Small Molecule Inhibitors Of Phosphodiesterases Discovered

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Small Molecule Inhibitors of Phosphodiesterases Discovered

Author : Mohd Ishaq Dar
Publisher : Mohammed Abdul Malik
ISBN 13 :
Total Pages : 0 pages
Book Rating : 4.2/5 (241 download)

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Book Synopsis Small Molecule Inhibitors of Phosphodiesterases Discovered by : Mohd Ishaq Dar

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.

Hepatotoxicity

Author : Hyman J. Zimmerman
Publisher : Lippincott Williams & Wilkins
ISBN 13 : 9780781719520
Total Pages : 848 pages
Book Rating : 4.7/5 (195 download)

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Book Synopsis Hepatotoxicity by : Hyman J. Zimmerman

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.

Evolving Methods for Macromolecular Crystallography

Author : Randy J. Read
Publisher : Springer Science & Business Media
ISBN 13 : 1402063148
Total Pages : 192 pages
Book Rating : 4.4/5 (2 download)

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Book Synopsis Evolving Methods for Macromolecular Crystallography by : Randy J. Read

Download or read book Evolving Methods for Macromolecular Crystallography written by Randy J. Read and published by Springer Science & Business Media. This book was released on 2007-06-25 with total page 192 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume draws on the expertise of leaders in the field of macromolecular crystallography to illuminate the dramatic developments that are accelerating progress in structural biology. Their contributions span the range of techniques from crystallization through data collection, structure solution and analysis. The book shows how modern high-throughput methods are contributing to a deeper understanding of medical problems.

Bioenvironmental Issues Affecting Men's Reproductive and Sexual Health

Author : Suresh C Sikka
Publisher : Academic Press
ISBN 13 : 0128013133
Total Pages : 638 pages
Book Rating : 4.1/5 (28 download)

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Book Synopsis Bioenvironmental Issues Affecting Men's Reproductive and Sexual Health by : Suresh C Sikka

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

Cyclic Nucleotide Signaling

Author : XiaoDong Cheng
Publisher : CRC Press
ISBN 13 : 9780367658809
Total Pages : 288 pages
Book Rating : 4.6/5 (588 download)

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Book Synopsis Cyclic Nucleotide Signaling by : XiaoDong Cheng

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.

Cyclic Nucleotide Phosphodiesterases in Health and Disease

Author : Joseph A. Beavo
Publisher : CRC Press
ISBN 13 : 1420020846
Total Pages : 728 pages
Book Rating : 4.4/5 (2 download)

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Book Synopsis Cyclic Nucleotide Phosphodiesterases in Health and Disease by : Joseph A. Beavo

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

Lower Urinary Tract Symptoms and Benign Prostatic Hyperplasia

Author : Giuseppe Morgia
Publisher : Academic Press
ISBN 13 : 0128113987
Total Pages : 330 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Lower Urinary Tract Symptoms and Benign Prostatic Hyperplasia by : Giuseppe Morgia

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

Phosphodiesterases and Their Inhibitors

Author : Spiros Liras
Publisher : John Wiley & Sons
ISBN 13 : 3527682368
Total Pages : 280 pages
Book Rating : 4.5/5 (276 download)

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Book Synopsis Phosphodiesterases and Their Inhibitors by : Spiros Liras

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.

Small Molecule Drug Discovery

Author : Andrea Trabocchi
Publisher : Elsevier
ISBN 13 : 0128183500
Total Pages : 358 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Small Molecule Drug Discovery by : Andrea Trabocchi

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

Caffeine for the Sustainment of Mental Task Performance

Author : Institute of Medicine
Publisher : National Academies Press
ISBN 13 : 0309082587
Total Pages : 172 pages
Book Rating : 4.3/5 (9 download)

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Book Synopsis Caffeine for the Sustainment of Mental Task Performance by : Institute of Medicine

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.

Small Molecule Microarrays: Methods and Protocols

Author : Mahesh Uttamchandani
Publisher : Methods in Molecular Biology
ISBN 13 : 9781493982424
Total Pages : 274 pages
Book Rating : 4.9/5 (824 download)

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Book Synopsis Small Molecule Microarrays: Methods and Protocols by : Mahesh Uttamchandani

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:

Pharmacotherapy of Pulmonary Hypertension

Author : Marc Humbert
Publisher : Springer Science & Business Media
ISBN 13 : 3642386644
Total Pages : 569 pages
Book Rating : 4.6/5 (423 download)

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Book Synopsis Pharmacotherapy of Pulmonary Hypertension by : Marc Humbert

Download or read book Pharmacotherapy of Pulmonary Hypertension written by Marc Humbert and published by Springer Science & Business Media. This book was released on 2013-10-04 with total page 569 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume focuses on current evidence-based pharmacological treatments of various forms of pulmonary hypertension and provides a comprehensive review of the latest developments in this area. The first part of the book covers the definition, classification, pathophysiology, pathology, biomarkers and animal models of the disease, thus laying the conceptual basis for what follows. The middle section provides an overview of the established therapies, such as calcium channel blockers, prostanoids, endothelin receptor antagonists, phosphodiesterase-5 inhibitors and inhaled nitric oxide. The last section explores novel pathways and emerging therapeutic approaches including soluble guanylate cyclase stimulators, Rho-kinase inhibitors, inhibitors of serotonin receptors and transporters, peptide growth factors, vasoactive peptides, modulators of redox equilibrium and cyclic nucleotide homeostasis, as well as immunosuppressive and anti-proliferative agents. Particular attention is given to the clinical applications of these experimental therapies, that are on the horizon. The book thus spans the continuum from basic science to clinical applications.

Fragment-based Drug Discovery

Author : Daniel A. Erlanson
Publisher : John Wiley & Sons
ISBN 13 : 352733775X
Total Pages : 524 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Fragment-based Drug Discovery by : Daniel A. Erlanson

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.

Human Drug Targets

Author : Edward D. Zanders
Publisher : John Wiley & Sons
ISBN 13 : 1118849825
Total Pages : 454 pages
Book Rating : 4.1/5 (188 download)

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Book Synopsis Human Drug Targets by : Edward D. Zanders

Download or read book Human Drug Targets written by Edward D. Zanders and published by John Wiley & Sons. This book was released on 2015-12-14 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.

Medicinal Chemistry of Neglected and Tropical Diseases

Author : Venkatesan Jayaprakash
Publisher : CRC Press
ISBN 13 : 1351011634
Total Pages : 461 pages
Book Rating : 4.3/5 (51 download)

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Book Synopsis Medicinal Chemistry of Neglected and Tropical Diseases by : Venkatesan Jayaprakash

Download or read book Medicinal Chemistry of Neglected and Tropical Diseases written by Venkatesan Jayaprakash and published by CRC Press. This book was released on 2019-08-15 with total page 461 pages. Available in PDF, EPUB and Kindle. Book excerpt: Medicinal Chemistry of Neglected and Tropical Diseases: Advances in the Design and Synthesis of Antimicrobial Agents consolidates and describes modern drug discovery and development approaches currently employed to identify effective chemotherapeutic agents for the treatment of Neglected Tropical Diseases (NTDs) from a medicinal chemistry perspective. Chapters are designed to cater to the needs of medicinal chemists who work with chemotherapeutic developments for NTDs, as well as serve as a guide to budding medicinal chemists who wish to work in this area. It will introduce rational drug design approaches adopted in designing chemotherapeutics and validated targets available for the purpose.

Electron Paramagnetic Resonance: Volume 27

Author : Bela E. Bode
Publisher : Royal Society of Chemistry
ISBN 13 : 183916171X
Total Pages : 277 pages
Book Rating : 4.8/5 (391 download)

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Book Synopsis Electron Paramagnetic Resonance: Volume 27 by : Bela E. Bode

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.

Drug Repurposing

Author : Farid A. Badria
Publisher : BoD – Books on Demand
ISBN 13 : 1839685204
Total Pages : 236 pages
Book Rating : 4.8/5 (396 download)

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Book Synopsis Drug Repurposing by : Farid A. Badria

Download or read book Drug Repurposing written by Farid A. Badria and published by BoD – Books on Demand. This book was released on 2020-12-02 with total page 236 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug repurposing or drug repositioning is a new approach to presenting new indications for common commercial and clinically approved existing drugs. For example, chloroquine, an old antimalarial drug, showed promising results for treating COVID-19, interfering with MDR in several types of cancer, and chemosensitizing human leukemic cells.This book focuses on the hypothesis, risk/benefits, and economic impacts of drug repurposing on drug discovery in dermatology, infectious diseases, neurological disorders, cancer, and orphan diseases. It brings together up-to-date research to provide readers with an informative, illustrative, and easy-to-read book useful for students, clinicians, and the pharmaceutical industry.