The completion of the human genome has resulted in the identification of large numbers of novel targets for drug development. Many of these targets belong to protein families with homologous structures and similar active sites. Against these targets, successful drugs must display high affinity and high selectivity, goals that have been difficult to accomplish and that emphasize the need for bet...

The study of 1:1 cyclodextrin inclusion compounds by isothermal titration calorimetry was explored in a theoretical and experimental point of view to compare the efficiency of conventional and non-conventional experiments. All direct and competitive protocols were described and evaluated in terms of accuracy on both binding constant and inclusion enthalpy. Significant improvement in the calorim...

Understanding the mechanism of protein fibrillization/aggregation and its prevention is the basis of development of therapeutic strategies for amyloidosis. An attempt has been made to understand the nature of interactions of osmolytes L-proline, 4-hydroxy-L-proline, sarcosine and trimethylamine N-oxide with the different stages of fibrillization of hen egg-white lysozyme by using a combination ...

Detailed stopped-flow studies in combination with site-directed mutagenesis, isothermal titration calorimetry data and x-ray crystallographic knowledge have revealed that the biphasic pre-equilibrium fluorescence changes reported for a single Ig-binding domain of protein L from Peptostreptococcus magnus binding to kappa light chain are due to the binding of the kappa light chain at two separate...

One key factor in stabilization of protein drugs in liquid formulations is the choice of appropriate excipients at optimum concentrations that provide extended shelf life while also ensuring highest safety to the patient. Although general principles of stabilization have emerged from the literature over the past decade, the mechanisms by which excipients can improve the stability of a protein d...

The ability of the jack bean lectin concanavalin A (ConA) to bind seven membered ring (septanose) monosaccharides has been investigated by isothermal titration calorimetry (ITC) and saturation transfer difference (STD) NMR spectroscopy.

Isothermal titration calorimetry (ITC) is one of the most interesting methods for the characterization of the interaction mechanisms of cyclodextrins (CDs) with drugs. In this review we explain how to conduct ITC experiments correctly for CD-guest interactions, how to choose an accurate fitting model for the titration curve and how to interpret carefully the ITC results. Finally, the use of ITC...