Allosteric Receptor Modulation in Drug Targeting
Allosteric Receptor Modulation in Drug Targeting

Author: Norman G. Bowery

Publisher: CRC Press

Published: 2006-06-19

Total Pages: 376

ISBN-13: 9780824727918

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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.

Allosteric Receptor Modulation in Drug Targeting
Allosteric Receptor Modulation in Drug Targeting

Author: Norman G. Bowery

Publisher: CRC Press

Published: 2016-04-19

Total Pages: 378

ISBN-13: 1420016180

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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 th

Allosterism in Drug Discovery
Allosterism in Drug Discovery

Author: Dario Doller

Publisher: Royal Society of Chemistry

Published: 2016-11-24

Total Pages: 458

ISBN-13: 1782624597

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Although the concept of allosterism has been known for over half a century, its application in drug discovery has exploded in recent years. The emergence of novel technologies that enable molecular-level ligand-receptor interactions to be studied in studied in unprecedented detail has driven this trend. This book, written by the leaders in this young research area, describes the latest developments in allosterism for drug discovery. Bringing together research in a diverse range of scientific disciplines, Allosterism in Drug Discovery is a key reference for academics and industrialists interested in understanding allosteric interactions. The book provides an in-depth review of research using small molecules as chemical probes and drug candidates that interact allosterically with proteins of relevance to life sciences and human disease. Knowledge of these interactions can then be applied in the discovery of the novel therapeutics of the future. This book will be useful for people working in all disciplines associated with drug discovery in academia or industry, as well as postgraduate students who may be working in the design of allosteric modulators.

Extrasynaptic GABAA Receptors
Extrasynaptic GABAA Receptors

Author: Adam C. Errington

Publisher: Springer

Published: 2014-09-22

Total Pages: 301

ISBN-13: 149391426X

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GABA is the principal inhibitory neurotransmitter in the CNS and acts via GABAA and GABAB receptors. Recently, a novel form of GABAA receptor-mediated inhibition, termed “tonic” inhibition, has been described. Whereas synaptic GABAA receptors underlie classical “phasic” GABAA receptor-mediated inhibition (inhibitory postsynaptic currents), tonic GABAA receptor-mediated inhibition results from the activation of extrasynaptic receptors by low concentrations of ambient GABA. Extrasynaptic GABAA receptors are composed of receptor subunits that convey biophysical properties ideally suited to the generation of persistent inhibition and are pharmacologically and functionally distinct from their synaptic counterparts. This book highlights ongoing work examining the properties of recombinant and native extrasynaptic GABAA receptors and their preferential targeting by endogenous and clinically relevant agents. In addition, it emphasizes the important role of extrasynaptic GABAA receptors in GABAergic inhibition throughout the CNS and identifies them as a major player in both physiological and pathophysiological processes.

Allosteric Modulation of G Protein-Coupled Receptors
Allosteric Modulation of G Protein-Coupled Receptors

Author: Robert Laprairie

Publisher: Academic Press

Published: 2022-02-05

Total Pages: 214

ISBN-13: 0128197722

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Allosteric Modulation of G Protein-Coupled Receptors reviews fundamental information on G protein-coupled receptors (GPCRs) and allosteric modulation, presenting original research in the area and collectively providing a comprehensive description of key issues in GPCR allosteric modulation. The book provides background on core concepts of molecular pharmacology while also introducing the most important advances and studies in the area. It also discusses key methodologies. This is an essential book for researchers and advanced students engaged in pharmacology, toxicology and pharmaceutical sciences training and research. Many of the GPCR-targeted drugs released in the past decade have specifically worked via allosteric mechanisms. Unlike direct orthosteric-acting compounds that occupy a similar receptor site to that of endogenous ligands, allosteric modulators alter GPCR-dependent signaling at a site apart from the endogenous ligand. Recent methodological and analytical advances have greatly improved our ability to understand the signaling mechanisms of GPCRs. We now know that allostery is a common regulatory mechanism for all GPCRs and not – as we once believed – unique to a few receptor subfamilies. - Introduces background on core concepts of molecular pharmacology, including statistical analyses, non-linear regression, complex models and GPCR-dependent signal transduction as they relate to allosteric modulation - Discusses critical advances and landmark studies, including discoveries in the area of GPCR allosteric modulation, which are reviewed for their importance in positive and negative regulation, protein-protein interactions, and small molecule drug discovery - Includes key methodologies used to study allosteric modulation at the in silico, in vitro, and in vivo levels of drug discovery and characterization

Protein Allostery in Drug Discovery
Protein Allostery in Drug Discovery

Author: Jian Zhang

Publisher: Springer Nature

Published: 2019-11-09

Total Pages: 386

ISBN-13: 9811387192

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The book focuses on protein allostery in drug discovery. Allosteric regulation, ʹthe second secret of lifeʹ, fine-tunes virtually most biological processes and controls physiological activities. Allostery can both cause human diseases and contribute to development of new therapeutics. Allosteric drugs exhibit unparalleled advantages compared to conventional orthosteric drugs, rendering the development of allosteric modulators as an appealing strategy to improve selectivity and pharmacodynamic properties in drug leads. The Series delineates the immense significance of protein allostery—as demonstrated by recent advances in the repertoires of the concept, its mechanistic mechanisms, and networks, characteristics of allosteric proteins, modulators, and sites, development of computational and experimental methods to predict allosteric sites, small-molecule allosteric modulators of protein kinases and G-protein coupled receptors, engineering allostery, and the underlying role of allostery in precise medicine. Comprehensive understanding of protein allostery is expected to guide the rational design of allosteric drugs for the treatment of human diseases. The book would be useful for scientists and students in the field of protein science and Pharmacology etc.

Biology of the NMDA Receptor
Biology of the NMDA Receptor

Author: Antonius M. VanDongen

Publisher: CRC Press

Published: 2008-10-29

Total Pages: 368

ISBN-13: 142004415X

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The NMDA receptor plays a critical role in the development of the central nervous system and in adult neuroplasticity, learning, and memory. Therefore, it is not surprising that this receptor has been widely studied. However, despite the importance of rhythms for the sustenance of life, this aspect of NMDAR function remains poorly studied. Written

Biased Signaling in Physiology, Pharmacology and Therapeutics
Biased Signaling in Physiology, Pharmacology and Therapeutics

Author: Brian J Arey

Publisher: Elsevier

Published: 2014-06-05

Total Pages: 317

ISBN-13: 0124115071

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Biased Signaling in Physiology, Pharmacology and Therapeutics is a unique and essential reference for the scientific community concerning how conformational-dependent activation is a common phenomenon across many classes of receptors or signaling molecules. It discusses the role of conformational dynamics in leading to signaling bias across different classes of receptors and signaling molecules. By providing a broader view of signaling bias, this resource helps to explain common mechanisms shared across receptor classes and how this can be utilized to elucidate their cellular activity and better understand their therapeutic potential. Written for both new and established scientists in pharmacology, cell biology, biochemistry, and signal transduction, as well as physicians, this book clearly illustrates how biased receptor signaling can be utilized to develop and understand complex pharmacology. Chapters are each focused on a specific class of receptor or other important topic and make use of real-world examples illustrating how the latest research in signal transduction has led to a better understanding of pharmacology and cell biology. This structure creates a basis for understanding that physiological signalling bias has been selected by nature in order to provide complex and tissue- specific biological responses in the face of limited receptors and signaling pathways. This book provides a framework to reveal that these physiological mechanisms are not restricted to one receptor type or family and thus presents receptor signaling from a newer, more global perspective. - Offers a unique and valuable resource on biased receptor signaling that provides a global view for better understanding pharmacology across many receptor families - Integrates biased receptor signaling, physiology, and pharmacology to place this emerging science within the context of treating disease - Includes important chapters on both the pharmaceutical and therapeutic implications of biased signaling

Structural Biology in Drug Discovery
Structural Biology in Drug Discovery

Author: Jean-Paul Renaud

Publisher: John Wiley & Sons

Published: 2020-01-09

Total Pages: 1437

ISBN-13: 1118900502

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With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins