Scholar 

  16. Di, L. and Kerns, E.H. (2003). Profilling drug-like properties in discovery research. Curr Opin Chem Biol 7, 402–408

    Article  PubMed  CAS  Google Scholar 

  17. Yengi, L.G., Leung, L., and Kao, J. (2007). The evolving role of drug metabolism in drug discovery and development. Pharm Res 24, 842–858

    Article  PubMed  CAS  Google Scholar 

  18. Lipinski, C.A., Lombardo, F., Dominy, B.W., and Feeney, P.J. (2001). Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 46, 3–26

    Article  PubMed  CAS  Google Scholar 

  19. Han, S. and Kim, S.H. (2007). Introduction to chemical proteomics for drug discovery and development. Arch Pharm 340, 169–177

    Article  CAS  Google Scholar 

  20. Ryan, T.E. and Patterson, S.D. (2002). Proteomics in drug target discovery – high-throughput meets high-efficiency. Drug Discov World 3, 43–52

    Google Scholar 

  21. Edwards, A.M., Arrowsnith, C.H., Christendat, D., Dharams, A., Friesen, J.D., Greenblatt, J.F., and Vedadi, M. (2000). Protein production: feeding the crystallographers and NMR spectroscopists. Nat Struct Biol 7, 970–972

    Article  PubMed  CAS  Google Scholar 

  22. Schmid, M.B. (2002). Structural proteomics: the potential of high-throughput structure determination. Trends Microbiol 10, S27–S31

    Article  PubMed  CAS  Google Scholar 

  23. Jain, K. (2002). New routes for drug discovery. Drug Discov Today 7, 900–902

    Article  PubMed  Google Scholar 

  24. Newman, D.J., Cragg, G.M., and Snader, K.M. (2000). The influence of natural products upon drug discovery. Nat Prod Rep 17, 215–234

    Article  PubMed  CAS  Google Scholar 

  25. Balaram, P. (2004). Drug discovery: myth and reality. Curr Sci 87, 847–848

    Google Scholar 

  26. Triggle, D.J. (2007). Drug discovery and delivery in the 21st century. Med Princ Pract 16, 1–14

    Article  PubMed  Google Scholar 

  27. Kayser, O. and Müller, R.H. (2004). Pharmaceutical Biotechnology, Drug Discovery and Clinical Applications. Wiley, England

    Book  Google Scholar 

  28. Walsh, G. (2003). Biopharmaceuticals: Biochemistry and Biotechnology. Wiley, England

    Google Scholar 

  29. Dudzinski, D.M. and Kesselheim, S. (2008). Scientific and legal viability of follow-on protein drugs. N Engl J Med 358, 843–848

    Article  PubMed  CAS  Google Scholar 

  30. Hughes, B. (2008). 2007 FDA drug appro-vals: a year of flux. Nat Rev Drug Discov 7, 107–109

    Article  Google Scholar 

  31. Tucker, J., Yakatan, S., and Yakatan, S. (2008). Biogenerics 2007: how far have we come? J Commer Biotechnol 14, 56–64

    Article  Google Scholar 

  32. Lawrence, S. (2007). Billion dollar babies - biotech drugs as blockbusters. Nat Biotechnol 25, 380–382

    Article  PubMed  CAS  Google Scholar 

  33. Sartipy, P., Björquist, P., Strehl, R., and Hyllner, J. (2007). The application of human embryonic stem cell technologies to drug discovery. Drug Discov Today 12, 688–699

    Article  PubMed  CAS  Google Scholar 

  34. Friel, R., van der Sar, S., and Mee, P.J. (2005). Embryonic stem cells: understanding their history, cell biology and signalling. Adv Drug Deliv Rev 57, 1894–1903

    Article  PubMed  CAS  Google Scholar 

  35. Keller, G. (2005). Embryonic stem cell differentiation: emergence of a new era in biology and medicine. Genes Dev 19, 1129–1155

    Article  PubMed  CAS  Google Scholar 

  36. McNeish, J.D. (2007). Stem cells as screening tools in drug discovery. Curr Opin Pharmacol 7, 515–520

    Article  PubMed  CAS  Google Scholar 

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© 2010 Humana Press

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Pina, A.S., Hussain, A., Roque, A.C.A. (2010). An Historical Overview of Drug Discovery. In: Roque, A. (eds) Ligand-Macromolecular Interactions in Drug Discovery. Methods in Molecular Biology, vol 572. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-60761-244-5_1

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  • DOI: https://doi.org/10.1007/978-1-60761-244-5_1

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  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-60761-243-8

  • Online ISBN: 978-1-60761-244-5

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