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Pure Appl. Chem., 2001, Vol. 73, No. 9, pp. 1487-1498

Combinatorial chemistry. Facing the challenge of chemical genomics

Ferenc Darvas1, Gyorgy Dorman1, Laszlo Urge1, Istvan Szabo1, Zsolt Ronai2 and Maria Sasvari-Szekely2

1 ComGenex Inc., H-1027 Budapest, Bem rkp. 33-34, Hungary
2 Semmelweis University Medical School, Institute of Medical Chemistry, Molecular Biology and Pathobiochemistry, H-1088, Budapest, Puskin u. 9, Hungary

In the age of high-throughput screening and combinatorial chemistry, the focus of drug discovery is to replace the sequential approach with the most effective parallel approach. By the completion of the human gene-map, understanding and healing a disease require the integration of genomics, proteomics, and, very recently, metabolomics with early utilization of diverse small-molecule libraries to create a more powerful "total" drug discovery approach.
In this post-genomic era, there is an enhanced demand for information-enriched combinatorial libraries which are high-quality, chemically and physiologically stable, diverse, and supported by measured and predicted data. Furthermore, specific marker libraries could be used for early functional profiling of the genome, proteome, and metabolome. In this new operating model, called "combinatorial chemical genomics", an optimal combination of the marker and high-quality libraries provides a novel synergy for the drug discovery process at a very early stage.