Introduction

The kinase group of an organism is a group of protein kinases in its genome that are potential targets in many therapeutic areas. Recent studies on the characterization of human kinase sets and the exploration of available kinase crystal structures have led to an increasing focus on kinases as potential targets for drug intervention.

Since the pharmaceutical industry began to focus on kinases in the late 1980s, most of the kinase inhibitors developed have targeted the ATP-binding site of the enzyme. However, the development of Gleevec® has injected new life into research in this area, a tyrosine kinase inhibitor that induces structural reorganization of the target BCR-Abl kinase. This led to innovative ideas for handling kinase inhibition, including binding outside of the ATP site and attempting to prevent kinase activation.

Detailed enzyme kinetic studies play an integral role in characterizing the mechanism of action of compounds based on novel ideas. One method of great value is isothermal titration calorimetry (ITC), which provides complete thermodynamic data on the binding of a compound to a target protein. The data generated using this method can be used to determine the affinity of a compound for binding to different forms of enzymes, such as free enzymes, enzyme-substrate complexes, enzyme-product complexes, active and inactive enzymes.

Enzyme signaling inhibition is a proven treatment for diseases in the field of tumors and inflammation. We already know that ITC can provide information to determine whether other ligands have an effect on the biological activity of the enzyme, so this application report focuses on how ITC can be applied to identify intermolecular complexes of enzymes that confer this biological activity.

ITC Overview

Isothermal titration calorimetry can determine a number of properties of binding in one experiment, including affinity (KD), number of ligand binding sites (n), and enthalpy (ΔH) of the binding reaction. The method is fast, does not require fluorescent labeling, and can be used to study proteins that are not catalytically active (these proteins are excluded from studies of enzyme kinetic analysis due to the absence of catalytic activity).

ITC experiments typically involve titrating a test compound against a target protein at a constant temperature and using an ITC instrument to determine the amount of heat released or absorbed during the binding activity. This method can be used in a variety of ways during drug development for protein kinases.

These include:

Protein structure characterization and preparation, not only the correct affinity of the model ligand, but also the correct stoichiometry to help assess the amount of functional protein without catalytic activity; analytical evaluation; identification of intermolecular complexes that confer biological activity , ITC can provide information to determine whether other ligands have an impact on the biological activity of the test compound, which is the focus of this application report.

To read the full article, please click on the following link:

Http://AN140630RevealKinaseInhibitorITC.aspx

Decomposition of kinase inhibitor mechanism: ITC leads the way.pdf

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