G Protein-coupled Receptors: Molecular Pharmacology / Edition 1

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G protein-coupled receptors (GPCRs) are membrane proteins that transduce a vast array of extracellular signals into intracellular reactions ranging from cell-cell communication processes to physiological responses. They play an important role in a variety of diseases from cancer and diabetes, to neurodegenerative, inflammatory and respiratory disorders. GPCRs are therefore of utmost interest in drug development: over half of all prescription drugs currently on the market act by targeting these receptors directly or indirectly.

G Protein-coupled Receptors - Molecular Pharmacology provides a clear summary of the current knowledge in this fast-evolving field. The book sets out with an introduction to signalling molecules and their receptors, and an overview of the technical approaches used to investigate these interactions. Structural, functional and especially pharmacological aspects of GPCRs are then discussed in more detail and much attention is devoted to the analysis and interpretation of experimental data. The now widespread use of recombinant cell lines, receptor mutants and related artifices in drug research is critically evaluated. Special attention is also devoted to topical but often poorly understood concepts, such as insurmountable antagonism, inverse agonism and allosteric interactions.

By combining general information with the major state-of-the-art concepts in GPCR research, the book equips the reader with the necessary background for understanding and critically evaluating the current literature.

Written by two experts from academia and industry, G Protein-coupled Receptors - Molecular Pharmacology offers a unique view of academic and applied approaches aiming toreveal new ideas in pharmaceutical research.

The book will be of interest to anyone involved in drug development and preclinical research and those who need to function within multi-disciplinary teams in the pharmaceutical industry: from investigators to product managers or clinicians who seek to have a broad mechanistic understanding of drug-receptor interactions. Final year undergraduate and postgraduate students in pharmacology and cell and molecular biology will also find the book an invaluable resource.

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Product Details

  • ISBN-13: 9780470516478
  • Publisher: Wiley, John & Sons, Incorporated
  • Publication date: 1/18/2008
  • Edition number: 1
  • Pages: 264
  • Product dimensions: 6.83 (w) x 9.80 (h) x 0.69 (d)

Meet the Author

Georges Vauquelin. Department of Molecular and Biochemical Pharmacology, Free University Brussels (VUB), Belgium

Bengt von Mentzer. Department of Molecular Pharmacology, AstraZeneca Inc, Sweden

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Table of Contents

Preface     xi
Foreword     xii
Chemical messengers and the cell membrane     1
Endocrine signalling by hormones     1
The nervous system and synaptic signalling by neurotransmitters     8
Small molecule neurotransmitters     11
Neuropeptides     13
Paracrine signalling by local chemical messengers     15
Hydrophobicity: effect on release and transport of messengers     16
Membrane proteins and membrane receptors     23
Ligand-receptor interactions     25
Radioliogand binding studies     29
Technical aspects of radioligand binding     29
Saturation binding     33
Competition binding     38
Kinetic experiments     46
Regional distribution of receptors     50
Functional studies     53
Dose-response curves and associated problems     53
From receptor occupation to stimulus and response     56
From receptor occupation to stimulus     56
From stimulus to response: linear relationship     59
From stimulus to response: non-linear relationship     61
Receptor classification and antagonist affinity     65
Pharmacological models     69
G protein-coupled receptors     77
From receptor to response: introduction to GPCRs     77
GPCR structure     86
Ligand interactions with family A, B and C receptors     97
Ligand interaction with family A receptors     98
Ligand interaction with family B receptors     102
Ligand interaction with family C receptors     104
Receptor activation     106
Activated GPCRs: interaction with G proteins     113
Techniques to study G protein-coupling preference     119
Divergence of intracellular signalling     123
Activated GPCRs: phosphorylation and internalization     125
Receptor phosphorylation     125
[beta]-Arrestin binding mediated GPCR endocytosis     129
Mechanisms to terminate signalling     134
[beta]-Arrestin-binding and MAP kinase activation     137
GPCR dimerization and association with other proteins     142
Introductory comments     142
GRCR dimerization     143
GRCR interaction with other membrane receptors     151
GPCR interaction with other membrane proteins     152
GPCR interactions with cytoplasmic proteins     156
Early models for GPCR activation      159
Restricted GPCR mobility and G protein coupling     163
Membrane compartimentalization     163
Restricted GPCR-G protein coupling: effector activity     173
Spontaneous receptor-G protein coupling     175
Models     175
Inverse agonism     179
Interaction of two G proteins with one activated receptor state     183
Fusion proteins between GPCRs and G proteins     185
Multiple receptor conformations     191
'Agonist trafficking': what do models predict?     196
Experimental 'evidence' for agonist trafficking: potential pitfalls     198
Multistate receptors: ligand-mediated sequential changes in receptor conformation     201
Multiple receptor states related to truncation, covalent modification and mutation     204
Multistate receptors and multiple ligand binding sites     207
The general allosteric ternary complex model     210
Exogenous and endogenous allosteric modulators     212
allosteric phenomena at GPCR: detection by radioligand binding     214
Detection of allosteric phenomena at GPCRs by functional assays     219
Usefulness of allosteric modulators     222
'Competitive', 'non-competitive' and 'insurmountable' antagonism      222
Co-incubation, no receptor reserve     222
Antagonist pre-incubation, no receptor reserve     224
Naturally occurring mutations of GPCRs     226
Concluding remarks     231
References     235
Index     244
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