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

p38α is considered as the key isoform involvedin modulating inflammatory response inrheumatoid arthritis and inflammatory painand is therefore a key target for compoundscreening in pharmaceutical industry. In thisstudy we demonstrate the use of MicroscaleThermophoresis to perform an essentiallylabel-free measurements of small moleculebinding to protein targets by using acompetitive approach. This approach thereforeallows screening projects aiming to identifyand characterize site-specific binders orbinders allosterically influencing a specificbinding site out of a compound library. Furthermore this approach also can be used toscreen for compounds that interrupt proteinprotein,protein-peptide or protein-nucleic acidinteractions.