Analysis Interactions of Lead Optimization by Isothermal Titration Calorimetry (ITC) (CAT#: STEM-MB-2517-LGZ)

Introduction

Completion of the human genome has identified a large number of new targets for drug development. Many of these targets belong to protein families with homologous structures and similar active sites. Successful drugs must exhibit high affinity and high selectivity against these targets, which have been elusive and underscore the need for better optimization strategies. These strategies require controlling forces that maximize affinity for the desired target and minimize affinity for other proteins. Since isothermal titration calorimetry (ITC) is the only experimental technique that splits the binding energy into enthalpy and entropy components, it is rapidly becoming a key technique for lead optimization.