Microarrays in Chemical Biology

Abstract Advances in both genomics and proteomics have provided researchers with access to large collections of biomolecules, including DNA, proteins, and metabolites. High‐throughput methods are needed to study the function and regulation of these biomolecules within complex systems. Microarrays have emerged as a common platform to study biomolecular interactions that involve nucleic acids, proteins, and small molecules. DNA microarrays have revolutionized genomic research by allowing researchers to study gene expression, sequence variation, and transcription factor binding sites on a whole‐genome scale. Protein microarrays can be used to study interactions with other proteins, DNA, RNA, and small molecules, including lipids, carbohydrates, and drugs. Protein microarrays can also be used as analytical tools to profile complex protein mixtures, such as fractionated cell lysates, in an effort to study antibody specificity, measure changes in protein abundance, or characterize disease states. Small‐molecule microarrays are useful tools for ligand discovery, comparing inhibitor specificity across enzyme classes, high‐throughput, cell‐based phenotypic screens, and as diagnostic tools for pathogen detection. The microarray approach has been extended to transfected cell microarrays, RNAi living cell microarrays, virus microarrays, and tissue microarrays. This article reviews chemical strategies for making microarrays and applications of microarrays in chemical biology.