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 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 Discovery of Small Molecule Inhibitors of EphA4 written by Carine Farenc and published by . This book was released on 2012 with total page 223 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Bioenvironmental Issues Affecting Men s Reproductive and Sexual Health written by Suresh C Sikka and published by Academic Press. This book was released on 2017-11-14 with total page 638 pages. Available in PDF, EPUB and Kindle. Book excerpt: Bioenvironmental Issues Affecting Men's Reproductive and Sexual Health is structured into two parts related to men's reproductive and sexual health with eight sections designed to enable a logical flow of such knowledge. The book is focused on the biology of key organs involved in male reproduction and the environmental influences affecting their functions with particular emphasis on clinical aspects. Individual chapters within the book range from basic to translational aspects, but all hold clinical relevance. This is an essential reference for those working and learning in the field of human reproduction, reproductive toxicology and environmental influences on reproductive and sexual health. - Brings together the leading authorities working in the field of male reproduction and sexual health and how the environment affects these issues - Provides guidelines and reference values of various reproductive hormones, semen parameters, inclusion/exclusion criteria for clinical trials - Discover the most efficient methods by which to design clinical protocols for sperm safety studies and reproductive toxicology trials
Download or read book Lower Urinary Tract Symptoms and Benign Prostatic Hyperplasia written by Giuseppe Morgia and published by Academic Press. This book was released on 2018-01-05 with total page 330 pages. Available in PDF, EPUB and Kindle. Book excerpt: Lower Urinary Tract Symptoms and Benign Prostatic Hyperplasia: From Research to Bedside offers full acknowledgment of the basic research of lower urinary tract symptoms (LUTS) and benign prostatic hyperplasia (BPH), also connecting the clinical and practice management of the disease. It provides a full comprehension of LUTS and BPH from several aspects, allowing for a schematic interpretation of the disease and subsequent medical management. Going beyond the guidelines in the field, this title enhances the knowledge of BPH onset, allowing for the advancement of research, beneficial clinical implication and treatment. Perfect for researchers, urologists, pathologists and endocrinologists, this must-have reference provides what is needed to understand LUTS and BPH in one easy to reference place. Provides a clear understanding of the pathological mechanisms that are present in lower urinary tract symptoms (LUTS) and benign prostatic hyperplasia (BPH) Incorporates research with the clinical aspects of LUTS and BPH, including surgical techniques Presents an overview of LUTS and BPH in one easy to reference place
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.
Download or read book Small Molecule Drug Discovery written by Andrea Trabocchi and published by Elsevier. This book was released on 2019-11-23 with total page 358 pages. Available in PDF, EPUB and Kindle. Book excerpt: Small Molecule Drug Discovery: Methods, Molecules and Applications presents the methods used to identify bioactive small molecules, synthetic strategies and techniques to produce novel chemical entities and small molecule libraries, chemoinformatics to characterize and enumerate chemical libraries, and screening methods, including biophysical techniques, virtual screening and phenotypic screening. The second part of the book gives an overview of privileged cyclic small molecules and major classes of natural product-derived small molecules, including carbohydrate-derived compounds, peptides and peptidomimetics, and alkaloid-inspired compounds. The last section comprises an exciting collection of selected case studies on drug discovery enabled by small molecules in the fields of cancer research, CNS diseases and infectious diseases. The discovery of novel molecular entities capable of specific interactions represents a significant challenge in early drug discovery. Small molecules are low molecular weight organic compounds that include natural products and metabolites, as well as drugs and other xenobiotics. When the biological target is well defined and understood, the rational design of small molecule ligands is possible. Alternatively, small molecule libraries are being used for unbiased assays for complex diseases where a target is unknown or multiple factors contribute to a disease pathology. - Outlines modern concepts and synthetic strategies underlying the building of small molecules and their chemical libraries useful for drug discovery - Provides modern biophysical methods to screening small molecule libraries, including high-throughput screening, small molecule microarrays, phenotypic screening and chemical genetics - Presents the most advanced chemoinformatics tools to characterize the structural features of small molecule libraries in terms of chemical diversity and complexity, also including the application of virtual screening approaches - Gives an overview of structural features and classification of natural product-derived small molecules, including carbohydrate derivatives, peptides and peptidomimetics, and alkaloid-inspired small molecules
Download or read book Caffeine for the Sustainment of Mental Task Performance written by Institute of Medicine and published by National Academies Press. This book was released on 2002-01-07 with total page 172 pages. Available in PDF, EPUB and Kindle. Book excerpt: This report from the Committee on Military Nutrition Research reviews the history of caffeine usage, the metabolism of caffeine, and its physiological effects. The effects of caffeine on physical performance, cognitive function and alertness, and alleviation of sleep deprivation impairments are discussed in light of recent scientific literature. The impact of caffeine consumption on various aspects of health, including cardiovascular disease, reproduction, bone mineral density, and fluid homeostasis are reviewed. The behavioral effects of caffeine are also discussed, including the effect of caffeine on reaction to stress, withdrawal effects, and detrimental effects of high intakes. The amounts of caffeine found to enhance vigilance and reaction time consistently are reviewed and recommendations are made with respect to amounts of caffeine appropriate for maintaining alertness of military personnel during field operations. Recommendations are also provided on the need for appropriate labeling of caffeine-containing supplements, and education of military personnel on the use of these supplements. A brief review of some alternatives to caffeine is also provided.
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 Evaluation of Enzyme Inhibitors in Drug Discovery written by Robert A. Copeland and published by John Wiley & Sons. This book was released on 2005-04-01 with total page 295 pages. Available in PDF, EPUB and Kindle. Book excerpt: Vital information for discovering and optimizing new drugs "Understanding the data and the experimental details that support it has always been at the heart of good science and the assumption challenging process that leads from good science to drug discovery. This book helps medicinal chemists and pharmacologists to do exactly that in the realm of enzyme inhibitors." -Paul S. Anderson, PhD This publication provides readers with a thorough understanding of enzyme-inhibitor evaluation to assist them in their efforts to discover and optimize novel drug therapies. Key topics such as competitive, noncompetitive, and uncompetitive inhibition, slow binding, tight binding, and the use of Hill coefficients to study reaction stoichiometry are all presented. Examples of key concepts are presented with an emphasis on clinical relevance and practical applications. Targeted to medicinal chemists and pharmacologists, Evaluation of Enzyme Inhibitors in Drug Discovery focuses on the questions that they need to address: * What opportunities for inhibitor interactions with enzyme targets arise from consideration of the catalytic reaction mechanism? * How are inhibitors evaluated for potency, selectivity, and mode of action? * What are the advantages and disadvantages of specific inhibition modalities with respect to efficacy in vivo? * What information do medicinal chemists and pharmacologists need from their biochemistry and enzymology colleagues to effectively pursue lead optimization? Beginning with a discussion of the advantages of enzymes as targets for drug discovery, the publication then explores the reaction mechanisms of enzyme catalysis and the types of interactions that can occur between enzymes and inhibitory molecules that lend themselves to therapeutic use. Next are discussions of mechanistic issues that must be considered when designing enzyme assays for compound library screening and for lead optimization efforts. Finally, the publication delves into special forms of inhibition that are commonly encountered in drug discovery efforts, but can be easily overlooked or misinterpreted. This publication is designed to provide students with a solid foundation in enzymology and its role in drug discovery. Medicinal chemists and pharmacologists can refer to individual chapters as specific issues arise during the course of their ongoing drug discovery efforts.
Download or read book Small Molecule Microarrays Methods and Protocols written by Mahesh Uttamchandani and published by Methods in Molecular Biology. This book was released on 2018-12-05 with total page 274 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Fragment Based Drug Discovery written by Steven Howard and published by Royal Society of Chemistry. This book was released on 2015-06-17 with total page 314 pages. Available in PDF, EPUB and Kindle. Book excerpt: Fragment-based drug discovery is a rapidly evolving area of research, which has recently seen new applications in areas such as epigenetics, GPCRs and the identification of novel allosteric binding pockets. The first fragment-derived drug was recently approved for the treatment of melanoma. It is hoped that this approval is just the beginning of the many drugs yet to be discovered using this fascinating technique. This book is written from a Chemist's perspective and comprehensively assesses the impact of fragment-based drug discovery on a wide variety of areas of medicinal chemistry. It will prove to be an invaluable resource for medicinal chemists working in academia and industry, as well as anyone interested in novel drug discovery techniques.
Download or read book Fragment based Drug Discovery written by Daniel A. Erlanson and published by John Wiley & Sons. This book was released on 2016-02-23 with total page 524 pages. Available in PDF, EPUB and Kindle. Book excerpt: From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets.
Download or read book Frontal subcortical Circuits in Psychiatric and Neurological Disorders written by David G. Lichter and published by Guilford Press. This book was released on 2001-01-01 with total page 474 pages. Available in PDF, EPUB and Kindle. Book excerpt: The authors review knowledge on the anatomy of the frontal-subcortical circuits, their connections to other brain regions, and their influences on motor, cognitive, affective, and behavioral functioning. Specific clinical problems are addressed, including Parkinson's disease, obsessive/compulsive disorder, ADHD, and more. of full-color illustrations.
Download or read book Electron Paramagnetic Resonance Volume 27 written by Bela E. Bode and published by Royal Society of Chemistry. This book was released on 2020-11-25 with total page 277 pages. Available in PDF, EPUB and Kindle. Book excerpt: Electron paramagnetic resonance (EPR) applications remain highly significant in modern analytical science and this volume compiles critical coverage of developments in the recent literature. The topics covered in this volume describe contrasting types of EPR application, including rapid scan EPR, using the EPR toolkit to investigate the structural dynamics of membrane proteins and pulse dipolar EPR spectroscopy for investigating biomolecular binding events. An additional chapter reviewing the PARACAT collaboration from the EU has also been included. Providing a snapshot of the area by a handpicked group of researchers at the cutting-edge of the field, this book is a useful addition to any library supporting this research.
Download or read book Case Studies in Modern Drug Discovery and Development written by Xianhai Huang and published by John Wiley & Sons. This book was released on 2012-04-19 with total page 488 pages. Available in PDF, EPUB and Kindle. Book excerpt: Learn why some drug discovery and development efforts succeed . . . and others fail Written by international experts in drug discovery and development, this book sets forth carefully researched and analyzed case studies of both successful and failed drug discovery and development efforts, enabling medicinal chemists and pharmaceutical scientists to learn from actual examples. Each case study focuses on a particular drug and therapeutic target, guiding readers through the drug discovery and development process, including drug design rationale, structure-activity relationships, pharmacology, drug metabolism, biology, and clinical studies. Case Studies in Modern Drug Discovery and Development begins with an introductory chapter that puts into perspective the underlying issues facing the pharmaceutical industry and provides insight into future research opportunities. Next, there are fourteen detailed case studies, examining: All phases of drug discovery and development from initial idea to commercialization Some of today's most important and life-saving medications Drugs designed for different therapeutic areas such as cardiovascular disease, infection, inflammation, cancer, metabolic syndrome, and allergies Examples of prodrugs and inhaled drugs Reasons why certain drugs failed to advance to market despite major research investments Each chapter ends with a list of references leading to the primary literature. There are also plenty of tables and illustrations to help readers fully understand key concepts, processes, and technologies. Improving the success rate of the drug discovery and development process is paramount to the pharmaceutical industry. With this book as their guide, readers can learn from both successful and unsuccessful efforts in order to apply tested and proven science and technologies that increase the probability of success for new drug discovery and development projects.
Download or read book HIV 1 Integrase written by Nouri Neamati and published by John Wiley & Sons. This book was released on 2011-08-10 with total page 710 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book comprehensively covers the mechanisms of action and inhibitor design for HIV-1 integrase. It serves as a resource for scientists facing challenging drug design issues and researchers in antiviral drug discovery. Despite numerous review articles and isolated book chapters dealing with HIV-1 integrase, there has not been a single source for those working to devise anti-AIDS drugs against this promising target. But this book fills that gap and offers a valuable introduction to the field for the interdisciplinary scientists who will need to work together to design drugs that target HIV-1 integrase.
