Download or read book Design Synthesis and Biological Activity of a Novel Class of Calcium Channel Blockers written by and published by . This book was released on 2001 with total page 238 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Design Synthesis and Biological Testing of a Novel Class of Calcium Channel Blockers written by Jinyung Kim and published by . This book was released on 1999 with total page 362 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Design Synthesis and Biological Evaluation of a Novel Class of Calcium Influx Inhibitors written by William Forest McCalmont and published by . This book was released on 2003 with total page 196 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book The Design Synthesis and Optimisation of Calcium Release activated Calcium CRAC Channel Inhibitors and Mitochondrial Permeability Transition Pore mPTP Modulators Using Phenotypic Screening written by Yannick Lacroix and published by . This book was released on 2015 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Several previous studies have shown that the current low success of new drug molecules reaching the market can be attributed to safety-related drug attrition. Additionally, the link between the physicochemical properties of small molecule drugs and their toxicity profile has been demonstrated. Moreover, the type of pharmacological assay used to measure the biological activity of compounds when carrying out a drug discovery effort is critical to ensure the efficacy of compounds towards modulating specific signalling pathways. Recent studies have suggested that phenotypic screening, for which a target-agnostic measure of a biological response is used to develop an assay, can be more appropriate than target-based screening when developing first-in-class small molecules in the context of under-defined biological targets. This thesis describes the efforts in improving the physicochemical properties of small molecules, using phenotypic screening, towards the identification of therapeutic agents modulating two biological targets, respectively: the calcium release-activated calcium channel and the mitochondrial permeability transition pore. CRAC channel The allergen stimulation of immune cells such as T cells and mast cells triggers the depletion of the calcium stores located in the endoplasmic reticulum, which in turn leads to an influx of calcium ions across the plasma membrane through calcium release-activated calcium (CRAC) channels. This process of store-operated calcium entry through CRAC channels is the main pathway of increasing the intracellular calcium concentration in T cells and mast cells, which controls a wide range of downstream cellular functions, such as the release of pro-inflammatory cytokines and mediators like histamine and prostaglandins. Inhibiting the ion current passing through the CRAC channel (ICRAC) could help to modulate immune inflammatory responses, and thus development of an ICRAC blocker would be of considerable clinical interest to treat conditions such as asthma. The aim of the first medicinal chemistry programme described in this thesis is to identify selective small molecule oral ICRAC inhibitors as novel agents for the treatment of asthma and other inflammatory diseases. This report describes the design, chemical synthesis and application of modern medicinal chemistry principles for the identification of novel ICRAC blockers, starting from hit molecules originating from a high throughput screen. mPTP The mitochondrial permeability transition pore (mPTP) is a voltage sensitive protein channel present in the inner membrane of mitochondria and it plays a key role in cellular apoptosis and necrosis. The exact composition of the pore is not fully elucidated, however, it is thought to be a combination of several molecular constituents. Under conditions of cellular stress, the channel transitions to a state of high conductance and becomes non-selectively permeable to a wide range of solutes which freely diffuse into the mitochondria. Additionally, proteins contained in the mitochondria, such as pro-apoptotic messengers, are released into the cytosol, which leads to cell death. The sustained opening of the mPTP is believed to be a key triggering event in the pathology of several diseases. The second part of this thesis describes the design and synthesis of small molecule modulators of the mPTP as novel agents for the treatment of diseases mediated by the opening of the mPTP.
Download or read book Synthesis of Best Seller Drugs written by Ruben Vardanyan and published by Academic Press. This book was released on 2016-01-07 with total page 870 pages. Available in PDF, EPUB and Kindle. Book excerpt: Synthesis of Best-Seller Drugs is a key reference guide for all those involved with the design, development, and use of the best-selling drugs. Designed for ease of use, this book provides detailed information on the most popular drugs, using a practical layout arranged according to drug type. Each chapter reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and synthesis. Of high interest to all those who work in the captivating areas of biologically active compounds and medicinal drug synthesis, in particular medicinal chemists, biochemists, and pharmacologists, the book aims to support current research efforts, while also encouraging future developments in this important field. Describes methods of synthesis, bioactivity and related drugs in key therapeutic areas Reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and more Presents a practical layout designed for use as a quick reference tool by those working in drug design, development and implementation
Download or read book Cumulated Index Medicus written by and published by . This book was released on 2000 with total page 1840 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Drug Induced Liver Injury written by and published by Academic Press. This book was released on 2019-07-13 with total page 288 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug-Induced Liver Injury, Volume 85, the newest volume in the Advances in Pharmacology series, presents a variety of chapters from the best authors in the field. Chapters in this new release include Cell death mechanisms in DILI, Mitochondria in DILI, Primary hepatocytes and their cultures for the testing of drug-induced liver injury, MetaHeps an alternate approach to identify IDILI, Autophagy and DILI, Biomarkers and DILI, Regeneration and DILI, Drug-induced liver injury in obesity and nonalcoholic fatty liver disease, Mechanisms of Idiosyncratic Drug-Induced Liver Injury, the Evaluation and Treatment of Acetaminophen Toxicity, and much more. Includes the authority and expertise of leading contributors in pharmacology Presents the latest release in the Advances in Pharmacology series
Download or read book Exercise Nutrition and the Older Woman written by Maria A. Fiatarone Singh and published by CRC Press. This book was released on 2000-04-21 with total page 623 pages. Available in PDF, EPUB and Kindle. Book excerpt: Exercise, Nutrition and the Older Woman: Wellness for Women Over Fifty is a comprehensive guide to the major wellness issues for women over fifty. The author is a physician who explores diet, exercise and lifestyle choices from a medical perspective. The book assists in the design and implementation of programs to optimize good health and quality o
Download or read book Innovations and Implementations of Computer Aided Drug Discovery Strategies in Rational Drug Design written by Sanjeev Kumar Singh and published by Springer Nature. This book was released on 2021-02-02 with total page 334 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents various computer-aided drug discovery methods for the design and development of ligand and structure-based drug molecules. A wide variety of computational approaches are now being used in various stages of drug discovery and development, as well as in clinical studies. Yet, despite the rapid advances in computer software and hardware, combined with the exponential growth in the available biological information, there are many challenges that still need to be addressed, as this book shows. In turn, it shares valuable insights into receptor-ligand interactions in connection with various biological functions and human diseases. The book discusses a wide range of phylogenetic methods and highlights the applications of Molecular Dynamics Simulation in the drug discovery process. It also explores the application of quantum mechanics in order to provide better accuracy when calculating protein-ligand binding interactions and predicting binding affinities. In closing, the book provides illustrative descriptions of major challenges associated with computer-aided drug discovery for the development of therapeutic drugs. Given its scope, it offers a valuable asset for life sciences researchers, medicinal chemists and bioinformaticians looking for the latest information on computer-aided methodologies for drug development, together with their applications in drug discovery.
Download or read book Beautifully Naked at Last written by Lisa Avery and published by . This book was released on 2015-04-04 with total page 72 pages. Available in PDF, EPUB and Kindle. Book excerpt: Poetry
Download or read book Calcium Channel Pharmacology written by Stefan I. McDonough and published by Springer Science & Business Media. This book was released on 2004 with total page 440 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume reviews the current ability, future prospects, and physiological and medical significance of being able to distinguish pharmacologically among different calcium channel subtypes. Chapters are organized around broad concepts addressing the state of the field that naturally cover the pharmacology of each different calcium channel. Mechanistic information on drug-channel interactions is also presented in several chapters, as a theoretical and practical guide to working with calcium channel blockers in general.
Download or read book Molecular Interaction Fields written by Gabriele Cruciani and published by John Wiley & Sons. This book was released on 2006-05-12 with total page 328 pages. Available in PDF, EPUB and Kindle. Book excerpt: This unique reference source, edited by the world's most respected expert on molecular interaction field software, covers all relevant principles of the GRID force field and its applications in medicinal chemistry. Entire chapters on 3D-QSAR, pharmacophore searches, docking studies, metabolism predictions and protein selectivity studies, among others, offer a concise overview of this emerging field. As an added bonus, this handbook includes a CD-ROM with the latest commercial versions of the GRID program and related software.
Download or read book Biology of the NMDA Receptor written by Antonius M. VanDongen and published by CRC Press. This book was released on 2008-10-29 with total page 368 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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
Download or read book Drug Discovery written by Robert A. Maxwell and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 443 pages. Available in PDF, EPUB and Kindle. Book excerpt: This treatise had its origins in the authors' strong opinion that the discovery of new drugs, especially of innovative therapeutic agents, really does not happen as a spontaneous sequel to investiga tive research, no matter how penetrating such research may be. Rather, it seemed to us that the discovery of innovative therapeutic agents was a very active process, existing in and of itself, and demanding full attention-it was not simply a passive, dependent by-process of investigative research. And yet, many researchers some close confreres of the authors, others more distant-believed otherwise. We felt that their view reflected unrealistic thinking and that reality probably lay closer to what Beyer" maintained: We are taught to believe that if we can understand a disease it should be easy enough to figure out, say, the molecular configuration of a definitive receptor mechanism somewhere along the line and to design a specific drug . . . . And so we start out to understand the disease but never get around to doing much about therapy. The authors very soon realized that there was essentially no quantitive information available on just where and how innovative therapeutic agents were discovered. There were only anecdotal accounts, and these were able to be selected and presented in ways that could be used to defend any point of view.
Download or read book Medicinal Natural Products written by Paul M. Dewick and published by John Wiley & Sons. This book was released on 2002-01-03 with total page 524 pages. Available in PDF, EPUB and Kindle. Book excerpt: This guide covers classes of natural products in medicine, whether derived from plants, micro-organisms or animals. Structured according to biosynthetic pathway, it is written from a chemistry-based approach.
Download or read book The Science of Flavonoids written by Erich Grotewold and published by Springer Science & Business Media. This book was released on 2008 with total page 300 pages. Available in PDF, EPUB and Kindle. Book excerpt: This is the only book of its kind to provide an overview of the science of flavonoids in plants.
Download or read book Chemical Epigenetics written by Antonello Mai and published by Springer Nature. This book was released on 2020-03-31 with total page 569 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents an authoritative review of the most significant findings about all the epigenetic targets (writers, readers, and erasers) and their implication in physiology and pathology. The book also covers the design, synthesis and biological validation of epigenetic chemical modulators, which can be useful as novel chemotherapeutic agents. Particular attention is given to the chemical mechanisms of action of these molecules and to the drug discovery prose which allows their identification. This book will appeal to students who want to know the extensive progresses made by epigenetics (targets and modulators) in the last years from the beginning, and to specialized scientists who need an instrument to quickly search and check historical and/or updated notices about epigenetics.
