20. Role of Metals in HIV-1 Integrase Inhibitor Design

  1. Nouri Neamati
  1. Mario Sechi1,
  2. Mauro Carcelli2,
  3. Dominga Rogolino2 and
  4. Nouri Neamati3

Published Online: 28 SEP 2011

DOI: 10.1002/9781118015377.ch20

HIV-1 Integrase: Mechanism and Inhibitor Design

HIV-1 Integrase: Mechanism and Inhibitor Design

How to Cite

Sechi, M., Carcelli, M., Rogolino, D. and Neamati, N. (2011) Role of Metals in HIV-1 Integrase Inhibitor Design, in HIV-1 Integrase: Mechanism and Inhibitor Design (ed N. Neamati), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9781118015377.ch20

Editor Information

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

Author Information

  1. 1

    Dipartimento di Scienze del Farmaco Università di Sassari, Sassari, Italy

  2. 2

    Dipartimento di Chimica Generale ed Inorganica, Chimica Analitica, Chimica Fisica, Università di Parma, Campus Universitario, Parma, Italy

  3. 3

    Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, School of Pharmacy, Los Angeles, California, 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:

  • metals in HIV-1 integrase inhibitor design;
  • metal cofactor catalytic role;
  • two-metal binding model

Summary

This chapter contains sections titled:

  • Introduction

  • Catalytic Role of Metal Cofactors: Two-Metal-Ion Mechanism

  • Other Metal Ions on IN Enzyme

  • General Basis to Target Metal Ion Cofactors

  • β-Diketo Acids (DKAs): Important Class of IN Inhibitors as Example of Chelating Agents

  • Structural Studies of DKA Pharmacophoric Motif

  • Other Potential Metal Chelating Inhibitors

  • Studies of Chelating Ability for Several Pharmacophore Fragments

  • Two-Metal Binding as Strategy for IN Inhibitor Design: Recent Study

  • Two-Metal Binding Model as Potential General Inhibition Mechanism

  • From Ligands to Metal Complexes

  • Conclusions and Perspectives

  • Acknowledgments

  • Abbreviations

  • References