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.
Recenzijos
This book will be certainly a valuable reference source for all those who are interested in antiviral drug discovery. All of the information contained in this text offers a rich scientific support for researchers in academia and industry at any level who are interested in enhancing their knowledge on a very fascinating scientific topic. (ChemMedChem, 2012)
| Preface |
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ix | |
| Contributors |
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xi | |
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1 HIV Life Cycle: Targets for Anti-HIV Agents |
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1 | (14) |
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15 | (8) |
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3 Integrase Mechanism and Function |
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23 | (12) |
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4 Structural Studies of Retroviral Integrases |
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35 | (16) |
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5 Retroviral Integration Target Site Selection |
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51 | (16) |
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6 Pleiotropic Nature of HIV-1 Integrase Mutations |
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67 | (16) |
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7 Insights into HIV-1 Integrase-DNA Interactions |
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83 | (12) |
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8 Functional Interaction Between Human Immunodeficiency Virus Type 1 Reverse Transcriptase and Integrase |
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95 | (10) |
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9 Cellular Cofactors of HIV Integration |
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105 | (26) |
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10 Structural Aspects of Lentiviral Integrase-LEDGF Interaction |
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131 | (10) |
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11 Host Factors that Affect Provirus Stability and Silencing |
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141 | (10) |
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12 Assays for Evaluation of HIV-1 Integrase Enzymatic Activity, DNA Binding, and Cofactor Interaction |
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151 | (14) |
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13 HIV-1 Integrase Inhibitor Design: Overview and Historical Perspectives |
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165 | (32) |
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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 |
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197 | (34) |
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15 Elvitegravir: Novel Quinolone HIV-1 Integrase Strand Transfer Inhibitor |
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231 | (8) |
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16 Conformationally Constrained Tricyclic HIV Integrase Inhibitors |
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239 | (16) |
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17 Slow-Onset Kinetics of HIV Integrase Inhibitors and Proposed Molecular Model |
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255 | (10) |
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18 Azaindole Hydroxamic Acids Are HIV-1 Integrase Inhibitors |
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265 | (10) |
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19 Simple and Accurate In Vitro Method for Predicting Serum Protein Binding of HIV Integrase Strand Transfer Inhibitors |
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275 | (12) |
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20 Role of Metals in HIV-1 Integrase Inhibitor Design |
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287 | (22) |
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21 Discovery and Development of Natural Product Inhibitors of HIV-1 Integrase |
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309 | (16) |
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22 Development of Styrylquinoline Integrase Inhibitors |
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325 | (16) |
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23 Dicaffeoyltartaric Acid and Dicaffeoylquinic Acid HIV Integrase Inhibitors |
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341 | (22) |
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24 Design and Discovery of Peptide-Based HIV-1 Integrase Inhibitors |
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363 | (16) |
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25 Nucleotide-Based Inhibitors of HIV Integrase |
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379 | (10) |
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26 Computer-Aided Techniques in Design of HIV-1 Integrase Inhibitors |
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389 | (26) |
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27 Application of Protein Covalent Modification to Studying Structure and Function of HIV-1 Integrase and Its Inhibitors |
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415 | (14) |
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28 HIV-1 Integrase-DNA Models |
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429 | (28) |
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29 New Paradigm for Integrase Inhibition: Blocking Enzyme Function Without Directly Targeting the Active Site |
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457 | (20) |
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30 Resistance to Inhibitors of HIV-1 Integrase |
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477 | (22) |
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| Index |
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499 | |
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.
