Chemogenomics: structuring the drug discovery process to gene families

In the post-genomic era, if all proteins in a gene family can putatively be identified, how can drug discovery effectively tackle so many novel targets that might lack structural and small-molecule inhibitory data? In response, chemogenomics, a new approach that guides drug discovery based on gene families, has been developed. By integrating all information available within a protein family (sequence, SAR data, protein structure), chemogenomics can efficiently enable cross-SAR exploitation, directed compound selection and early identification of optimum selectivity panel members. This review examines recent developments in chemogenomics technologies and illustrates their predictive capabilities with successful examples from two of the major protein families: protein kinases and G-protein-coupled receptors.