Functional selectivity of G protein-coupled receptor ligands : new opportunities for drug discovery / edited by Kim Neve.

Format:

Book

Contributor:

Neve, Kim A.

Series:

Receptors (Series)

The receptors

Language:

English

Subjects (All):

G proteins.

Ligands (Biochemistry).

Drug receptors.

GTP-Binding Proteins.

Ligands.

Receptors, Drug.

Medical Subjects:

GTP-Binding Proteins.

Ligands.

Receptors, Drug.

Physical Description:

x, 290 pages, 2 unnumbered pages of plates : illustrations (partly color) ; 25 cm.

Place of Publication:

[New York, NY] : Humana, [2009]

Summary:

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 Receptor Ligands, expert neuroscientists and pharmacologists reviewed 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 G protein-coupled receptors (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 Receptor Ligands is a valuable educational tool and reference source for students and scientists interested in drug development, chemical biology, and GPCR function.

Contents:

Part I Theoretical And Mechanistic Aspects Of Functional Selectivity

1 Historical Overview of the Concept of Functional Selectivity / Bryan L. Roth 3

2 Functional Selectivity: Theoretical Considerations and Future Directions / Terry Kenakin 9

3 Agonist-Selective Coupling of G Protein-Coupled Receptors / Barbara Bosier, Emmanuel Hermans 25

4 Ligand-Selective Receptor Desensitization and Endocytosis / Jennifer L. Whistler 55

5 Selectivity for G Protein or Arrestin-Mediated Signaling / Laura M. Bohn 71

6 In Vivo Evidence for and Consequences of Functional Selectivity / Kim A. Neve, Marc G. Caron, Jean-Martin Beaulieu 87

Part II Subfamilies Of Therapeutically Relevant Receptors

7 Functional Selectivity at Adrenergic Receptors / Richard R. Neubig 107

8 Signaling Diversity Mediated by Muscarinic Acetylcholine Receptor Subtypes and Evidence for Functional Selectivity / R.A. John Challiss, Rachel L. Thomas 125

9 Functional Selectivity at Serotonin Receptors / Kelly A. Berg, William P. Clarke 155

10 Functional Selectivity at Dopamine Receptors / Richard B. Mailman, Yan-Min Wang, Andrew Kant, Justin Brown 177

11 Functional Selectivity at Receptors for Cannabinoids and Other Lipids / Allyn C. Howlett 211

12 Functional Selectivity at Opioid Receptors / Graciela Pineyro 243

13 Functional Selectivity at Non-Opioid Peptide Receptors / Anushree Bhatnagar, Sadashiva Karnik 267.

Notes:

Includes bibliographical references and index.

ISBN:

9781603273343

1603273344

OCLC:

295000902