Competitive Assay Approach: Binding of Small Molecules to the Active Form of p38
Krishna Saxena, Moran Jerabek‐Willemsen · 2011
p38 α 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 measurements 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.