Measurements of binding thermodynamics in drug discovery.
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.
Holdgate
Geoffrey A
GA
Molecular Enzymology Group, AstraZeneca, Alderley Park, Macclesfield, Cheshire SK10 4TG, UK. geoff.holdgate@astrazeneca.com
Ward
Walter H J
WH
D002151:Calorimetry / Q000295:instrumentation / Q000379:methods; D015195:Drug Design; D011485:Protein Binding; D011489:Protein Denaturation; D011506:Proteins / Q000737:chemistry; D013816:Thermodynamics
D011506:Proteins