Chemogenomic Approach to Drug Discovery

Chemogenomics is the interdisciplinary approach that attempts to derive predictive links between the chemical structures of bioactive molecules and the receptors with which these molecules interact.

Chemogenomics thus unites medicinal chemistry with molecular biology and uses low-resolution sequence homology to identify genomic targets of interest. Insights from chemogenomics are used for the rational compilation of screening sets and for the rational design and synthesis of directed chemical libraries to accelerate drug discovery. Ligands identified by this method can be used in secondary biological assays to check for biological activity. In the case of targets of unknown function, lowthroughput secondary assays can be used to determine the therapeutic relevance of a novel target. Chemogenomics can be applied to the discovery and description of all possible drug compounds (all of the chemical possibilities) directed at all possible drug targets. This approach has the potential to cover a broad range of therapeutic areas, because while gene families code for structurally similar proteins, each protein in a gene family can have a very different biological function.

Different targets within a gene family may be implicated in widely different diseases. In practice, the chemogenomics approach is accelerating the drug discovery and will increase the flow of new drug candidates into development.