The Receptors

Functional Selectivity of G Protein-Coupled Receptor Ligands

New Opportunities for Drug Discovery

Editors: Neve, Kim (Ed.)

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About this book

Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique combinations; that is, one drug can be an agonist at pathway A and an antagonist or partial agonist at pathway B, and another drug can have the reverse profile. Functional selectivity has profound implications for drug development, for chemical biology, and for the design of experiments to characterize receptor function. In Functional Selectivity of G Protein-Coupled Receptors expert neuroscientists and pharmacologists review the work that demonstrated the existence of functional selectivity, placed it within a theoretical framework, and provided a mechanistic basis for the phenomenon. This exciting, comprehensive, and future-oriented volume includes chapters that focus on theoretical and mechanistic aspects of functional selectivity and that cut across subfamilies of GPCRs. Additional chapters focus on subfamilies of therapeutically relevant receptors where there is considerable evidence of ligand functional selectivity. Accessible and authoritative, Functional Selectivity of G Protein-Coupled Receptors is a valuable educational tool and reference source for students and scientists interested in drug development, chemical biology, and GPCR function.

Reviews

From the reviews:

“This book presents the current status of knowledge about ligand-specific intracellular signaling. … This book will be of greatest interest and utility to scientists actively involved in research into G protein-coupled receptors or drug discovery. … This is a … thorough, and detailed assessment of the current state of knowledge and recent developments in the field of G protein-coupled receptor function, signaling, and pharmacology.” (Beth Levant, Doody’s Review Service, December, 2009)

“Gives a comprehensive overview on all aspects of the functional selectivity concept of GPCR ligands … . It will help to generate more awareness for a key topic within the research community. … the volume at hand is of great educational benefit. … In general, the volume under review can be considered an excellent book … . can be an excellent companion for researchers just jumping into the field of GPCR agonist research, as well as for the expert scientist in the field.” (Christoph Boss, ChemMedChem, Vol. 5, 2010)


Table of contents (13 chapters)

  • Functional Selectivity at Non-Opioid Peptide Receptors

    Bhatnagar, Anushree (et al.)

    Pages 1-15

  • Historical Overview of the Concept of Functional Selectivity

    Roth, Bryan L.

    Pages 3-7

  • Functional Selectivity: Theoretical Considerations and Future Directions

    Kenakin, Terry

    Pages 9-24

  • Agonist-Selective Coupling of G Protein-Coupled Receptors

    Bosier, Barbara (et al.)

    Pages 25-53

  • Ligand-Selective Receptor Desensitization and Endocytosis

    Whistler, Jennifer L.

    Pages 55-69

Buy this book

eBook $199.00
price for USA (gross)
  • ISBN 978-1-60327-335-0
  • Digitally watermarked, DRM-free
  • Included format: EPUB, PDF
  • ebooks can be used on all reading devices
  • Immediate eBook download after purchase
Hardcover $259.00
price for USA
  • ISBN 978-1-60327-334-3
  • Free shipping for individuals worldwide
  • Online orders shipping within 2-3 days.
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Bibliographic Information

Bibliographic Information
Book Title
Functional Selectivity of G Protein-Coupled Receptor Ligands
Book Subtitle
New Opportunities for Drug Discovery
Editors
  • Kim Neve
Series Title
The Receptors
Copyright
2009
Publisher
Humana Press
Copyright Holder
Humana Press
eBook ISBN
978-1-60327-335-0
DOI
10.1007/978-1-60327-335-0
Hardcover ISBN
978-1-60327-334-3
Edition Number
1
Number of Pages
X, 292
Topics