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Competitive Assay Approach: Binding of Small Molecules to the Active Form of p38

p38α is considered as the key isoform involved in modulating inflammatory response in rheumatoid arthritis and inflammatory pain and is therefore a key target for compound screening in pharmaceutical industry. In this study we demonstrate the use of MicroScale Thermophoresis to perform an essentially label-free measurement of small molecule binding to protein targets by using a competitive approach. This approach therefore allows screening projects aiming to identify and characterize site-specific binders or binders allosterically influencing a specific binding site out of a compound library. Furthermore this approach also can be used to screen for compounds that interrupt protein-protein, protein-peptide or protein-nucleic acid interactions.

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