Hiv-1 Integrase

Mechanism and Inhibitor Design
Ed. by Nouri Neamati and Binghe Wang

• Gebundenes Buch

Produktbeschreibung

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.

Produktdetails

• Wiley series in drug discovery and development
• Verlag: Wiley & Sons
• Artikelnr. des Verlages: 14518474000
• 1. Auflage
• Seitenzahl: 520
• Erscheinungstermin: 27. September 2011
• Englisch
• Abmessung: 286mm x 225mm x 35mm
• Gewicht: 1470g
• ISBN-13: 9780470184745
• ISBN-10: 0470184744
• Artikelnr.: 33213843

Autorenporträt

Nouri Neamati, PhD, is an Associate Professor of Pharmacology and Pharmaceutical Sciences at the University of Southern California School of Pharmacy. He is the recipient of numerous awards and has published more than 170 peer-reviewed manuscripts, several book chapters, and patents in the area of drug design and discovery. Dr. Neamati is the Editor-in-Chief of Current Molecular Pharmacology; an Associate Editor of Current Cancer Drug Targets; and an Editorial Advisory Board member of several journals including Expert Opinion on Drug Discovery, Expert Opinion on Investigational Drugs, and Hormones & Cancer.

Inhaltsangabe

Chapter 1. HIV life cycle: Targets for anti-HIV agents (Erik De Clercq
(Rega Institute)). Chapter 2. PP32 is hot (Duane P. Grandgenett (SLU)).
Chapter 3. Integrase mechanism and function (Robert Craigie (NIDDK, NIH)).
Chapter 4. Structural studies of retroviral integrases (Mariusz Jaskolski,
Jerry N. Alexandratos, Grzegorz Bujacz and Alexander Wlodawer (NIDDK, NCI,
NIH)). Chapter 5. Retroviral integration target site selection (Angela
Ciuffi and Frederick Bushman (U. Penn)). Chapter 6. The pleiotropic nature
of human immunodeficiency virus type 1 integrase mutations (Alan Engelman
(Harvard)). Chapter 7. Insights into HIV-1 integrase-DNA interaction
(Allison Johnson, Christopse Marchand, and Yves Pommier (NCI, NIH)).
Chapter 8. Functional interaction between human immunodeficiency virus type
1 reverse transcriptase and integrase (Thomas Wilkinson and Samson A. Chow
(UCLA)). Chapter 9. Cellular cofactors of HIV integration (Wannes Thys,
Koen Bartholomeeusen, Zeger Debyser and Jan De Rijck (KULeuven)). Chapter
10. Structural aspects of the lentiviral integrase - LEDGF interaction
(Steve Hare, Alan Engelman and Peter Cherepanov (Imperial College London
and Harvard)). Chapter 11. Host factors that affect provirus stability and
silencing (Richard A. Katz, René Daniel and Anna Marie Skalka (Fox Chase)).
Chapter 12. Assays for the evaluation of HIV-1 integrase enzymatic
activity, DNA-binding and co-factor interaction (Frauke Christ, Katrien
Busschots, Jelle Hendrix, Melissa McNeely, Yves Engelborghs, Zeger Debyser
(KU Leuven, Belgium)). Chapter 13. HIV-1 integrase inhibitor design:
Overview and historical perspectives (Nouri Neamati (USC)). Chapter 14. HIV
integrase inhibitors: from diketoacids to heterocyclic templates: A history
of HIV integrase medicinal chemistry at Merck West Point and Merck Rome
(IRBM) leading to the discovery of raltegravir (Melissa S. Egbertson,
Neville J. Anthony and Vincenzo Summa). Chapter 15. Elvitegravir, a novel
quinolone HIV-1 integrase strand transfer inhibitor (Hisashi Shinkai,
Motohide Sato, and Yuji Matsuzaki, Central Pharmaceutical Research
Institute, JT Inc., Takatsuki, Japan). Chapter 16. Conformationally
constrained tricyclic HIV integrase inhibitors (Maria Fardis, Haolun Jin,
Xiaowu Chen, Manuel Tsiang, James Chen, Choung Kim, Matthew Wright
(Gilead)). Chapter 17. Slow onset kinetics of HIV integrase inhibitors and
proposed molecular model (Edward P. Garvey and Benjamin Schwartz). Chapter
18. Azaindole hydroxamic acids are hiv-1 integrase inhibitors (Michael B.
Plewe, Ted W. Johnson). Chapter 19. A simple and accurate in vitro method
for predicting serum protein binding of hiv integrase strand transfer
inhibitors (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 (BMS)). Chapter 20. Role of metals in HIV-1
integrase inhibitor design (Mario Sechi, Mauro Carcelli, Dominga Rogolino
and Nouri Neamati). Chapter 21. Discovery and development of natural
product inhibitors of HIV-1 integrase (Sheo B. Singh (Merck)). Chapter 22.
Development of styrylquinoline integrase inhibitors (Jean-Francois
Mouscadet, Eric Deprez, Didier Desmaele, Jean d'Angelo (CNRS, France)).
Chapter 23. Dicaffeoyltartaric acid and dicaffeoylquinic acid HIV integrase
inhibitors (David c. Crosby and W. Edward Robinson, Jr. (UCI)). Chapter 24.
Design and discovery of peptide-based inhibitors (Ya-Qiu Long and Nouri
Neamati (Shanghai & USC)). Chapter 25. Nucleotide-Based Inhibitors of HIV
Integrase (Vasu Nair and Guochen Chi (U. Georgia)). Chapter 26. Design of
HIV-1 Integrase Inhibitors Using Computer-aided techniques (Erik Serrao,
Rambabu Gundla, Jinxia Deng, Srinivas Odde, Nouri Neamati (USC)). Chapter
27. Application of protein covalent modification to studying the structure
and function of HIV-1 integrase and its inhibitors (Xue Zhi Zhao and
Terrence R. Burke, Jr.). Chapter 28. HIV-1 intergase-DNA models (Chenzhong
Liao, Marc C. Nicklaus (NCI)). Chapter 29. A new paradigm for integrase
inhibition: blocking enzyme function without directly targeting the active
site (Laith Q. Al-Mawsawi and Nouri Neamati). Chapter 30. Resistance to
integrase inhibitors (Leen Hombrouck, Zeger Debyser and Myriam Witvrouw (KU
Leuven, Belgium)).