جزییات کتاب
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.Content: Chapter 1 HIV Life Cycle: Targets for Anti?HIV Agents (pages 1–14): Erik De ClercqChapter 2 pp32 Is Hot (pages 15–21): Duane P. GrandgenettChapter 3 Integrase Mechanism and Function (pages 23–33): Robert CraigieChapter 4 Structural Studies of Retroviral Integrases (pages 35–49): Mariusz Jaskolski, Jerry N. Alexandratos, Grzegorz Bujacz and Alexander WlodawerChapter 5 Retroviral Integration Target Site Selection (pages 51–65): Angela Ciuffi and Frederic BushmanChapter 6 Pleiotropic Nature of HIV?1 Integrase Mutations (pages 67–81): Alan EngelmanChapter 7 Insights into HIV?1 Integrase–DNA Interactions (pages 83–94): Allison Johnson, Christophe Marchand and Yves PommierChapter 8 Functional Interaction between Human Immunodeficiency Virus Type 1 Reverse Transcriptase and Integrase (pages 95–103): Thomas A. Wilkinson and Samson A. ChowChapter 9 Cellular Cofactors of HIV Integration (pages 105–129): Wannes Thys, Koen Bartholomeeusen, Zeger Debyser and Jan De RijckChapter 10 Structural aspects of Lentiviral Integrase–LEDGF Interaction (pages 131–140): Stephen Hare, Alan Engelman and Peter CherepanovChapter 11 Host Factors that affect Provirus Stability and Silencing (pages 141–150): Richard A. Katz, Rene Daniel and Anna Marie SkalkaChapter 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 DebyserChapter 13 HIV?1 Integrase Inhibitor Design: Overview and Historical Perspectives (pages 165–196): Nouri NeamatiChapter 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 SummaChapter 15 Elvitegravir: Novel Quinolone HIV?1 Integrase Strand Transfer Inhibitor (pages 231–238): Hisashi Shinkai, Motohide Sato and Yuji MatsuzakiChapter 16 Conformationally Constrained Tricyclic HIV Integrase Inhibitors (pages 239–254): Maria Fardis, Haolun Jin, Xiaowu Chen, Manuel Tsiang, James Chen, Choung Kim and Matthew WrightChapter 17 Slow?Onset Kinetics of HIV Integrase Inhibitors and Proposed Molecular Model (pages 255–263): Edward P. Garvey and Benjamin SchwartzChapter 18 Azaindole Hydroxamic Acids are HIV?1 Integrase Inhibitors (pages 265–274): Michael B. Plewe and Ted W. JohnsonChapter 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 KrystalChapter 20 Role of Metals in HIV?1 Integrase Inhibitor Design (pages 287–307): Mario Sechi, Mauro Carcelli, Dominga Rogolino and Nouri NeamatiChapter 21 Discovery and Development of Natural Product Inhibitors of HIV?1 Integrase (pages 309–323): Sheo B. SinghChapter 22 Development of Styrylquinoline Integrase Inhibitors (pages 325–339): Jean?Francois Mouscadet, Eric Deprez, Didier Desmaele and Jean D'AngeloChapter 23 Dicaffeoyltartaric Acid and Dicaffeoylquinic Acid HIV Integrase Inhibitors (pages 341–362): David C. Crosby and W. Edward RobinsonChapter 24 Design and Discovery of Peptide?Based HIV?1 Integrase Inhibitors (pages 363–377): Ya?Qiu Long and Nouri NeamatiChapter 25 Nucleotide?Based Inhibitors of HIV Integrase (pages 379–388): Vasu Nair and Guochen ChiChapter 26 Computer?Aided Techniques in Design of HIV?1 Integrase Inhibitors (pages 389–413): Erik Serrao, Rambabu Gundla, Jinxia Deng, Srinivas Odde and Nouri NeamatiChapter 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. BurkeChapter 28 HIV?1 Integrase–DNA Models (pages 429–455): Chenzhong Liao and Marc C. NicklausChapter 29 New Paradigm for Integrase Inhibition: Blocking Enzyme Function without Directly Targeting the Active Site (pages 457–476): Laith Q. Al?Mawsawi and Nouri NeamatiChapter 30 Resistance to Inhibitors of HIV?1 Integrase (pages 477–498): Anneleen Hombrouck, Reginald Clayton, Arnout Voet, Myriam Witvrouw and Zeger Debyser