G Protein-Coupled Receptors as Drug Targets: Analysis of Activation and Constitutive Activity (Methods and Principles in Medicinal Chemistry)

With its particular emphasis on the constitutive activity of G-protein-coupled receptors (GPCRs)s, this book comprehensively discusses an important biological process that has not yet been covered in such depth in any other existing books on GPCRs. The international team of highly distinguished authors addresses in detail current models and concepts, to introduce medicinal chemists, physiologists, pharmacologists, and medical researchers into the advances in the understanding of GPCR activation and constitutive activity. In addition, the book provides an overview on methods of investigating constitutive GPCR activity. The text is well illustrated by selected experimental data and schemes._The chaptes are all cross-referenced with each other and cover general mechnisms, methodological approaches and cover selected important GPCR sysstems, the consequences for drug action, including, side effects, and rational drug design for GPCR targets. A highly recommended reference for researchers in academia and industry. authors addresses in detail current models and concepts, so as to introduce pharmaceutical chemists, physiologists and medical researchers to the advances in the understanding of GPCR activation and constitutive activity, and provides an overview of the methods of investigating GPCR activity. The text is backed by abundant case studies and methodological advice for analyzing GPCRs, covering selected pharmacologically relevant GPCR systems, the consequences for drug action, including unwanted side effects, and rational drug design for GPCR targets. A highly practical reference for researchers in academia and industry.

g Protein-coupled Receptors (gpcrs) Are Important Conformational Switches In Transmembrane Signal Transduction And Represent The Largest Gene Family In The Human Genome Reflecting The Importance Of Gpcrs As Targets For Hormones, Neurotransmitters And Local Mediators In Virtually Any Cell Type Of The Human Body. Since Gpcrs Discriminate Well Between Natural And Synthetic Ligands And Because Of Their Localization In The Plasma Membrane, They Are The Single Most Important Class Of Drug Targets.

with Its Particular Emphasis On The Constitutive Activity Of Gpcrs, This Book Recognizes A Biological Process That Has Not Yet Been Covered By Existing Books On Gpcrs. An International Team Of Highly Distinguished Authors Discusses Current Models And Concepts In Detail, Introducing The Advances Made In Our Understanding Gpcr Activation And Constitutive Activity. In Addition, The Text Provides An Overview On The Methods Of Investigating Gpcr Activity.

from The Contents:

part I: General Concepts

models Of Constitutive Activity

molecular Mechanisms Of Gpcr Activation

impact Of G Proteins On Constitutive Gpcr Activity

physiological And Therapeutic Relevance Of Constitutive Gpcr Activity

methodological Approaches

part Ii: Selected Gpcr Systems

chemokine Receptors And Human Disease

α-adrenoceptors

β-adrenoceptors

muscarinic Acetylcholine Receptors

histamine Receptors

5-ht Receptors

virally Pirated Chemokine Receptors And Human Disease

illustrated By Numerous Experimental Examples, Schemes And Methodological Advice For Analyzing Gpcrs, This Is A Highly Practical Reference For Pharmaceutical Chemists, Physiologists And Medical Researchers In Academia And Industry.

"Illustrated by numerous experimental examples and schemes, and methodological advice for analyzing constitutive activity of GPCRs, this is a highly practical reference for pharmaceutical chemists, physiologists and medical researchers in academia and industry."--Jacket This highly recommended reference for researchers in academia and industry introduces current models and concepts, while providing an overview of the methods of investigating constitutive GPCR activity. Well illustrated with experimental data and schemes.