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The Chapter reviews the scope of the chemical genetic approach in the investigation of biological mechanisms. Particular emphasis is placed on the impact of chemistry in the synthesis of libraries of diverse small molecules; the screening of small molecule libraries for biological function; and the identification of the proteins that specific ligands target. The features of the chemical genetics are placed in the context of other approaches that may be used to modulate the functions of proteins (such as classical genetics and RNAi). Insights into specific fundamental biological mechanisms that have been gleaned from a chemical genetic approach are described. In addition, some of the major challenges in the future that will need to be addressed are outlined.

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