Pure Appl. Chem., 2001, Vol. 73, No. 9, pp. 1487-1498
doi:10.1351/pac200173091487
Combinatorial chemistry. Facing the challenge of chemical genomics*
Ferenc Darvas,#, Gyorgy Dorman, Laszlo Urge, Istvan Szabo, Zsolt Ronai, and Maria Sasvari-Szekely
1ComGenex Inc., H-1027 Budapest, Bem rkp. 33-34, Hungary; 2Semmelweis University Medical School, Institute of Medical Chemistry, Molecular Biology and Pathobiochemistry, H-1088, Budapest, Puskin u. 9, Hungary
Abstract:
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.