Advances in calorimetry for drug discovery

Abstract

Calorimetry is a universally applicable label-free and immobilization-free method that directly measures heat changes associated with binding interactions, enzymatic reactions, cell growth, and macromolecule folding and stability. Isothermal titration calorimetry (ITC), the only method that can simultaneously determine all binding parameters (enthalpy, entropy, affinity, and number of sites) in a single experiment, has long been regarded as the gold standard assay for binding. Due to the low throughput and relatively large quantities of material required for the measurements, the application of ITC in drug discovery has been limited. This presentation looks at the advances in the miniaturization of calorimeters and how the increased throughput and reduced sample consumption of these devices could expand the application of calorimetry in drug discovery.