Presentation: 3C04

HTS using in vitro biochemical assays offer a straightforward approach to discovering small molecule inhibitors. The challenge is choosing a model substrate that both insures the relevance of reactive inhibitors and increases their likelihood of cellular activity. Microfluidic screening of kinase families typically use a peptide substrate whose phosphorylated product can be separated by voltage and pressure. Routine screening of a peptide library revealed multiple substrates for several kinases that have a common motif. These circumstances raise the question as to whether the chosen substrate is valid. Alternatively, a microfluidic-based coupled assay will be described that takes advantage of the linear nature of the kinase pathway. This approach provides a potentially more relevant substrate, offers economic advantages and allows screening of target classes that may not have a model peptide substrate.

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