Activation State-Selective Kinase Inhibitor Assay Based by Ion Mobility-Mass Spectrometry (CAT#: STEM-ST-0143-LJX)

Introduction

The discovery of activation state dependent kinase inhibitors, which bind specifically to the inactive conformation of the protein, is considered to be a promising pathway to improved cancer treatments. Identifying such inhibitors is challenging, however, because they can have Kd values similar to molecules known to inhibit kinase function by interacting with the active form. Further, while inhibitor induced changes within the kinase tertiary structure are significant, few technologies are able to correctly assign inhibitor binding modes in a high-throughput fashion based exclusively on protein–inhibitor complex formation and changes in local protein structure. Ion migration mass spectrometry can rapidly detect inhibitor binding and classifying the resultant kinase binding modes.