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Overview
Offering a wide array of illustrations and tables in every chapter, this book extensively covers the principles of allosterism in reference to drug action and progresses to a detailed examination of individual ionotropic and G-protein coupled receptor systems-helping those new to the subject understand the importance of allosterism and providing those already working in the field with specific reference information. This title provides in-depth chapters on basic principles of allosterism and its significance at GABAA, 5HT3, nicotinic, and GABAB receptors, ionotropic and metabotropic receptors for glutamate, muscarinic receptors and alpha 2 adrenoceptors to provide a firm foundation to the subject.
Synopsis
Offering a wide array of illustrations and tables in every chapter, this book extensively covers the principles of allosterism in reference to drug action and progresses to a detailed examination of individual ionotropic and G-protein coupled receptor systems-helping those new to the subject understand the importance of allosterism and providing those already working in the field with specific reference information. This title provides in-depth chapters on basic principles of allosterism and its significance at GABAA, 5HT3, nicotinic, and GABAB receptors, ionotropic and metabotropic receptors for glutamate, muscarinic receptors and alpha 2 adrenoceptors to provide a firm foundation to the subject.
Doody Review Services
Reviewer:S.J. Enna, PhD(University of Kansas City School of Medicine)
Description:This multiauthored work contains a series of chapters describing the role of allosterism in regulating neurotransmitter receptor responses. An allosteric agent is one that binds to a portion of a receptor distinct from the neurotransmitter recognition component and in so doing increases or decreases the response to an agonist or antagonist acting at the orthosteric site. Particular emphasis is placed on characterizing the pharmacological and clinical importance of drug-induced allosteric modifications in transmitter systems.
Purpose:The aim of the book is to provide information that could be used to facilitate the design and development of allosteric modulators for regulating neurotransmitter receptor function. Such a book is a timely addition to the literature given the growing interest in this topic due to the increased appreciation of the clinical value of such agents. While the book has some shortcomings, overall it meets the objectives set forth by the editor.
Audience:While not explicitly stated, this book appears to be intended for neuroscientists engaged in drug discovery. Those with an interest in neuropharmacology, from advanced graduate students to senior scientists, will have no trouble understanding the material. All of the authors are recognized internationally as authorities in this field.
Features:The book is divided into three sections. The first, consisting of three chapters, covers historical and theoretical aspects of neurotransmitter receptor allosterism. The second section, which is composed of four chapters, details allosteric regulation of ionotrophic receptors, such as nicotinic cholinergic and GABA-A sites. The final six chapters are devoted to describing allosterism and G protein-coupled sites, including muscarinic cholinergic, GABA-B and metabotropic glutamate receptors. While some of the contributions focus on describing the basic properties of allosterism as they pertain to a particular system, others are more general overviews of the biochemical and pharmacological responses to agents known to allosterically modify the target site. In some cases detailed descriptions of structure-activity data are provided, which will be of particular interest to medicinal chemists. Virtually all chapters include mention of the clinical potential of allosteric modulators. Many will be surprised by the number and diversity of neurotransmitter receptor allosteric agents, both endogeneous and exogenous. The former includes zinc, sodium, calcium, some L-amino acids and steroids. Benzodiazepines, barbiturates, general anesthetics, both fixed and volatile, certain convulsants and anticonvulsants, and some drugs of abuse are representative xenobiotic allosteric modulators. As detailed in this book, it now appears that virtually all neurotransmitter receptors are subject to allosteric regulation, vastly increasing the number of target sites for drug discovery. Although the information is authoritative, and the authors leaders in the field, some of the offerings are somewhat dated, with literature citations only through 2003 or 2004, although other chapters include work published in 2006. Moreover, there is some redundancy with, for example, the allosteric properties of GABA-B receptors covered in two different chapters. Some might also question the rationale for devoting a chapter to alpha-2 adrenergic sites given the paucity of information on its allosteric regulation. It could also be argued that the value of this monograph would have been enhanced if a chapter had been devoted to describing high throughput screening techniques for identifying chemical entities that allosterically modify receptor systems. As noted in the book, ligand binding assays alone are inadequate for this purpose since a functional response must be measured. While selected assays are mentioned in individual offerings, a single chapter devoted to this topic would have been a useful addition.
Assessment:This book provides valuable theoretical and practical information on receptor allosterism and its potential importance in the design and development of novel therapeutics. It is a unique offering in stressing the importance of allosterism in drug discovery. This makes it a particularly important contribution for industrial and academic scientists and clinicians with an interest in new approaches for designing safer, more selective, and efficacious drugs.
Editorials
From The Critics
Reviewer: S.J. Enna, PhD(University of Kansas City School of Medicine)Description: This multiauthored work contains a series of chapters describing the role of allosterism in regulating neurotransmitter receptor responses. An allosteric agent is one that binds to a portion of a receptor distinct from the neurotransmitter recognition component and in so doing increases or decreases the response to an agonist or antagonist acting at the orthosteric site. Particular emphasis is placed on characterizing the pharmacological and clinical importance of drug-induced allosteric modifications in transmitter systems.
Purpose: The aim of the book is to provide information that could be used to facilitate the design and development of allosteric modulators for regulating neurotransmitter receptor function. Such a book is a timely addition to the literature given the growing interest in this topic due to the increased appreciation of the clinical value of such agents. While the book has some shortcomings, overall it meets the objectives set forth by the editor.
Audience: While not explicitly stated, this book appears to be intended for neuroscientists engaged in drug discovery. Those with an interest in neuropharmacology, from advanced graduate students to senior scientists, will have no trouble understanding the material. All of the authors are recognized internationally as authorities in this field.
Features: The book is divided into three sections. The first, consisting of three chapters, covers historical and theoretical aspects of neurotransmitter receptor allosterism. The second section, which is composed of four chapters, details allosteric regulation of ionotrophic receptors, such as nicotinic cholinergic and GABA-A sites. The final six chapters are devoted to describing allosterism and G protein-coupled sites, including muscarinic cholinergic, GABA-B and metabotropic glutamate receptors. While some of the contributions focus on describing the basic properties of allosterism as they pertain to a particular system, others are more general overviews of the biochemical and pharmacological responses to agents known to allosterically modify the target site. In some cases detailed descriptions of structure-activity data are provided, which will be of particular interest to medicinal chemists. Virtually all chapters include mention of the clinical potential of allosteric modulators. Many will be surprised by the number and diversity of neurotransmitter receptor allosteric agents, both endogeneous and exogenous. The former includes zinc, sodium, calcium, some L-amino acids and steroids. Benzodiazepines, barbiturates, general anesthetics, both fixed and volatile, certain convulsants and anticonvulsants, and some drugs of abuse are representative xenobiotic allosteric modulators. As detailed in this book, it now appears that virtually all neurotransmitter receptors are subject to allosteric regulation, vastly increasing the number of target sites for drug discovery. Although the information is authoritative, and the authors leaders in the field, some of the offerings are somewhat dated, with literature citations only through 2003 or 2004, although other chapters include work published in 2006. Moreover, there is some redundancy with, for example, the allosteric properties of GABA-B receptors covered in two different chapters. Some might also question the rationale for devoting a chapter to alpha-2 adrenergic sites given the paucity of information on its allosteric regulation. It could also be argued that the value of this monograph would have been enhanced if a chapter had been devoted to describing high throughput screening techniques for identifying chemical entities that allosterically modify receptor systems. As noted in the book, ligand binding assays alone are inadequate for this purpose since a functional response must be measured. While selected assays are mentioned in individual offerings, a single chapter devoted to this topic would have been a useful addition.
Assessment: This book provides valuable theoretical and practical information on receptor allosterism and its potential importance in the design and development of novel therapeutics. It is a unique offering in stressing the importance of allosterism in drug discovery. This makes it a particularly important contribution for industrial and academic scientists and clinicians with an interest in new approaches for designing safer, more selective, and efficacious drugs.