Measurements of binding thermodynamics in drug discovery

Measurements of binding thermodynamics in drug discovery
Available online 27 October 2005.
Geoffrey A. Holdgate and Walter H.J. Ward
Drug Discovery Today
Volume 10, Issue 22 , 15 November 2005
Molecular Enzymology Group, AstraZeneca, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK
Thermodynamics governs the process of biomolecular recognition. The steps of characterizing, understanding and exploiting binding thermodynamics have the potential to contribute to an improved rational drug design process that is more robust and reliable. It is only relatively recently that instrumentation capable of direct and full thermodynamic characterization has been improved, giving impetus to the application of thermodynamic measurements in drug discovery. This review highlights current instruments and methods that can be employed to measure binding thermodynamics and their use in studies of biomolecular recognition and drug discovery.
Improved methods are now available to characterize binding thermodynamics. This review summarizes these methods and the exploitation of the derived thermodynamic information in drug discovery.
Author Keywords: Thermodynamics; ligand binding; calorimetry; protein stability; isothermal titration calorimetry; ITC; differential scanning calorimetry; DSC
Subject-index terms: Pharmaceutical Science; Drug Discovery; Biophysics
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