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Updated: Feb 25, 2026
Isothermal Titration Calorimetry for Measuring Macromolecule-Ligand Affinity
Published on: September 7, 2011
Binding properties of different categories of IDO1 inhibitors: a microscale thermophoresis study
Francesco Antonio Greco1, Alice Coletti1, Chiara Custodi1
1Dipartimento di Scienze Farmaceutiche, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy.
Aim:
Inhibition of IDO1 is a strategy pursued in the immune-oncology pipeline for the development of novel anticancer therapies. At odds with an ever-increasing number of inhibitors being disclosed in the literature and patent applications, only very few compounds have hitherto advanced in clinical settings.
Materials & Methods:
We have used MicroScale Thermophoresis analysis and docking calculations to assess on a quantitative basis the binding properties of distinct categories of inhibitors to IDO1.
Results:
Results shed further light on hidden molecular aspects governing the recognition by the enzyme of compounds with different mechanism of inhibition.
Conclusion:
Results pinpoint specific binding features of distinct inhibitors to IDO1 that offer clues for the design of next-generation inhibitors of the enzyme.
