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Small molecules have long been recognized as an invaluable part of human medicine. Well before chemistry, biology, and chemical genomics were established as scientific disciplines, people routinely used plants to treat and prevent illnesses. Not until the advent of modern science, however, were we able to isolate and identify the active ingredients that conferred on the flora around us such a vast array of effects. Along with synthetic and semisynthetic molecules, these naturally occurring compounds have formed the cornerstone of today's therapeutics and have provided a way of improving our understanding of fundamental biological processes.
Exploration of these processes using chemical genetics requires certain basic elements common to all studies: 1) a small molecule with good target specificity, 2) a protein of interest, 3) a phenotype that is being investigated, and 4) an assay or screen that will bring these elements together to provide useful information (Figure 2.1).
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