19. Simple and Accurate In Vitro Method for Predicting Serum Protein Binding of HIV Integrase Strand Transfer Inhibitors

  1. Nouri Neamati
  1. Ira B. Dicker1,
  2. Michael A. Walker2,
  3. Zeyu Lin1,
  4. Brian Terry1,
  5. Lori Pajor3,
  6. Ming Zheng3,
  7. B. Narasimhulu Naidu2,
  8. Jacques Banville2,
  9. Nicholas A. Meanwell2 and
  10. Mark Krystal1

Published Online: 28 SEP 2011

DOI: 10.1002/9781118015377.ch19

HIV-1 Integrase: Mechanism and Inhibitor Design

HIV-1 Integrase: Mechanism and Inhibitor Design

How to Cite

Dicker, I. B., Walker, M. A., Lin, Z., Terry, B., Pajor, L., Zheng, M., Naidu, B. N., Banville, J., Meanwell, N. A. and Krystal, M. (2011) Simple and Accurate In Vitro Method for Predicting Serum Protein Binding of HIV Integrase Strand Transfer Inhibitors, in HIV-1 Integrase: Mechanism and Inhibitor Design (ed N. Neamati), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9781118015377.ch19

Editor Information

  1. Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, School of Pharmacy, Los Angeles, California, USA

Author Information

  1. 1

    Department of Virology, Bristol-Myers Squibb Research & Development, Wallingford, Connecticut, USA

  2. 2

    Department of Discovery Chemistry, Bristol-Myers Squibb Research & Development, Wallingford, Connecticut, USA

  3. 3

    Department of Preclinical Candidate Optimization, Bristol-Myers Squibb Research & Development, Wallingford, Connecticut, USA

Publication History

  1. Published Online: 28 SEP 2011
  2. Published Print: 9 SEP 2011

Book Series:

  1. Wiley Series in Drug Discovery and Development

Book Series Editors:

  1. Binghe Wang

ISBN Information

Print ISBN: 9780470184745

Online ISBN: 9781118015377

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Keywords:

  • HIV integrase inhibitor serum protein binding;
  • protein binding effects;
  • in vitro displacement assay

Summary

This chapter contains sections titled:

  • Introduction

  • Identification of Early Leads in Bristol-Myers Squibb (BMS) Discovery Program

  • Evaluating Protein Binding Effect on Integrase Inhibitors

  • Development of In Vitro Displacement Assay for Protein Binding Estimations

  • Conclusion

  • Experimental Methods

  • Acknowledgments

  • References