13. HIV-1 Integrase Inhibitor Design: Overview and Historical Perspectives
- Nouri Neamati
Published Online: 28 SEP 2011
DOI: 10.1002/9781118015377.ch13
Copyright © 2011 John Wiley & Sons, Inc.
Book Title
HIV-1 Integrase: Mechanism and Inhibitor Design
Additional Information
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
Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, School of Pharmacy, Los Angeles, California, USA
Publication History
- Published Online: 28 SEP 2011
- Published Print: 9 SEP 2011
ISBN Information
Print ISBN: 9780470184745
Online ISBN: 9781118015377
- Summary
- Chapter
- References
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