HIV-1 Integrase: Mechanism and Inhibitor Design

Copyright © 2011 John Wiley & Sons, Inc.

HIV-1 Integrase: Mechanism and Inhibitor Design

Editor(s): Nouri Neamati

Published Online: 28 SEP 2011 09:48AM EST

Print ISBN: 9780470184745

Online ISBN: 9781118015377

DOI: 10.1002/9781118015377

Series Editor(s): Binghe Wang

About this Book

Product Information

About The Product

This book comprehensively covers the mechanisms of action and inhibitor design for HIV-1 integrase. It serves as a resource for scientists facing challenging drug design issues and researchers in antiviral drug discovery. Despite numerous review articles and isolated book chapters dealing with HIV-1 integrase, there has not been a single source for those working to devise anti-AIDS drugs against this promising target. But this book fills that gap and offers a valuable introduction to the field for the interdisciplinary scientists who will need to work together to design drugs that target HIV-1 integrase.

Table of contents

    1. You have free access to this content
      Frontmatter (pages i–xiii)

    2. You have free access to this content
      Color Plates (pages c1–c16)

    3. Chapter 1

      HIV Life Cycle: Targets for Anti-HIV Agents (pages 1–14)

      Erik De Clercq

    4. Chapter 2

      pp32 Is Hot (pages 15–21)

      Duane P. Grandgenett

    5. Chapter 3

      Integrase Mechanism and Function (pages 23–33)

      Robert Craigie

    6. Chapter 4

      Structural Studies of Retroviral Integrases (pages 35–49)

      Mariusz Jaskolski, Jerry N. Alexandratos, Grzegorz Bujacz and Alexander Wlodawer

    7. Chapter 5

      Retroviral Integration Target Site Selection (pages 51–65)

      Angela Ciuffi and Frederic Bushman

    8. Chapter 6

      Pleiotropic Nature of HIV-1 Integrase Mutations (pages 67–81)

      Alan Engelman

    9. Chapter 7

      Insights into HIV-1 Integrase–DNA Interactions (pages 83–94)

      Allison Johnson, Christophe Marchand and Yves Pommier

    10. Chapter 8

      Functional Interaction between Human Immunodeficiency Virus Type 1 Reverse Transcriptase and Integrase (pages 95–103)

      Thomas A. Wilkinson and Samson A. Chow

    11. Chapter 9

      Cellular Cofactors of HIV Integration (pages 105–129)

      Wannes Thys, Koen Bartholomeeusen, Zeger Debyser and Jan De Rijck

    12. Chapter 10

      Structural aspects of Lentiviral Integrase–LEDGF Interaction (pages 131–140)

      Stephen Hare, Alan Engelman and Peter Cherepanov

    13. Chapter 11

      Host Factors that affect Provirus Stability and Silencing (pages 141–150)

      Richard A. Katz, René Daniel and Anna Marie Skalka

    14. Chapter 12

      Assays for Evaluation of HIV-1 Integrase Enzymatic Activity, DNA Binding, and Cofactor Interaction (pages 151–163)

      Frauke Christ, Katrien Busschots, Jelle Hendrix, Melissa McNeely, Yves Engelborghs and Zeger Debyser

    15. Chapter 13

      HIV-1 Integrase Inhibitor Design: Overview and Historical Perspectives (pages 165–196)

      Nouri Neamati

    16. Chapter 14

      HIV Integrase Inhibitors: From Diketo Acids to Heterocyclic Templates: History of HIV Integrase Medicinal Chemistry at Merck West Point and Merck Rome (IRBM) Leading to Discovery of Raltegravir (pages 197–229)

      Melissa S. Egbertson, Neville J. Anthony and Vincenzo Summa

    17. Chapter 15

      Elvitegravir: Novel Quinolone HIV-1 Integrase Strand Transfer Inhibitor (pages 231–238)

      Hisashi Shinkai, Motohide Sato and Yuji Matsuzaki

    18. Chapter 16

      Conformationally Constrained Tricyclic HIV Integrase Inhibitors (pages 239–254)

      Maria Fardis, Haolun Jin, Xiaowu Chen, Manuel Tsiang, James Chen, Choung Kim and Matthew Wright

    19. Chapter 17

      Slow-Onset Kinetics of HIV Integrase Inhibitors and Proposed Molecular Model (pages 255–263)

      Edward P. Garvey and Benjamin Schwartz

    20. Chapter 18

      Azaindole Hydroxamic Acids are HIV-1 Integrase Inhibitors (pages 265–274)

      Michael B. Plewe and Ted W. Johnson

    21. Chapter 19

      Simple and Accurate In Vitro Method for Predicting Serum Protein Binding of HIV Integrase Strand Transfer Inhibitors (pages 275–286)

      Ira B. Dicker, Michael A. Walker, Zeyu Lin, Brian Terry, Lori Pajor, Ming Zheng, B. Narasimhulu Naidu, Jacques Banville, Nicholas A. Meanwell and Mark Krystal

    22. Chapter 20

      Role of Metals in HIV-1 Integrase Inhibitor Design (pages 287–307)

      Mario Sechi, Mauro Carcelli, Dominga Rogolino and Nouri Neamati

    23. Chapter 21

      Discovery and Development of Natural Product Inhibitors of HIV-1 Integrase (pages 309–323)

      Sheo B. Singh

    24. Chapter 22

      Development of Styrylquinoline Integrase Inhibitors (pages 325–339)

      Jean-François Mouscadet, Eric Deprez, Didier Desmaele and Jean D'Angelo

    25. Chapter 23

      Dicaffeoyltartaric Acid and Dicaffeoylquinic Acid HIV Integrase Inhibitors (pages 341–362)

      David C. Crosby and W. Edward Robinson

    26. Chapter 24

      Design and Discovery of Peptide-Based HIV-1 Integrase Inhibitors (pages 363–377)

      Ya-Qiu Long and Nouri Neamati

    27. Chapter 25

      Nucleotide-Based Inhibitors of HIV Integrase (pages 379–388)

      Vasu Nair and Guochen Chi

    28. Chapter 26

      Computer-Aided Techniques in Design of HIV-1 Integrase Inhibitors (pages 389–413)

      Erik Serrao, Rambabu Gundla, Jinxia Deng, Srinivas Odde and Nouri Neamati

    29. Chapter 27

      Application of Protein Covalent Modification to Studying Structure and Function of HIV-1 Integrase and Its Inhibitors (pages 415–427)

      Xue Zhi Zhao and Terrence R. Burke

    30. Chapter 28

      HIV-1 Integrase–DNA Models (pages 429–455)

      Chenzhong Liao and Marc C. Nicklaus

    31. Chapter 29

      New Paradigm for Integrase Inhibition: Blocking Enzyme Function without Directly Targeting the Active Site (pages 457–476)

      Laith Q. Al-Mawsawi and Nouri Neamati

    32. Chapter 30

      Resistance to Inhibitors of HIV-1 Integrase (pages 477–498)

      Anneleen Hombrouck, Reginald Clayton, Arnout Voet, Myriam Witvrouw and Zeger Debyser

    33. You have free access to this content
      Index (pages 499–506)

    34. You have free access to this content
      Wiley Series in Drug Discovery and Development (pages 507–508)

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