6. Selecting the Best HTS Hits to Move Forward: ITC Ligand Binding Characterization Provides Guidance

  1. Matthew Cooper2 and
  2. Lorenz M. Mayr3
  1. Ronan O'Brien and
  2. Richard Brown

Published Online: 24 FEB 2011

DOI: 10.1002/9780470979129.ch6

Label-Free Technologies for Drug Discovery

Label-Free Technologies for Drug Discovery

How to Cite

O'Brien, R. and Brown, R. (2011) Selecting the Best HTS Hits to Move Forward: ITC Ligand Binding Characterization Provides Guidance, in Label-Free Technologies for Drug Discovery (eds M. Cooper and L. M. Mayr), John Wiley & Sons, Ltd, Chichester, UK. doi: 10.1002/9780470979129.ch6

Editor Information

  1. 2

    Institute for Molecular Bioscience, University of Queensland, Australia

  2. 3

    Biology Unit, Protease Platform, Novartis Pharma AG, Basel, Switzerland

Author Information

  1. GE Healthcare, MicroCal Products Group, 22 Industrial Drive East, Northampton, MA, USA

Publication History

  1. Published Online: 24 FEB 2011
  2. Published Print: 25 FEB 2011

ISBN Information

Print ISBN: 9780470746837

Online ISBN: 9780470979129

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Keywords:

  • selecting the best HTS hits to move forward - ITC ligand binding characterization providing guidance;
  • isothermal titration calorimetry (ITC) - “gold standard” in determining affinity of biomolecular interactions;
  • ITC, and latest developments - iTC200 and AutoiTC200;
  • principles of isothermal titration calorimetry (ITC);
  • isothermal titration calorimeters - measuring temperature changes, two molecule interaction;
  • ITC in HIT validation applications;
  • assay design for Hit confirmation and affinity determination;
  • high speed ITC Hit characterization assays;
  • “fragment-based” strategy for ligand design - in pharmaceutical industry;
  • ITC, facilitating decision making of medicinal chemists - ensuring “rule of five” compliance

Summary

This chapter contains sections titled:

  • Introduction

  • Principles of Isothermal Titration Calorimetry (ITC)

  • Applications of ITC in Hit Validation

  • Applications of ITC in Fragment-Based Drug Discovery

  • Applications of ITC in Mechanism of Action Studies

  • Applications of ITC in Lead Optimization

  • ITC as an Enzyme Activity Monitor

  • Conclusion

  • References