HIV-1 integrase : mechanism and inhibitor design / edited by Nouri Neamati.

Format:

Book

Contributor:

Neamati, Nouri.

Series:

Wiley Series in Drug Discovery and Development

Wiley series on drug discovery and development

Language:

English

Subjects (All):

HIV (Viruses)--Enzymes.

HIV (Viruses).

HIV (Viruses)--Enzymes--Inhibitors.

Antiviral agents.

Physical Description:

1 online resource (540 p.)

Edition:

1st ed.

Place of Publication:

Hoboken, N.J. : Wiley, c2011.

Language Note:

English

Summary:

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

Contents:

HIV-1 INTEGRASE: Mechanism and Inhibitor Design; CONTENTS; PREFACE; CONTRIBUTORS; 1 HIV Life Cycle: Targets for Anti-HIV Agents; 2 pp32 Is Hot; 3 Integrase Mechanism and Function; 4 Structural Studies of Retroviral Integrases; 5 Retroviral Integration Target Site Selection; 6 Pleiotropic Nature of HIV-1 Integrase Mutations; 7 Insights into HIV-1 Integrase-DNA Interactions; 8 Functional Interaction Between Human Immunodeficiency Virus Type 1 Reverse Transcriptase and Integrase; 9 Cellular Cofactors of HIV Integration; 10 Structural Aspects of Lentiviral Integrase-LEDGF Interaction

11 Host Factors that Affect Provirus Stability and Silencing12 Assays for Evaluation of HIV-1 Integrase Enzymatic Activity, DNA Binding, and Cofactor Interaction; 13 HIV-1 Integrase Inhibitor Design: Overview and Historical Perspectives; 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; 15 Elvitegravir: Novel Quinolone HIV-1 Integrase Strand Transfer Inhibitor; 16 Conformationally Constrained Tricyclic HIV Integrase Inhibitors

17 Slow-Onset Kinetics of HIV Integrase Inhibitors and Proposed Molecular Model18 Azaindole Hydroxamic Acids Are HIV-1 Integrase Inhibitors; 19 Simple and Accurate In Vitro Method for Predicting Serum Protein Binding of HIV Integrase Strand Transfer Inhibitors; 20 Role of Metals in HIV-1 Integrase Inhibitor Design; 21 Discovery and Development of Natural Product Inhibitors of HIV-1 Integrase; 22 Development of Styrylquinoline Integrase Inhibitors; 23 Dicaffeoyltartaric Acid and Dicaffeoylquinic Acid HIV Integrase Inhibitors; 24 Design and Discovery of Peptide-Based HIV-1 Integrase Inhibitors

25 Nucleotide-Based Inhibitors of HIV Integrase26 Computer-Aided Techniques in Design of HIV-1 Integrase Inhibitors; 27 Application of Protein Covalent Modification to Studying Structure and Function of HIV-1 Integrase and Its Inhibitors; 28 HIV-1 Integrase-DNA Models; 29 New Paradigm for Integrase Inhibition: Blocking Enzyme Function Without Directly Targeting the Active Site; 30 Resistance to Inhibitors of HIV-1 Integrase; INDEX; Colour Plates; Wiley Series in Drug Discovery and Development

Notes:

Description based upon print version of record.

Includes bibliographical references and index.

ISBN:

9781118015360

1118015363

9781118015377

1118015371

9781118015353

1118015355

OCLC:

757827332