Receptor Tyrosine Kinase Screening - Closer To Physiology

Screening of kinases is mostly performed in biochemical assays with purified enzymes. The success story of Gleevec however has shown that inhibitors binding to the inactive state of a kinase have the potential of becoming marketable drugs. This poster will give insight into a project where the initial screening of the soluble kinase domain of a receptor tyrosine kinase (RTK) did not give valuable hits. We therefore set forth to develop a cell based HTS-compatible assay for this RTK, where one would have the chance to find new inhibitors binding to a different activation state of the kinase.