Chemogenomics

Chemogenomics, or Chemical Genomics, is the systematic screening of targeted chemical libraries of small molecules against individual drug target families (e.g., GPCRs, nuclear receptors, kinases, proteases, etc.) with the ultimate goal of identification of novel drugs and drug targets. Typically some members of a target library have been well characterized where both the function has been determined and compounds that modulate the function of those targets (ligands in the case of receptors, inhibitors of enzymes, or blockers of ion channels) have been identified. Other members of the target family may have unknown function with no known ligands and hence are classified as orphan receptors. By identifying screening hits that modulate the activity of the less well characterized members of the target family, the function of these novel targets can be elucidated. Furthermore the hits for these targets can be used as a starting point for drug discovery.

A common method to construct a targeted chemical library is to include known ligands of at least one and preferably several members of the target family. Since a portion of ligands that were designed and synthesized to bind to one family member will also bind to additional family members, the compounds contained in a targeted chemical library should collectively bind to a high percentage of the target family.

See also

• Chemical biology
• Chemical genetics

Further reading

• Folkers G, Kubinyi H, Müller G, Mannhold R (2004). Chemogenomics in drug discovery: a medicinal chemistry perspective. Weinheim: Wiley-VCH. ISBN 3-527-30987-X. 
• Jacoby E (2009). Chemogenomics: methods and applications. Totowa, NJ: Humana Press. ISBN 1-60761-273-9. 
• Weill N (2011). "Chemogenomic approaches for the exploration of GPCR space". Curr Top Med Chem. 11 (15): 1944–1955. doi:10.2174/156802611796391212. PMID 21470168. 

External links

• Kubinyi's slides