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Phosphodiesterases as Drug Targets

  • Book
  • © 2011

Overview

Editors:
  1. Sharron H. Francis

    1. School of Medicine, Dept. Molecular Physiology & Biophysics, Vanderbilt University, Nashville, USA

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    You can also search for this editor in PubMed   Google Scholar

  2. Marco Conti

    1. HSW 1656, Center for Reproductive Sciences, San Francisco, USA

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    You can also search for this editor in PubMed   Google Scholar

  3. Miles D. Houslay

    1. Wolfson Building, University of Glasgow, Glasgow, United Kingdom

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    You can also search for this editor in PubMed   Google Scholar

  • provides a summary of the major concepts related to the design and use of PDE inhibitors
  • describes exciting ideas and developments that are currently emerging in this dynamic and important field
  • written by leading authorities in the field
  • Includes supplementary material: sn.pub/extras

Part of the book series: Handbook of Experimental Pharmacology (HEP, volume 204)

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Table of contents (20 chapters)

  1. Front Matter

    Pages i-xvii
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  2. Phosphodiesterase Inhibitors: History of Pharmacology

    • Christian Schudt, Armin Hatzelmann, Rolf Beume, Hermann Tenor
    Pages 1-46

  3. Phosphodiesterase Inhibitors: Factors That Influence Potency, Selectivity, and Action

    • Sharron H. Francis, Miles D. Houslay, Marco Conti
    Pages 47-84

  4. Pharmacology, Clinical Efficacy, and Tolerability of Phosphodiesterase-4 Inhibitors: Impact of Human Pharmacokinetics

    • Hermann Tenor, Armin Hatzelmann, Rolf Beume, Gezim Lahu, Karl Zech, Thomas D. Bethke
    Pages 85-119

  5. Structural Insight into the Substrate Specificity of Phosphodiesterases

    • Hengming Ke, Huanchen Wang, Mengchun Ye
    Pages 121-134

  6. A Fission Yeast-Based Platform for Phosphodiesterase Inhibitor HTSs and Analyses of Phosphodiesterase Activity

    • Didem Demirbas, Ozge Ceyhan, Arlene R. Wyman, Charles S. Hoffman
    Pages 135-149

  7. The GAF-Tandem Domain of Phosphodiesterase 5 as a Potential Drug Target

    • Joachim E. Schultz, Torsten Dunkern, Elvira Gawlitta-Gorka, Gabriele Sorg
    Pages 151-166

  8. Small Molecule Allosteric Modulators of Phosphodiesterase 4

    • Mark E. Gurney, Alex B. Burgin, Olafur T. Magnusson, Lance J. Stewart
    Pages 167-192

  9. Regulation of Endothelial Barrier Function by Cyclic Nucleotides: The Role of Phosphodiesterases

    • James Surapisitchat, Joseph A. Beavo
    Pages 193-210

  10. Phosphodiesterases as Targets for Intermittent Claudication

    • Yongge Liu, Yasmin Shakur, Junichi Kambayashi
    Pages 211-236

  11. Phosphodiesterase Inhibition in Heart Failure

    • Matthew A. Movsesian, Rakesh C. Kukreja
    Pages 237-249

  12. Phosphodiesterases: Emerging Therapeutic Targets for Neonatal Pulmonary Hypertension

    • Kathryn N. Farrow, Robin H. Steinhorn
    Pages 251-277

  13. Role of Phosphodiesterases in Adult-Onset Pulmonary Arterial Hypertension

    • F. Murray, M. R. MacLean, P. A. Insel
    Pages 279-305

  14. Treatment of Erectile Dysfunction and Lower Urinary Tract Symptoms by Phosphodiesterase Inhibitors

    • Stefan Ückert, Christian G. Stief
    Pages 307-322

  15. Evaluation of the Therapeutic Utility of Phosphodiesterase 5A Inhibition in the mdx Mouse Model of Duchenne Muscular Dystrophy

    • Justin M. Percival, Candace M. Adamo, Joseph A. Beavo, Stanley C. Froehner
    Pages 323-344

  16. Phosphodiesterases as Targets for Modulating T-Cell Responses

    • Elisa Bjørgo, Kristine Moltu, Kjetil Taskén
    Pages 345-363

  17. Cyclic Nucleotides and Phosphodiesterases in Monocytic Differentiation

    • Angie L. Hertz, Joseph A. Beavo
    Pages 365-390

  18. Phosphodiesterase Inhibitors in the Treatment of Inflammatory Diseases

    • C. P. Page, D. Spina
    Pages 391-414

  19. Harnessing the Clinical Efficacy of Phosphodiesterase 4 Inhibitors in Inflammatory Lung Diseases: Dual-Selective Phosphodiesterase Inhibitors and Novel Combination Therapies

    • Mark A. Giembycz, Robert Newton
    Pages 415-446

  20. Phosphodiesterases in the Central Nervous System: Implications in Mood and Cognitive Disorders

    • Ying Xu, Han-Ting Zhang, James M. O’Donnell
    Pages 447-485
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Keywords

About this book

Cyclic nucleotide phosphodiesterases (PDEs) are promising targets for pharmacological intervention. Multiple PDE genes, isoform diversity, selective expression and compartmentation of the isoforms, and an array of conformations of PDE proteins are properties that challenge development of drugs that selectively target this class of enzymes. Novel characteristics of PDEs are viewed as unique opportunities to increase specificity and selectivity when designing novel compounds for certain therapeutic indications. This chapter provides a summary of the major concepts related to the design and use of PDE inhibitors.

Editors and Affiliations

  • School of Medicine, Dept. Molecular Physiology & Biophysics, Vanderbilt University, Nashville, USA

    Sharron H. Francis

  • HSW 1656, Center for Reproductive Sciences, San Francisco, USA

    Marco Conti

  • Wolfson Building, University of Glasgow, Glasgow, United Kingdom

    Miles D. Houslay

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