ABSTRACT

Thermodynamic properties such as the enthalpy of reaction and entropy change of reaction are important characteristics of binding interactions between drugs and their targets. Calorimetry is a valuable method for studying the thermodynamics of binding reactions and can be used by pharmaceutical researchers to accelerate the pace and reduce the cost of developing new drugs and result in therapeutics with improved efcacy. Unlike the rest of the material in this book, this chapter presents technology used to support the development of targeted therapies, rather than directly advance diagnosis or prognosis of cancer. This is done by addressing key limitations associated with isothermal titration calorimetry (ITC), namely, that too much compound and protein are required to perform a calorimetry experiment and the experimental throughput is too low and incompatible with the scale of the drug development process.