To determine the protein linearity of enzymatic action
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Enzymes are important drug targets. Many marketed drugs today function through inhibition of enzymes mediating disease phenotypes. To design, develop and validate robust enzymatic assays for HTS applications, it is critical to have a thorough understanding of the enzyme biochemistry and the kinetics of enzyme action. This chapter contains basic concepts in enzyme kinetics, selection of appropriate substrates for assay design and the estimation and significance of Km and Vmax, the intrinsic kinetic parameters of enzyme targets. These concepts are addressed in the context of drug discovery and HTS assay development.
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