Isothermal titration calorimetry in membrane protein research

• ITC is an excellent tool to characterize energetics of ligand–protein interactions.
• Membrane proteins are molecular targets to almost 50% of drugs used in therapies.
• Tremendous progress is observed recently in characterization of membrane proteins.
• Precise applications of ITC methods to study these systems are reviewed.

Isothermal titration calorimetry is a versatile method to characterize energetics of intermolecular reactions and in particular interactions between drug molecules and their macromolecular targets. The assay is widely used in medicinal chemistry to quantification and characterization of molecular mechanisms of these interactions. The article reviews applications of the method to study ligand interactions with various classes of embedded membrane proteins. These proteins constitute very important fraction of macromolecular targets for medicinal compounds used in current therapies and recently emerged for detailed structural, functional and biochemical characterization of their interactions with drug molecules.

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