Download or read book Phosphodiesterases as Drug Targets written by Sharron H. Francis and published by Springer Science & Business Media. This book was released on 2011-06-21 with total page 531 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cyclic nucleotide phosphodiesterases (PDEs) are promising targets for pharmacological intervention. Multiple PDE genes, isoform diversity, selective expression and compartmentation of the isoforms, and an array of conformations of PDE proteins are properties that challenge development of drugs that selectively target this class of enzymes. Novel characteristics of PDEs are viewed as unique opportunities to increase specificity and selectivity when designing novel compounds for certain therapeutic indications. This chapter provides a summary of the major concepts related to the design and use of PDE inhibitors.
Download or read book Phosphodiesterases as Drug Targets written by Sharron H. Francis and published by Springer. This book was released on 2011-08-02 with total page 522 pages. Available in PDF, EPUB and Kindle. Book excerpt: Cyclic nucleotide phosphodiesterases (PDEs) are promising targets for pharmacological intervention. Multiple PDE genes, isoform diversity, selective expression and compartmentation of the isoforms, and an array of conformations of PDE proteins are properties that challenge development of drugs that selectively target this class of enzymes. Novel characteristics of PDEs are viewed as unique opportunities to increase specificity and selectivity when designing novel compounds for certain therapeutic indications. This chapter provides a summary of the major concepts related to the design and use of PDE inhibitors.
Download or read book Phosphodiesterases and Their Inhibitors written by Spiros Liras and published by John Wiley & Sons. This book was released on 2014-03-03 with total page 280 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by the pioneers of Viagra, the first blockbuster PDE inhibitor drug. Beginning with a review of the first wave of phosphodiesterase (PDE) inhibitors, this book focuses on new and emerging PDE targets and their inhibitors. Drug development options for all major human PDE families are discussed and cover diverse therapeutic fields, such as neurological/psychiatric, cardiovascular/metabolic, pain, and allergy/respiratory diseases. Finally, emerging chemotherapeutic applications of PDE inhibitors against malaria and other tropical diseases are discussed.
Download or read book Cyclic Nucleotide Phosphodiesterases in the Central Nervous System written by Nicholas J. Brandon and published by John Wiley & Sons. This book was released on 2014-03-07 with total page 429 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book reviews advances in understanding phosphodiesterases within the central nervous system and their therapeutic applications. A range of expert authors from both academia and industry describe these, then focus on the areas of greatest scientific and medical interest to provide more detailed coverage. Therapeutic and drug discovery applications are covered for diseases including Alzheimer's, Parkinson's, schizophrenia, erectile dysfunction, and spinal cord injuries. There is also a chapter on drug discovery tools such as in vitro assays and X-ray structures for medicinal chemistry studies.
Download or read book Cyclic Nucleotide Phosphodiesterases in Health and Disease written by Joseph A. Beavo and published by CRC Press. This book was released on 2006-12-05 with total page 728 pages. Available in PDF, EPUB and Kindle. Book excerpt: Since the last major compendium dedicated to cyclic nucleotide phosphodiesterases (PDEs) was published over 15 years ago, an enormous amount of progress has occurred in the field. There is great need for a centralized source for key information in this burgeoning and therapeutically important area of medical research. Cyclic Nucleotide Phosph
Download or read book Small Molecule Inhibitors of Phosphodiesterases Discovered written by Mohd Ishaq Dar and published by Mohammed Abdul Malik. This book was released on 2024-02-21 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Phosphodiesterases (PDEs) are a group of enzymes that catalyze the hydrolysis of cyclic nucleotides, such as cAMP and cGMP, which play crucial roles in various signaling pathways in the body. Small molecule inhibitors of phosphodiesterases have been discovered as a promising strategy for the development of drugs that target these enzymes. The discovery of small molecule inhibitors of phosphodiesterases has great potential in drug development for a wide range of therapeutic applications. These inhibitors have shown promising results in the treatment of several diseases such as heart failure, pulmonary arterial hypertension, Alzheimer's disease, Parkinson's disease, and cancer. The inhibitors have been found to have anti-inflammatory, antiplatelet, neuroprotective, antidepressant, and cognition-enhancing properties, making them attractive for drug development. Phosphodiesterase inhibitors work by preventing the breakdown of cyclic nucleotides, resulting in increased levels of cAMP and cGMP. This, in turn, leads to smooth muscle relaxation, vasodilation, and bronchodilation. The inhibitors also modulate other signaling pathways, including cyclic AMP-dependent protein kinase and protein kinase G, leading to a broad range of therapeutic effects. The discovery of small molecule inhibitors of phosphodiesterases involves several approaches such as virtual screening, molecular docking, structure-based drug design, ligand-based drug design, and high-throughput screening. The process also includes lead optimization, pharmacophore modeling, drug binding, binding affinity, and structure-activity relationships (SAR) analysis. Furthermore, the inhibitors' pharmacokinetics, pharmacodynamics, ADME, toxicity, and drug delivery aspects are also evaluated during the drug development process. Preclinical studies and clinical trials are conducted to assess the efficacy and safety of these inhibitors. The results of these studies have demonstrated the therapeutic potential of these inhibitors in various diseases. In summary, the discovery of small molecule inhibitors of phosphodiesterases has opened up new avenues for drug development in several therapeutic areas. The inhibitors have shown great promise in the treatment of various diseases and have a broad range of therapeutic effects. The drug development process involves several approaches, including virtual screening, molecular docking, and structure-based drug design. The safety and efficacy of these inhibitors are evaluated in preclinical studies and clinical trials to assess their potential for therapeutic use.
Download or read book Hepatotoxicity written by Hyman J. Zimmerman and published by Lippincott Williams & Wilkins. This book was released on 1999 with total page 848 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by the foremost authority in the field, this volume is a comprehensive review of the multifaceted phenomenon of hepatotoxicity. Dr. Zimmerman examines the interface between chemicals and the liver; the latest research in experimental hepatotoxicology; the hepatotoxic risks of household, industrial, and environmental chemicals; and the adverse effects of drugs on the liver. This thoroughly revised, updated Second Edition features a greatly expanded section on the wide variety of drugs that can cause liver injury. For quick reference, an appendix lists these medications and their associated hepatic injuries. Also included are in-depth discussions of drug metabolism and factors affecting susceptibility to liver injury.
Download or read book Mechanisms of Neuroinflammation written by Gonzalo Emiliano Aranda Abreu and published by BoD – Books on Demand. This book was released on 2017-08-23 with total page 320 pages. Available in PDF, EPUB and Kindle. Book excerpt: "Mechanisms of Neuroinflammation" book explains how the neuronal cells become swollen at the moment of the blood-brain barrier disruption and how they lose their immunological isolation. A cascade of cytokines and immune cells from the bloodstream enters the nervous system, inflaming neurons and activating the glia. This produces a neuroinflammatory process that can generate different neurodegenerative diseases. Better understanding of mechanisms that are activated at the time when the damage to the brain occurs could lead to the development of suitable therapies that revert the neuronal inflammation and thus prevent further damage to the nervous system.
Download or read book Therapeutic Targets written by Luis M. Botana and published by John Wiley & Sons. This book was released on 2012-04-20 with total page 503 pages. Available in PDF, EPUB and Kindle. Book excerpt: The Latest Applications For Cellmechanism Research in Drug Discovery Designed to connect research on cell mechanisms with the drug discovery process, Therapeutic Targets: Modulation, Inhibition, and Activation introduces readers to a range of new concepts and novel approaches to drug screening and therapeutic drug targeting to help inform future avenues of drug research. Highly topical, this accessible edited volume features chapters contributed by respected experts from around the globe. The book helps postgraduate students and professional scientists working in academia and industry understand the molecular mechanisms of pharmacology, current pharmacological knowledge, and future perspectives in drug discovery, focusing on important biochemical protein targets and drug targeting strategies for specific diseases. Examining the pharmacology of therapeutically undefined targets and their potential applications, it includes chapters on traditional therapeutic targets, including enzymes (phosphodiesterases and proteases), ion channels, and G protein-coupled receptors, as well as more recently identified avenues of exploration, such as lipids, nuclear receptors, gene promoters, and more. Since different diseases require different targeting techniques, the book also includes dedicated chapters on strategies for investigating Alzheimer's, diabetes, pain, and inflammation treatments. Concluding with a cross-sectional look at new approaches in drug screening, Therapeutic Targets is an invaluable resource for understanding where the next generation of drugs are likely to emerge.
Download or read book Cyclic Nucleotide Phosphodiesterases written by J. Beavo and published by . This book was released on 1990 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Anesthetic Pharmacology written by Alex S. Evers and published by Cambridge University Press. This book was released on 2011-03-10 with total page 2902 pages. Available in PDF, EPUB and Kindle. Book excerpt: In recent years our understanding of molecular mechanisms of drug action and interindividual variability in drug response has grown enormously. Meanwhile, the practice of anesthesiology has expanded to the preoperative environment and numerous locations outside the OR. Anesthetic Pharmacology: Basic Principles and Clinical Practice, 2nd edition, is an outstanding therapeutic resource in anesthesia and critical care: Section 1 introduces the principles of drug action, Section 2 presents the molecular, cellular and integrated physiology of the target organ/functional system and Section 3 reviews the pharmacology and toxicology of anesthetic drugs. The new Section 4, Therapeutics of Clinical Practice, provides integrated and comparative pharmacology and the practical application of drugs in daily clinical practice. Edited by three highly acclaimed academic anesthetic pharmacologists, with contributions from an international team of experts, and illustrated in full colour, this is a sophisticated, user-friendly resource for all practitioners providing care in the perioperative period.
Download or read book Protein Protein Interactions as New Drug Targets written by Enno Klussmann and published by Springer Science & Business Media. This book was released on 2008-05-20 with total page 511 pages. Available in PDF, EPUB and Kindle. Book excerpt: Disease-relevant intracellular protein-protein interactions occurring at defined cellular sites possess great potential as drug targets. They permit highly specific pharmacological interference with defined cellular functions. Drugs targeting such interactions are likely to act with fewer side effects than conventional medication influencing whole cell functions. This book discusses therapeutically relevant protein-protein interactions with a major focus on scaffolding proteins tethering signal transduction processes to defined cellular compartments by direct protein-protein interactions. Recent advances in the development of pharmacological agents interfering with protein-protein interactions are highlighted.
Download or read book Platelets in Thrombotic and Non Thrombotic Disorders written by Paolo Gresele and published by Springer. This book was released on 2017-03-08 with total page 1445 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book reviews current science and applications in fields including thrombosis and hemostasis, signal transduction, and non-thrombotic conditions such as inflammation, allergy and tumor metastasis. It is a detailed, up-to-date, highly referenced text for clinical scientists and physicians, including recent developments in this rapidly expanding field. More than a scientific resource, this is also an authoritative reference and guide to the diagnosis.
Download or read book Biologic and Systemic Agents in Dermatology written by Paul S. Yamauchi and published by Springer. This book was released on 2018-01-02 with total page 574 pages. Available in PDF, EPUB and Kindle. Book excerpt: Written by leading experts in the field and designed for dermatologists and residents, this book includes evidence-based medicine that underscores the clinical data, as well as practical tips on how to use both biologic and systemic agents in the field of dermatology. In the past decade, there have been several groundbreaking advances in medical dermatology. Novel biologic and systemic agents have been developed to treat inflammatory disorders, including psoriasis and atopic dermatitis, as well as skin malignancies such as melanoma. Biologic and Systemic Agents in Dermatology encompasses these developments by describing the mechanism of action of these various agents and the clinical efficacy and safety to treating these respective disorders. The utilization of biologic and systemic agents in other dermatologic conditions, pharmacoeconomics, pharmacovigilance, and clinical trials outcomes are discussed as well as topics including tumor necrosis, conventional systemic agents for psoriatic disease, and oral agents for atopic dermatitis.
Download or read book Human Drug Targets written by Edward D. Zanders and published by John Wiley & Sons. This book was released on 2015-11-09 with total page 454 pages. Available in PDF, EPUB and Kindle. Book excerpt: The identification of drug targets in a given disease has been central to pharmaceutical research from the latter half of the 20th century right up to the modern genomics era. Human Drug Targets provides an essential guide to one of the most important aspects of drug discovery – the identification of suitable protein and RNA targets prior to the creation of drug development candidates. The first part of the book consists of introductory chapters that provide the background to drug target discovery and highlight the way in which these targets have been organised into online databases. It also includes a user’s guide to the list of entries that forms the bulk of the book. Since this is not designed to be a compendium of drugs, the emphasis will be on the known (or speculated) biological role of the targets and not on the issues associated with pharmaceutical development. The objective is to provide just enough information to be informative and prompt further searches, while keeping the amount of text for each of the many entries to a minimum. Human Drug Targets will prove invaluable to those drug discovery professionals, in both industry and academia, who need to make some sense of the bewildering array of online information sources on current and potential human drug targets. As well as creating order out of a complex target landscape, the book will act as an ideas generator for potentially novel targets that might form the basis of future discovery projects.
Download or read book Blood Brain Barrier in Drug Discovery written by Li Di and published by John Wiley & Sons. This book was released on 2015-02-02 with total page 604 pages. Available in PDF, EPUB and Kindle. Book excerpt: Focused on central nervous system (CNS) drug discovery efforts, this book educates drug researchers about the blood-brain barrier (BBB) so they can affect important improvements in one of the most significant – and most challenging – areas of drug discovery. • Written by world experts to provide practical solutions to increase brain penetration or minimize CNS side-effects • Reviews state-of-the-art in silico, in vitro, and in vivo tools to assess brain penetration and advanced CNS drug delivery strategies • Covers BBB physiology, medicinal chemistry design principles, free drug hypothesis for the BBB, and transport mechanisms including passive diffusion, uptake/efflux transporters, and receptor-mediated processes • Highlights the advances in modelling BBB pharmacokinetics and dynamics relationships (PK/PD) and physiologically-based pharmacokinetics (PBPK) • Discusses case studies of successful CNS and non-CNS drugs, lessons learned and paths to the market
Download or read book Cyclic Nucleotide Signaling written by XiaoDong Cheng and published by CRC Press. This book was released on 2021-03-30 with total page 288 pages. Available in PDF, EPUB and Kindle. Book excerpt: Showcasing the recent progresses of the field, Cyclic Nucleotide Signaling covers the major tools and methodologies used in various areas of research. The majority of the chapters are protocol oriented, with the goal of providing clear directions for laboratory use. Students and investigators new to the field will find this book particularly informative, as will scientists already actively researching nucleotide signaling.
