Chemical microarrays, fragment diversity, label-free imaging by plasmon resonance--a chemical genomics approach.

Abstract

Chemical genomics aim to create synergy between synthetic small molecule chemistry and biosciences employing genomic tools and information. Central to chemical genomics is the discovery of bioactive compounds from novel targets for pharmaceutical lead development. The field is challenged both by the multitude and novelty of protein and other biomacromolecular targets to be studied. Affinity fingerprints, data sets of binding interactions between collections of chemicals and their macromolecular receptors, hold promise to guide drug design and study protein function for groups of related compounds and families of biomacromolecules. Despite their fundamental relevance, neither experimental protocols nor databases of quantitative and comprehensive description of binding interactions for small molecule ligands and biomacromolecular receptors are available. Chemical microarrays in combination with label-free imaging provide a novel route towards the systematic and standardized acquisition and application of such affinity fingerprint information.