Coverart for item
The Resource Antitargets : prediction and prevention of drug side effects, edited by Roy J. Vaz and Thomas Klabunde

Antitargets : prediction and prevention of drug side effects, edited by Roy J. Vaz and Thomas Klabunde

Label
Antitargets : prediction and prevention of drug side effects
Title
Antitargets
Title remainder
prediction and prevention of drug side effects
Statement of responsibility
edited by Roy J. Vaz and Thomas Klabunde
Contributor
Subject
Language
eng
Cataloging source
NLM
Illustrations
illustrations
Index
index present
Literary form
non fiction
Nature of contents
bibliography
http://library.link/vocab/relatedWorkOrContributorName
  • Vaz, Roy J.
  • Klabunde, Thomas.
Series statement
Methods and principles in medicinal chemistry
Series volume
38
http://library.link/vocab/subjectName
  • Pharmaceutical Preparations
  • Cytochrome P-450 Enzyme System
  • Drug Design
  • Drug Interactions
  • Ion Channels
  • Receptors, G-Protein-Coupled
  • Drugs
  • Drugs
  • Drug interactions
  • Drug development
  • Drugs
Label
Antitargets : prediction and prevention of drug side effects, edited by Roy J. Vaz and Thomas Klabunde
Instantiates
Publication
Bibliography note
Includes bibliographical references and index
Carrier category
volume
Carrier category code
  • nc
Carrier MARC source
rdacarrier
Content category
text
Content type code
  • txt
Content type MARC source
rdacontent
Contents
Machine derived contents note: List of Contributors. -- Preface. -- A Personal Foreword. -- I General Aspects. -- 1 Why Drugs Fail -- A Study on Side Effects in New Chemical Entities (Daniela Schuster, Christian Laggner, Thierry Langer). -- 1.1 Introduction. -- 1.2 Drugs Withdrawn from the Market between 1992 and 2006 Listed Alphabetically. -- 1.3 Borderline Cases. -- 1.4 Investigational Drugs That Failed in Clinical Phases from 1992 to 2002. -- 1.5 Strategies for Avoiding Failure. -- 1.6 An Unusual Case: The Revival of Thalidomide. -- References. -- 2 Use of Broad Biological Profiling as a Relevant Descriptor to Describe and Differentiate Compounds: Structure-In Vitro (Pharmacology-ADME)-In Vivo (Safety) Relationships (Jonathan S. Mason, Jacques Migeon, Philippe Dupuis, Annie Otto-Bruc). -- 2.1 Introduction. -- 2.3 Structure-In Vitro Relationships. -- 2.4 Chemogenomic Analysis -- Target-Target Relationships. -- 2.5 In Vitro-In Vivo Relationships -- Placing Drug Candidates in the Context of BioPrint1. -- 2.6 A Perspective for the Future. -- References. -- II Antitargets: Ion Channels and GPCRs. -- 3 Pharmacological and Regulatory Aspects of QT Prolongation (Fabrizio De Ponti). -- 3.1 Introduction. -- 3.2 hERG: Target Versus Antitarget. -- 3.3 Pharmacology of QT Prolongation. -- 3.4 Significance of Drug-Induced QT Prolongation. -- 3.5 Regulatory Aspects of QT Prolongation. -- 3.6 Conclusions. -- References. -- 4 hERG Channel Physiology and Drug-Binding Structure-Activity Relationships (Sarah Dalibalta, John S. Mitcheson). -- 4.1 Introduction. -- 4.2 hERG Channel Structure. -- 4.3 hERG Potassium Channels and the Cardiac Action Potential. -- 4.4 Mutations in hERG Are Associated with Cardiac Arrhythmias. -- 4.5 Acquired Long QT Syndrome. -- 4.6 Drug-Binding Site of hERG. -- 4.7 Structural Basis for hERG Block. -- 4.8 Alternative Mechanisms of Block. -- 4.9 Role of Inactivation in hERG Block. -- 4.10 Inhibition of hERG Trafficking by Pharmacological Agents. -- 4.11 Computational Approaches to Predict hERG Kþ Channel Block. -- 4.12 Conclusions. -- References. -- 5 QSAR and Pharmacophores for Drugs Involved in hERG Blockage (Maurizio Recanatini, Andrea Cavalli). -- 5.1 Introduction. -- 5.2 Ligand-Based Models for hERG-Blocking Activity. -- 5.3 Ligand-Derived Models in the Light of the hERG Channel Structure. -- 5.4 Conclusions. -- References. -- 6 GPCR Antitarget Modeling: Pharmacophore Models to Avoid GPCR-Mediated Side Effects (Thomas Klabunde, Andreas Evers). -- 6.1 Introduction: GPCRs as Antitargets. -- 6.2 In Silico Tools for GPCR Antitarget Modeling. -- 6.3 GPCR Antitarget Pharmacophore Modeling: The a1a Adrenergic Receptor. -- 6.4 Summary. -- References. -- 7 The Emergence of Serotonin 5-HT2B Receptors as DRUG Antitargets (Vincent Setola, Bryan L. Roth). -- 7.1 Receptorome Screening to Identify Drug Targets and Antitargets. -- 7.2 Post-Receptorome Screening Data Implicate 5-HT2B Receptors in Drug-Induced VHD and PH. -- 7.3 Drug Structural Classes and VHD/PH. -- 7.4 Conclusions. -- References. -- 8 Computational Modeling of Selective Pharmacophores at the a1-Adrenergic Receptors (Francesca Fanelli, Pier G. De Benedetti). -- 8.1 Introduction. -- 8.2 Ligand-Based and Receptor-Based Pharmacophore Modeling and QSAR Analysis. -- 8.3 The General 1-AR Pharmacophore. -- 8.4 Modeling the a1-AR Subtype Selectivities of Different Classes of Antagonists. -- 8.5 Antitarget Modeling of Biogenic Amine-Binding GPCRs: Common Features and Subtle Differences
Control code
ocn192026518
Extent
xxiv, 480 p.
Isbn
9783527318216
Lccn
2008272820
Media category
unmediated
Media MARC source
rdamedia
Media type code
  • n
Other physical details
ill.
Label
Antitargets : prediction and prevention of drug side effects, edited by Roy J. Vaz and Thomas Klabunde
Publication
Bibliography note
Includes bibliographical references and index
Carrier category
volume
Carrier category code
  • nc
Carrier MARC source
rdacarrier
Content category
text
Content type code
  • txt
Content type MARC source
rdacontent
Contents
Machine derived contents note: List of Contributors. -- Preface. -- A Personal Foreword. -- I General Aspects. -- 1 Why Drugs Fail -- A Study on Side Effects in New Chemical Entities (Daniela Schuster, Christian Laggner, Thierry Langer). -- 1.1 Introduction. -- 1.2 Drugs Withdrawn from the Market between 1992 and 2006 Listed Alphabetically. -- 1.3 Borderline Cases. -- 1.4 Investigational Drugs That Failed in Clinical Phases from 1992 to 2002. -- 1.5 Strategies for Avoiding Failure. -- 1.6 An Unusual Case: The Revival of Thalidomide. -- References. -- 2 Use of Broad Biological Profiling as a Relevant Descriptor to Describe and Differentiate Compounds: Structure-In Vitro (Pharmacology-ADME)-In Vivo (Safety) Relationships (Jonathan S. Mason, Jacques Migeon, Philippe Dupuis, Annie Otto-Bruc). -- 2.1 Introduction. -- 2.3 Structure-In Vitro Relationships. -- 2.4 Chemogenomic Analysis -- Target-Target Relationships. -- 2.5 In Vitro-In Vivo Relationships -- Placing Drug Candidates in the Context of BioPrint1. -- 2.6 A Perspective for the Future. -- References. -- II Antitargets: Ion Channels and GPCRs. -- 3 Pharmacological and Regulatory Aspects of QT Prolongation (Fabrizio De Ponti). -- 3.1 Introduction. -- 3.2 hERG: Target Versus Antitarget. -- 3.3 Pharmacology of QT Prolongation. -- 3.4 Significance of Drug-Induced QT Prolongation. -- 3.5 Regulatory Aspects of QT Prolongation. -- 3.6 Conclusions. -- References. -- 4 hERG Channel Physiology and Drug-Binding Structure-Activity Relationships (Sarah Dalibalta, John S. Mitcheson). -- 4.1 Introduction. -- 4.2 hERG Channel Structure. -- 4.3 hERG Potassium Channels and the Cardiac Action Potential. -- 4.4 Mutations in hERG Are Associated with Cardiac Arrhythmias. -- 4.5 Acquired Long QT Syndrome. -- 4.6 Drug-Binding Site of hERG. -- 4.7 Structural Basis for hERG Block. -- 4.8 Alternative Mechanisms of Block. -- 4.9 Role of Inactivation in hERG Block. -- 4.10 Inhibition of hERG Trafficking by Pharmacological Agents. -- 4.11 Computational Approaches to Predict hERG Kþ Channel Block. -- 4.12 Conclusions. -- References. -- 5 QSAR and Pharmacophores for Drugs Involved in hERG Blockage (Maurizio Recanatini, Andrea Cavalli). -- 5.1 Introduction. -- 5.2 Ligand-Based Models for hERG-Blocking Activity. -- 5.3 Ligand-Derived Models in the Light of the hERG Channel Structure. -- 5.4 Conclusions. -- References. -- 6 GPCR Antitarget Modeling: Pharmacophore Models to Avoid GPCR-Mediated Side Effects (Thomas Klabunde, Andreas Evers). -- 6.1 Introduction: GPCRs as Antitargets. -- 6.2 In Silico Tools for GPCR Antitarget Modeling. -- 6.3 GPCR Antitarget Pharmacophore Modeling: The a1a Adrenergic Receptor. -- 6.4 Summary. -- References. -- 7 The Emergence of Serotonin 5-HT2B Receptors as DRUG Antitargets (Vincent Setola, Bryan L. Roth). -- 7.1 Receptorome Screening to Identify Drug Targets and Antitargets. -- 7.2 Post-Receptorome Screening Data Implicate 5-HT2B Receptors in Drug-Induced VHD and PH. -- 7.3 Drug Structural Classes and VHD/PH. -- 7.4 Conclusions. -- References. -- 8 Computational Modeling of Selective Pharmacophores at the a1-Adrenergic Receptors (Francesca Fanelli, Pier G. De Benedetti). -- 8.1 Introduction. -- 8.2 Ligand-Based and Receptor-Based Pharmacophore Modeling and QSAR Analysis. -- 8.3 The General 1-AR Pharmacophore. -- 8.4 Modeling the a1-AR Subtype Selectivities of Different Classes of Antagonists. -- 8.5 Antitarget Modeling of Biogenic Amine-Binding GPCRs: Common Features and Subtle Differences
Control code
ocn192026518
Extent
xxiv, 480 p.
Isbn
9783527318216
Lccn
2008272820
Media category
unmediated
Media MARC source
rdamedia
Media type code
  • n
Other physical details
ill.

Library Locations

    • Harold Cohen LibraryBorrow it
      Ashton Street, Liverpool, L69 3DA, GB
      53.418074 -2.967913
Processing Feedback ...