Target Identification for Biologically Active Small Molecules Using Chemical Biology Approaches

The identification and validation of the targets of biologically active molecules is an important step in the field of chemical biology. While recent advances in proteomic and genomic technology have accelerated this identification process, the discovery of small molecule targets remains the most challenging step. A general method for the identification of these small molecule targets has not yet been established. To overcome the difficulty in target identification, new technology derived from the fields of genomics, proteomics, and bioinformatics has been developed. To date, pull-down methods using small molecules immobilized on a solid support followed by mass spectrometry have been the most successful approach. Here, we discuss current procedures for target identification. We also review the most recent target identification approaches and present several examples that illustrate advanced target identification technology.