Small Molecule Drug Discovery
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Small Molecule Drug Discovery
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Author : Andrea Trabocchi
language : en
Publisher: Elsevier
Release Date : 2019-11-23
Small Molecule Drug Discovery written by Andrea Trabocchi and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2019-11-23 with Science categories.
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
Introduction To Biological And Small Molecule Drug Research And Development
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Author : C. Robin Ganellin
language : en
Publisher: Academic Press
Release Date : 2013-05-07
Introduction To Biological And Small Molecule Drug Research And Development written by C. Robin Ganellin and has been published by Academic Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-05-07 with Science categories.
Introduction to Biological and Small Molecule Drug Research and Development provides, for the first time, an introduction to the science behind successful pharmaceutical research and development programs. The book explains basic principles, then compares and contrasts approaches to both biopharmaceuticals (proteins) and small molecule drugs, presenting an overview of the business and management issues of these approaches. The latter part of the book provides carefully selected real-life case studies illustrating how the theory presented in the first part of the book is actually put into practice. Studies include Herceptin/T-DM1, erythropoietin (Epogen/Eprex/NeoRecormon), anti-HIV protease inhibitor Darunavir, and more. Introduction to Biological and Small Molecule Drug Research and Development is intended for late-stage undergraduates or postgraduates studying chemistry (at the biology interface), biochemistry, medicine, pharmacy, medicine, or allied subjects. The book is also useful in a wide variety of science degree courses, in post-graduate taught material (Masters and PhD), and as basic background reading for scientists in the pharmaceutical industry. - For the first time, the fundamental scientific principles of biopharmaceuticals and small molecule chemotherapeutics are discussed side-by-side at a basic level - Edited by three senior scientists with over 100 years of experience in drug research who have compiled the best scientific comparison of small molecule and biopharmaceuticals approaches to new drugs - Illustrated with key examples of important drugs that exemplify the basic principles of pharmaceutical drug research and development
Natural Small Molecule Drugs From Plants
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Author : Guan-Hua Du
language : en
Publisher: Springer
Release Date : 2018-11-19
Natural Small Molecule Drugs From Plants written by Guan-Hua Du and has been published by Springer this book supported file pdf, txt, epub, kindle and other format this book has been release on 2018-11-19 with Medical categories.
This book discusses 120 types of natural, small-molecule drugs derived from plants. They are grouped into 7 parts according their clinical uses, such as drugs for cardiovascular diseases, for metabolic diseases, for neuropsychiatric diseases, for immune-mediated inflammatory diseases, anti-tumor drugs, and drugs for parasites and bacterial infection. Each chapter systematically summarizes one drug, including its physicochemical properties, sources, pharmacological effects and clinical applications. To help readers understand the drug better, the research and pharmacological activity for each drug is also described, which serves as a salutary lesson for future drug development. Written by frontline researchers, teachers and clinicians working in field of pharmacy and pharmacology it provides an overview of natural, small-molecule drugs derived from plants for researchers in the field.
Macrocycles In Drug Discovery
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Author : Jeremy I Levin
language : en
Publisher: Royal Society of Chemistry
Release Date : 2015
Macrocycles In Drug Discovery written by Jeremy I Levin and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015 with Medical categories.
This series provides a comprehensive resource for postgraduate students and for scientists in academia or industry wanting to learn topics outside their own areas of expertise.
New Therapeutic Strategies For Type 2 Diabetes
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Author : Rob M Jones
language : en
Publisher: Royal Society of Chemistry
Release Date : 2012-09-30
New Therapeutic Strategies For Type 2 Diabetes written by Rob M Jones and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2012-09-30 with Science categories.
The diabetes mellitus epidemic is unfolding across the globe with the World Health Organization (WHO) reporting a worldwide prevalence of 177 million patients with diabetes. Type 2 diabetes accounts for approximately ninety percent of all diabetes cases. Long-term complications of type 2 diabetes include atherosclerosis, heart disease, stroke, end-stage renal disease, retinopathy leading to blindness, nerve damage, sexual dysfunction, frequent infections, and difficult-to-treat foot ulcers, sometimes resulting in lower limb amputation. Diabetics are twice as likely to develop cardiovascular disease or have a stroke, two to six times more likely to have transient ischemic attacks, and fifteen to forty times more likely to require lower-limb amputation compared with the general population. In 2002, the total economic cost of diabetes was estimated to be $132 billion accounting for one in every ten health care dollars spent in the United States. As a direct consequence of this economic impact and in light of the fact that current approved therapies fail to provide adequate therapeutic advantage in preventing hyperglycemia, industry has been heavily focused on addressing new fundamental cellular mechanisms that will potentially address this unmet need. New Therapeutic Strategies for Type 2 Diabetes provides the reader with the most comprehensive survey to-date of the most innovative small molecule research strategies targeted at treating the burgeoning type 2 diabetes epidemic. Each chapter is written by a recognised thought-leader in this field. The book will be an invaluable reference for researchers and medicinal chemists that concisely explains the biological mechanisms underpinning each cutting-edge therapeutic strategy along with key medicinal chemistry rationales and up-to- date clinical findings.
Reactive Oxygen Species
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Author : Harald H. H. W. Schmidt
language : en
Publisher: Springer Nature
Release Date : 2021-02-23
Reactive Oxygen Species written by Harald H. H. W. Schmidt and has been published by Springer Nature this book supported file pdf, txt, epub, kindle and other format this book has been release on 2021-02-23 with Medical categories.
Reactive oxygen species (ROS) have been implicated in almost every human disease phenotype, without much, if any, therapeutic consequence foremost exemplified by the failure of the so-called anti-oxidants. This book is a game changer for the field and many clinical areas such as cardiology and neurology. The term ‘oxidative stress’ is abandoned and replaced with a systems medicine and network pharmacology-based mechanistic approach to disease. The ROS-related drugs discussed here target either ROS- forming or ROS -modifying enzymes for which there is strong clinical evidence. In addition, ROS targets are included as they jointly participate in causal mechanisms of disease. This approach is transforming the ROS field and represents a breakthrough in redox medicine indicating a path to patient benefit. In the coming years more targets and drugs may be discovered, but the approach will remain the same and this book will thus become, and for many years remain, the leading reference for ROSopathies and their treatment by network pharmacology. Chapter "Soluble Guanylate Cyclase Stimulators and Activators" is available open access under a Creative Commons Attribution 4.0 International License via link.springer.com.
Peptide Based Drug Discovery
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Author : Ved Srivastava
language : en
Publisher: Royal Society of Chemistry
Release Date : 2017-06-22
Peptide Based Drug Discovery written by Ved Srivastava and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2017-06-22 with Science categories.
With potentially high specificity and low toxicity, biologicals offer promising alternatives to small-molecule drugs. Peptide therapeutics have again become the focus of innovative drug development efforts backed up by a resurgence of venture funds and small biotechnology companies. What does it take to develop a peptide-based medicine? What are the key challenges and how are they overcome? What are emerging therapeutics for peptide modalities? This book answers these questions with a holistic story from molecules to medicine, combining the themes of design, synthesis and clinical applications of peptide-based therapeutics and biomarkers. Chapters are written and edited by leaders in the field from industry and academia and they cover the pharmacokinetics of peptide therapeutics, attributes necessary for commercially successful metabolic peptides, medicinal chemistry strategies for the design of peptidase-resistant peptide analogues, disease classes for which peptide therapeutic are most relevant, and regulatory issues and guidelines. The critical themes covered provide essential background information on what it takes to develop peptide-based medicine from a chemistry perspective and views on the future of peptide drugs. This book will be a valuable resource not only as a reference book for the researcher engaged in academic and pharmaceutical setting, from basic research to manufacturing and from organic chemistry to biotechnology, but also a valuable resource to graduate students to understand discovery and development process for peptide-based medicine.
Implantable Technologies
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Author : Ved Srivastava
language : en
Publisher: Royal Society of Chemistry
Release Date : 2021-10-20
Implantable Technologies written by Ved Srivastava and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2021-10-20 with Science categories.
Implantable technologies allow for a sustained control over the release of pharmaceuticals into the bloodstream thereby achieving a controlled concentration with the potential to minimise side-effects while increasing patient compliance. Significant progress has been made in various alternative implantable delivery technologies, notably in intraocular and subcutaneous devices. Despite success in research and clinical studies, long-term clinical efficacy may be more limited and different aspects related to drug development and commercialization using these technologies are not well understood or practiced in the commercial setting. This book provides a comprehensive and cohesive picture of the latest in the field while also outlining the opportunities and challenges in implantable technology. Implantable Technologies: Pepties and Biologic Drug Development is an ideal reference for any postgraduate or researcher interested in utilising implantable technologies and novel routes of drug administration. The book will also be of interest to those involved in formulation and clinical application for a wide array of disease areas in addition to more established paradigms such as diabetes and pain management.
Small Molecule Medicinal Chemistry
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Author : Werngard Czechtizky
language : en
Publisher: John Wiley & Sons
Release Date : 2015-09-21
Small Molecule Medicinal Chemistry written by Werngard Czechtizky and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015-09-21 with Science categories.
Stressing strategic and technological solutions to medicinal chemistry challenges, this book presents methods and practices for optimizing the chemical aspects of drug discovery. Chapters discuss benefits, challenges, case studies, and industry perspectives for improving drug discovery programs with respect to quality and costs. • Focuses on small molecules and their critical role in medicinal chemistry, reviewing chemical and economic advantages, challenges, and trends in the field from industry perspectives • Discusses novel approaches and key topics, like screening collection enhancement, risk sharing, HTS triage, new lead finding approaches, diversity-oriented synthesis, peptidomimetics, natural products, and high throughput medicinal chemistry approaches • Explains how to reduce design-make-test cycle times by integrating medicinal chemistry, physical chemistry, and ADME profiling techniques • Includes descriptive case studies, examples, and applications to illustrate new technologies and provide step-by-step explanations to enable them in a laboratory setting
Virtual Screening
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Author : Christoph Sotriffer
language : en
Publisher: John Wiley & Sons
Release Date : 2011-03-31
Virtual Screening written by Christoph Sotriffer and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2011-03-31 with Medical categories.
Drug discovery is all about finding small molecules that interact in a desired way with larger molecules, namely proteins and other macromolecules in the human body. If the three-dimensional structures of both the small and large molecule are known, their interaction can be tested by computer simulation with a reasonable degree of accuracy. Alternatively, if active ligands are already available, molecular similarity searches can be used to find new molecules. This virtual screening can even be applied to compounds that have yet to be synthesized, as opposed to "real" screening that requires cost- and labor-intensive laboratory testing with previously synthesized drug compounds. Unique in its focus on the end user, this is a real "how to" book that does not presuppose prior experience in virtual screening or a background in computational chemistry. It is both a desktop reference and practical guide to virtual screening applications in drug discovery, offering a comprehensive and up-to-date overview. Clearly divided into four major sections, the first provides a detailed description of the methods required for and applied in virtual screening, while the second discusses the most important challenges in order to improve the impact and success of this technique. The third and fourth, practical parts contain practical guidelines and several case studies covering the most important scenarios for new drug discovery, accompanied by general guidelines for the entire workflow of virtual screening studies. Throughout the text, medicinal chemists from academia, as well as from large and small pharmaceutical companies report on their experience and pass on priceless practical advice on how to make best use of these powerful methods.