An assessment of the number of molecular targets that represent an opportunity for therapeutic intervention is crucial to the development of post-genomic research strategies within the pharmaceutical industry. Now that we know the size of the human genome, it is interesting to consider just how many molecular targets this opportunity represents. We start from the position that we understand the properties that are required for a good drug, and therefore must be able to understand what makes a good drug target.
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Lipinski, C., Lombardo, F., Dominy, B. & Feeney, P. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv. Drug Deliv. Rev. 23, 3–25 (1997).
Drews, J. Genomic sciences and the medicine of tomorrow. Nature Biotechnol. 14, 1516–1518 (1996).
Drews, J. & Ryser, S. Classic drug targets. Nature Biotechnol. 15, 1318–1319 (1997).
Drews, J. Drug discovery: a historical perspective. Science 287, 1960–1964 (2000).
Bailey, D., Zanders, E. & Dean, P. The end of the beginning for genomic medicine. Nature Biotechnol. 19, 207–209 (2001).
Apweiler, R. et al. The InterPro database, an integrated documentation resource for protein families, domains and functional sites. Nucleic Acids Res. 29, 37–40 (2001).
Proteome Analysis Database [online], (version analysed with release date 29 Oct 01) 〈http://www.ebi.ac.uk/proteome/〉 (2001).
Lander, E. et al. Initial sequencing and analysis of the human genome. Nature 409, 860–921 (2001).
Venter, J. C. et al. The sequence of the human genome. Science 291, 1304–1351 (2001).
Tweeddale, H., Notley-McRobb, L. & Ferenci, T. Effect of slow growth on metabolism of Escherichia coli, as revealed by global metabolite pool ('metabolome') analysis. J. Bacteriol. 180, 5109–5119 (1998).
Fiehn, O. et al. Metabolite profiling for plant functional genomics. Nature Biotechnol. 18, 1157–1161 (2000).
Raamsdonk, L. et al. A functional genomics strategy that uses metabolome data to reveal the phenotype of silent mutations. Nature Biotechnol. 19, 45–50 (2001).
Claverie, J.-M. What if there are only 30,000 human genes? Science 291, 1255–1257 (2001).
Walke, D. W. et al. In vivo drug target discovery: identifying the best targets from the genome. Curr. Opin. Biotechnol. 12, 626–631 (2001)
Lehman Brothers. The Fruits of Genomics (Lehman Brothers, 2001).
Rubin, G.et al Comparative genomics of the eukaryotes. Science 287, 2204–2215 (2000).
We are indebted to J. P. Overington (Inpharmatica, London), A. Alex and L. Beeley for their contributions to the ideas on the physico-chemical limits for protein-binding sites. We also thank R. W. Spencer and C. Lipinski (Pfizer, Groton, Connecticut, USA) for much stimulating discussion.
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