Synthesis Of Novel Allosteric Modulators Of The G Protein Coupled Receptor Cb1

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Allosteric Modulation of G Protein-Coupled Receptors

Author : Robert Laprairie
Publisher : Academic Press
ISBN 13 : 0128197722
Total Pages : 214 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Allosteric Modulation of G Protein-Coupled Receptors by : Robert Laprairie

Download or read book Allosteric Modulation of G Protein-Coupled Receptors written by Robert Laprairie and published by Academic Press. This book was released on 2022-02-05 with total page 214 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Phytocannabinoids

Author : A. Douglas Kinghorn
Publisher : Springer
ISBN 13 : 3319455419
Total Pages : 137 pages
Book Rating : 4.3/5 (194 download)

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Book Synopsis Phytocannabinoids by : A. Douglas Kinghorn

Download or read book Phytocannabinoids written by A. Douglas Kinghorn and published by Springer. This book was released on 2017-01-24 with total page 137 pages. Available in PDF, EPUB and Kindle. Book excerpt: The book presents the current state of the art on phytocannnabinoid chemistry and pharmacology and will be of much use to those wishing to understand the current landscape of the exciting and intriguing phytocannabinoid science. The focus is on natural product cannabinoids which have been demonstrated to act at specific receptor targets in the CNS.

Handbook of Cannabis and Related Pathologies

Author : Victor R Preedy
Publisher : Academic Press
ISBN 13 : 012800827X
Total Pages : 1382 pages
Book Rating : 4.1/5 (28 download)

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Book Synopsis Handbook of Cannabis and Related Pathologies by : Victor R Preedy

Download or read book Handbook of Cannabis and Related Pathologies written by Victor R Preedy and published by Academic Press. This book was released on 2016-12-31 with total page 1382 pages. Available in PDF, EPUB and Kindle. Book excerpt: Handbook of Cannabis and Related Pathologies: Biology, Pharmacology, Diagnosis, and Treatment is the first book to take an interdisciplinary approach to the understanding of cannabis use and misuse. Recent worldwide trends toward decriminalizing marijuana for medical use have increased legal use of the drug and recreational use remains high, making cannabis one of the most commonly used drugs. Cannabis has a wide range of adverse neurological effects, and use and abuse can lead to physical, social, and psychopathological issues that are multifarious and complex. Effective understanding and treatment requires knowledge of the drug's effects from across scientific disciplines. This book provides an overview of the biological and pharmacological components of the cannabis plant, outlines its neurological, social, and psychopathological effects, assists in the diagnosis and screening for use and dependency, and aids researchers in developing effective treatments for cannabis-related issues and disorders. Fully illustrated, with contributions from internationally recognized experts, it is the go-to resource for neuroscientists, pharmacologists, pathologists, public-health workers, and any other researcher who needs an in-depth and cross-disciplinary understanding of cannabis and its effects. - Comprehensive chapters include an abstract, key facts, mini dictionary of terms, and summary points - Presents illustrations with at least six figures, tables, and diagrams per chapter - Provides a one-stop-shopping synopsis of everything to do with cannabis and its related pathology, from chemicals and cells, individuals and communities, and diagnosis and treatment - Offers an integrated and informed synopsis of the complex issues surrounding cannabis as a substance, its use, and its misuse

GPCRs

Author : Beata Jastrzebska
Publisher : Academic Press
ISBN 13 : 0128167289
Total Pages : 502 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis GPCRs by : Beata Jastrzebska

Download or read book GPCRs written by Beata Jastrzebska and published by Academic Press. This book was released on 2019-09-11 with total page 502 pages. Available in PDF, EPUB and Kindle. Book excerpt: GPCRS: Structure, Function, and Drug Discovery provides a comprehensive overview of recent discoveries and our current understanding of GPCR structure, signaling, physiology, pharmacology and methods of study. In addition to the fundamental aspects of GPCR function and dynamics, international experts discuss crystal structures, GPCR complexes with partner proteins, GPCR allosteric modulation, biased signaling through protein partners, deorphanization of GPCRs, and novel GPCR-targeting ligands that could lead to the development of new therapeutics against human diseases. GPCR association with, and possible therapeutic pathways for, retinal degenerative diseases, Alzheimer's disease, Parkinson's disease, cancer and diabetic nephropathy, among other illnesses, are examined in-depth. - Addresses our current understanding and novel advances in the GPCR field, directing readers towards recent finding of key significance for translational medicine - Combines a thorough discussion of structure and function of GPCRs with disease association and drug discovery - Features chapter contributions from international experts in GPCR structure, signaling, physiology and pharmacology

Cannabinoids and Their Receptors

Author :
Publisher : Academic Press
ISBN 13 : 0128121572
Total Pages : 562 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Cannabinoids and Their Receptors by :

Download or read book Cannabinoids and Their Receptors written by and published by Academic Press. This book was released on 2017-07-24 with total page 562 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cannabinoids and Their Receptors, Volume 593, the latest release in the Methods in Enzymology series, continues the legacy of this premier serial with quality chapters authored by leaders in the field. This updated volume includes comprehensive chapters on a variety of topics, including Real time cAMP signaling in response to CB1 activation, CB1 signaling in mitochondria, Lipidomics of cannabinoid systems, Studying endocannabinoid transport, Metabolic profiling of CB1 neutral antagonists, Approaches to assess biased signaling at the CB1 receptor, and the Development of CB1 allosteric modulators. - Continues the legacy of this premier serial with a new and updated release - Covers research cannabinoids and their receptors

Principles of Endocrinology and Hormone Action

Author : Antonino Belfiore
Publisher : Springer
ISBN 13 : 9783319446745
Total Pages : 0 pages
Book Rating : 4.4/5 (467 download)

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Book Synopsis Principles of Endocrinology and Hormone Action by : Antonino Belfiore

Download or read book Principles of Endocrinology and Hormone Action written by Antonino Belfiore and published by Springer. This book was released on 2018-02-08 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume provides comprehensive coverage of the current knowledge of the physiology of the endocrine system and hormone synthesis and release, transport, and action at the molecular and cellular levels. It presents essential as well as in-depth information of value to both medical students and specialists in Endocrinology, Gynecology, Pediatrics, and Internal Medicine. Although it is well established that the endocrine system regulates essential functions involved in growth, reproduction, and homeostasis, it is increasingly being recognized that this complex regulatory system comprises not only hormones secreted by the classic endocrine glands but also hormones and regulatory factors produced by many organs, and involves extensive crosstalk with the neural and immune system. At the same time, our knowledge of the molecular basis of hormone action has greatly improved. Understanding this complexity of endocrine physiology is crucial to prevent endocrine disorders, to improve the sensitivity of our diagnostic tools, and to provide the rationale for pharmacological, immunological, or genetic interventions. It is such understanding that this book is designed to foster.

Receptor - Based Drug Design

Author : Paul Leff
Publisher : CRC Press
ISBN 13 : 9781420001136
Total Pages : 816 pages
Book Rating : 4.0/5 (11 download)

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Book Synopsis Receptor - Based Drug Design by : Paul Leff

Download or read book Receptor - Based Drug Design written by Paul Leff and published by CRC Press. This book was released on 1998-04-10 with total page 816 pages. Available in PDF, EPUB and Kindle. Book excerpt: Employing a wide range of examples from G-protein-coupled receptors and ligand-gated ion channels, this detailed, single-source reference illustrates the principles of pharmacological analysis and receptor classification that are the basis of rational drug design. Explains the experimental and theoretical methods used to characterize interactions between ligands and receptors-providing the pharmacological information needed to solve treatment problems and facilitate the drug design process! Demonstrating the achievements of the receptor-based approach in therapeutics and indicating future directions, Receptor-Based Drug Design introduces novel computer-assisted strategies for the design of new agonists, antagonists, and inverse agonists for G-protein-coupled receptors shows how to assess agonist concentration-effect curve data discusses radioligand binding assays presents new in vitro multiarray assays for G-protein-coupled receptors explains the use of individual second messenger signaling responses in analyzing drug-receptor interactions examines the role of electrophysiology in finding new drugs and drug targets describes selectively acting b-adrenoceptor agonists and glucocorticoid steroids for asthma treatment outlines the rationale for using angiotensin receptor antagonists and more! Written by over 25 international authorities and containing nearly 1200 bibliographic citations, Receptor-Based Drug Design is a practical resource for pharmacologists, pharmacists, and pharmaceutical scientists; organic and medicinal chemists and biochemists; molecular biologists; biomedical researchers; and upper-level undergraduate and graduate students in these disciplines.

The Endothelium

Author : Michel Félétou
Publisher : Morgan & Claypool Publishers
ISBN 13 : 1615041230
Total Pages : 309 pages
Book Rating : 4.6/5 (15 download)

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Book Synopsis The Endothelium by : Michel Félétou

Download or read book The Endothelium written by Michel Félétou and published by Morgan & Claypool Publishers. This book was released on 2011 with total page 309 pages. Available in PDF, EPUB and Kindle. Book excerpt: The endothelium, a monolayer of endothelial cells, constitutes the inner cellular lining of the blood vessels (arteries, veins and capillaries) and the lymphatic system, and therefore is in direct contact with the blood/lymph and the circulating cells. The endothelium is a major player in the control of blood fluidity, platelet aggregation and vascular tone, a major actor in the regulation of immunology, inflammation and angiogenesis, and an important metabolizing and an endocrine organ. Endothelial cells controls vascular tone, and thereby blood flow, by synthesizing and releasing relaxing and contracting factors such as nitric oxide, metabolites of arachidonic acid via the cyclooxygenases, lipoxygenases and cytochrome P450 pathways, various peptides (endothelin, urotensin, CNP, adrenomedullin, etc.), adenosine, purines, reactive oxygen species and so on. Additionally, endothelial ectoenzymes are required steps in the generation of vasoactive hormones such as angiotensin II. An endothelial dysfunction linked to an imbalance in the synthesis and/or the release of these various endothelial factors may explain the initiation of cardiovascular pathologies (from hypertension to atherosclerosis) or their development and perpetuation. Table of Contents: Introduction / Multiple Functions of the Endothelial Cells / Calcium Signaling in Vascular Cells and Cell-to-Cell Communications / Endothelium-Dependent Regulation of Vascular Tone / Conclusion / References

Sensing the Environment: Regulation of Local and Global Homeostasis by the Skin's Neuroendocrine System

Author : Andrzej T. Slominski
Publisher : Springer Science & Business Media
ISBN 13 : 3642196837
Total Pages : 128 pages
Book Rating : 4.6/5 (421 download)

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Book Synopsis Sensing the Environment: Regulation of Local and Global Homeostasis by the Skin's Neuroendocrine System by : Andrzej T. Slominski

Download or read book Sensing the Environment: Regulation of Local and Global Homeostasis by the Skin's Neuroendocrine System written by Andrzej T. Slominski and published by Springer Science & Business Media. This book was released on 2012-06-02 with total page 128 pages. Available in PDF, EPUB and Kindle. Book excerpt: The skin, the body’s largest organ, is strategically located at the interface with the external environment where it detects, integrates and responds to a diverse range of stressors, including solar radiation. It has already been established that the skin is an important peripheral neuroendocrine-immune organ that is closely networked with central regulatory systems. These capabilities contribute to the maintenance of peripheral homeostasis. Specifically, epidermal and dermal cells produce and respond to classical stress neurotransmitters, neuropeptides and hormones, production which is stimulated by ultraviolet radiation (UVR), biological factors (infectious and non-infectious) and other physical and chemical agents. Examples of local biologically active products are cytokines, biogenic amines (catecholamines, histamine, serotonin and N-acetyl-serotonin), melatonin, acetylocholine, neuropeptides including pituitary (proopiomelanocortin-derived ACTH, b-endorphin or MSH peptides, thyroid stimulating hormone) and hypothalamic (corticotropin-releasing factor and related urocortins, thyroid-releasing hormone) hormones, as well as enkephalins and dynorphins, thyroid hormones, steroids (glucocorticoids, mineralocorticoids, sex hormones, 7-δ steroids), secosteroids, opioids and endocannabinoids. The production of these molecules is hierarchical, organized along the algorithms of classical neuroendocrine axes such as the hypothalamic pituitary adrenal axis (HPA), hypothalamic-thyroid axis (HPT), serotoninergic, melatoninergic, catecholaminergic, cholinergic, steroid/secosteroidogenic, opioid and endocannabinoid systems. Disruptions of these axes or of communication between them may lead to skin and/or systemic diseases. These local neuroendocrine networks also serve to limit the effect of noxious environmental agents to preserve local and consequently global homeostasis. Moreover, the skin-derived factors/systems can also activate cutaneous nerve endings to alert the brain to changes in the epidermal or dermal environments, or alternatively to activate other coordinating centers by direct (spinal cord) neurotransmission without brain involvement. Furthermore, rapid and reciprocal communications between epidermal and dermal and adnexal compartments are also mediated by neurotransmission including antidromic modes of conduction. Lastly, skin cells and the skin as an organ coordinate and/or regulate not only peripheral but also global homeostasis.

The Cannabinoid Receptors

Author : Patricia H. Reggio
Publisher : Springer Science & Business Media
ISBN 13 : 1597455032
Total Pages : 407 pages
Book Rating : 4.5/5 (974 download)

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Book Synopsis The Cannabinoid Receptors by : Patricia H. Reggio

Download or read book The Cannabinoid Receptors written by Patricia H. Reggio and published by Springer Science & Business Media. This book was released on 2008-11-09 with total page 407 pages. Available in PDF, EPUB and Kindle. Book excerpt: As research has progressed, the cannabinoid CB 1 and CB 2 receptors have expanded significantly in importance within the neuroscience mainstream. In The Cannabinoid Receptors, leading experts introduce newcomers to the cannabinoid field with chapters covering cannabinoid ligand synthesis and structure activity relationships, the molecular pharmacology of the cannabinoid receptors and the endocannabinoid system, and ultimately, the whole animal pharmacology and therapeutic applications for cannabinoid drugs. Adding to those key topics, the book also examines the current direction of the field with chapters on new putative cannabinoid receptors and challenges for future research. As a part of The Receptors TM series, this volume highlights its receptor with the most thorough, focused and essential information available. Comprehensive and cutting-edge, The Cannabinoid Receptors serves as an ideal guidebook to what continues to be a fascinating and vital field.

Novel Molecular Targets for the Treatment of Pain

Author : Tally Largent-Milnes
Publisher : Frontiers Media SA
ISBN 13 : 2889664422
Total Pages : 164 pages
Book Rating : 4.8/5 (896 download)

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Book Synopsis Novel Molecular Targets for the Treatment of Pain by : Tally Largent-Milnes

Download or read book Novel Molecular Targets for the Treatment of Pain written by Tally Largent-Milnes and published by Frontiers Media SA. This book was released on 2021-02-02 with total page 164 pages. Available in PDF, EPUB and Kindle. Book excerpt: Topic Editor John Streicher is a co-founder and equity partner of Teleport Pharmaceuticals, LLC. All other Topic Editors declare no competing interests with regards to the Research Topic subject.

TRP Ion Channel Function in Sensory Transduction and Cellular Signaling Cascades

Author : Wolfgang B. Liedtke, MD, PH.D.
Publisher : CRC Press
ISBN 13 : 1420005847
Total Pages : 502 pages
Book Rating : 4.4/5 (2 download)

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Book Synopsis TRP Ion Channel Function in Sensory Transduction and Cellular Signaling Cascades by : Wolfgang B. Liedtke, MD, PH.D.

Download or read book TRP Ion Channel Function in Sensory Transduction and Cellular Signaling Cascades written by Wolfgang B. Liedtke, MD, PH.D. and published by CRC Press. This book was released on 2006-09-29 with total page 502 pages. Available in PDF, EPUB and Kindle. Book excerpt: Since the first TRP ion channel was discovered in Drosophila melanogaster in 1989, the progress made in this area of signaling research has yielded findings that offer the potential to dramatically impact human health and wellness. Involved in gateway activity for all five of our senses, TRP channels have been shown to respond to a wide range of st

Drug-Acceptor Interactions

Author : Niels Bindslev
Publisher : CRC Press
ISBN 13 : 1351660578
Total Pages : 847 pages
Book Rating : 4.3/5 (516 download)

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Book Synopsis Drug-Acceptor Interactions by : Niels Bindslev

Download or read book Drug-Acceptor Interactions written by Niels Bindslev and published by CRC Press. This book was released on 2017-02-10 with total page 847 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug-Acceptor Interactions: Modeling theoretical tools to test and evaluate experimental equilibrium effects suggests novel theoretical tools to test and evaluate drug interactions seen with combinatorial drug therapy. The book provides an in-depth, yet controversial, exploration of existing tools for analysis of dose-response studies at equilibrium or steady state. The book is recommended reading for post-graduate students and researchers engaged in the study of systems biology, networks, and the pharmacodynamics of natural or industrial drugs, as well as for medical clinicians interested in drug application and combinatorial drug therapy. Even people without mathematical skills will be able to follow the pros and cons of reaction schemes and their related distribution equations. Chapter 9 is a hands-on guide for software to plot, fit and analyze one’s own data.

The Health Effects of Cannabis and Cannabinoids

Author : National Academies of Sciences, Engineering, and Medicine
Publisher : National Academies Press
ISBN 13 : 0309453070
Total Pages : 487 pages
Book Rating : 4.3/5 (94 download)

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Book Synopsis The Health Effects of Cannabis and Cannabinoids by : National Academies of Sciences, Engineering, and Medicine

Download or read book The Health Effects of Cannabis and Cannabinoids written by National Academies of Sciences, Engineering, and Medicine and published by National Academies Press. This book was released on 2017-03-31 with total page 487 pages. Available in PDF, EPUB and Kindle. Book excerpt: Significant changes have taken place in the policy landscape surrounding cannabis legalization, production, and use. During the past 20 years, 25 states and the District of Columbia have legalized cannabis and/or cannabidiol (a component of cannabis) for medical conditions or retail sales at the state level and 4 states have legalized both the medical and recreational use of cannabis. These landmark changes in policy have impacted cannabis use patterns and perceived levels of risk. However, despite this changing landscape, evidence regarding the short- and long-term health effects of cannabis use remains elusive. While a myriad of studies have examined cannabis use in all its various forms, often these research conclusions are not appropriately synthesized, translated for, or communicated to policy makers, health care providers, state health officials, or other stakeholders who have been charged with influencing and enacting policies, procedures, and laws related to cannabis use. Unlike other controlled substances such as alcohol or tobacco, no accepted standards for safe use or appropriate dose are available to help guide individuals as they make choices regarding the issues of if, when, where, and how to use cannabis safely and, in regard to therapeutic uses, effectively. Shifting public sentiment, conflicting and impeded scientific research, and legislative battles have fueled the debate about what, if any, harms or benefits can be attributed to the use of cannabis or its derivatives, and this lack of aggregated knowledge has broad public health implications. The Health Effects of Cannabis and Cannabinoids provides a comprehensive review of scientific evidence related to the health effects and potential therapeutic benefits of cannabis. This report provides a research agendaâ€"outlining gaps in current knowledge and opportunities for providing additional insight into these issuesâ€"that summarizes and prioritizes pressing research needs.

Novel Antipsychotic Drugs

Author : Herbert Y. Meltzer
Publisher :
ISBN 13 : 9780608058085
Total Pages : 284 pages
Book Rating : 4.0/5 (58 download)

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Book Synopsis Novel Antipsychotic Drugs by : Herbert Y. Meltzer

Download or read book Novel Antipsychotic Drugs written by Herbert Y. Meltzer and published by . This book was released on 1992-01-01 with total page 284 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Medicinal Cannabis and CBD in Mental Healthcare

Author : Kylie O'Brien
Publisher : Springer Nature
ISBN 13 : 3030785599
Total Pages : 591 pages
Book Rating : 4.0/5 (37 download)

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Book Synopsis Medicinal Cannabis and CBD in Mental Healthcare by : Kylie O'Brien

Download or read book Medicinal Cannabis and CBD in Mental Healthcare written by Kylie O'Brien and published by Springer Nature. This book was released on 2021-10-27 with total page 591 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book functions as a clinician’s guide to the use of cannabidiol (CBD) in the treatment of mental health conditions. It conveys the scientific evidence of efficacy of CBD as well as THC and addresses the social stigma attached to its medical use. The book describes the endocannabinoid system, how stress and the endocannabinoid system interact and key constituents, pharmacokinetics and safety aspects of medicinal cannabis, focusing on CBD and THC. Chapters on specific mental health conditions describe the underpinning pathomechanisms including how the endocannabinoid system is involved, and summarises the scientific evidence including animal and human research for the use of CBD and THC in treatment of such conditions. Topics covered include anxiety, depression, post-traumatic stress disorder, insomnia, Alzheimer's Disease and autism spectrum disorder. Chapters also discuss treatment guidelines and case studies. Unique and focused, Medicinal Cannabis and CBD in Mental Healthcare is an invaluable reference for medical practitioners seeking to adopt CBD-use in their treatment plans.

Structure-Based Drug Design

Author : Pandi Veerapandian
Publisher : Routledge
ISBN 13 : 1351413066
Total Pages : 665 pages
Book Rating : 4.3/5 (514 download)

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Book Synopsis Structure-Based Drug Design by : Pandi Veerapandian

Download or read book Structure-Based Drug Design written by Pandi Veerapandian and published by Routledge. This book was released on 2018-03-29 with total page 665 pages. Available in PDF, EPUB and Kindle. Book excerpt: Introducing the most recent advances in crystallography, nuclear magnetic resonance, molecular modeling techniques, and computational combinatorial chemistry, this unique, interdisciplinary reference explains the application of three-dimensional structural information in the design of pharmaceutical drugs. Furnishing authoritative analyses by world-renowned experts, Structure-Based Drug Design discusses protein structure-based design in optimizing HIV protease inhibitors and details the biochemical, genetic, and clinical data on HIV-1 reverse transcriptase presents recent results on the high-resolution three-dimensional structure of the catalytic core domain of HIV-1 integrase as a foundation for divergent combination therapy focuses on structure-based design strategies for uncovering receptor antagonists to treat inflammatory diseases demonstrates a systematic approach to the design of inhibitory compounds in cancer treatment reviews current knowledge on the Interleukin-1 (IL-1) system and progress in the development of IL-1 modulators describes the influence of structure-based methods in designing capsid-binding inhibitors for relief of the common cold and much more!