13. HIV-1 Integrase Inhibitor Design: Overview and Historical Perspectives

  1. Nouri Neamati
  1. Nouri Neamati

Published Online: 28 SEP 2011

DOI: 10.1002/9781118015377.ch13

HIV-1 Integrase: Mechanism and Inhibitor Design

HIV-1 Integrase: Mechanism and Inhibitor Design

How to Cite

Neamati, N. (2011) HIV-1 Integrase Inhibitor Design: Overview and Historical Perspectives, in HIV-1 Integrase: Mechanism and Inhibitor Design (ed N. Neamati), John Wiley & Sons, Inc., Hoboken, NJ, USA. doi: 10.1002/9781118015377.ch13

Editor Information

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

Author Information

  1. 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:

  • HIV-1 integrase inhibitor design;
  • highly active antiretroviral therapy (HAART);
  • nucleotides, nucleosides, guanosine quartets

Summary

This chapter contains sections titled:

  • Introduction

  • HIV-1 Integrase as Target for Antiviral Therapy

  • Why Did It Take Such a Long Time to Develop Selective IN Inhibitors?

  • Early Days: Clues from Inhibitors of Other DNA-Processing Enzymes

  • Hydroxylated Aromatics (Catechol-Containing Inhibitors): False Positives?

  • Non-Catechol-Containing Aromatics

  • Nucleotides, Nucleosides, and Guanosine Quartets

  • DNA Binders as Inhibitors of IN

  • Peptides and Peptidomimetics

  • Dual-Inhibitor Approach: Killing Two Birds with One Stone

  • Random Versus Biased Screening

  • NCI Chemical Database

  • Diketo Acid–Containing Inhibitors: Emergence of Bona Fide IN Inhibitors

  • Medicinal Chemistry: Optimization and Second-Generation Drugs

  • Clinical Progress of HIV-1 Integrase Inhibitors

  • Pharmacology of Raltegravir

  • Resistance and Treatment Failure

  • Conclusions and Future Perspectives

  • Acknowledgments

  • References