Monitoring Conformational Changes upon Ligand Binding

Monitoring Conformational Changes upon Ligand Binding 

We have developed FLiK as a widely-apphcable assay system for both identifying and characterizing DFG-out binding ligands [6, 7]. Kinases are site-specificaUy 

In this chapter, we focus on the development and application of the FLiK and FLIP approaches, championed by our laboratories in Dortmund. Our group has employed these assays to address a number of kinases and phosphatases from different organisms and to facilitate the development of novel inhibitors and functional probes. We then utilize such probes and tool compounds to decipher phosphorylation and dephosphorylation events within complex disease states and to Foster drug development. Rather than detailing the findings of the different studies, this chapter will focus on the structure-based design of FLiK and FLiP protein constructs to enable these assays and their application in screening initiatives. 

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Monitoring Conformational Changes upon Ligand Binding... 

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