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The 4th edition of this successful reference book contains an updated selection of the most frequently used assays for reliably detecting the pharmacological effects of potential drugs. Effects covered include cardiovascular, analgesic, endocrine, psychotropic, respiratory, renal and immunomodulatory activities. Each of the more than 1,000 assays comprises a detailed protocol outlining the purpose and rationale of the method, a critical assessment of the results and their pharmacological and clinical relevance. In addition, animal models of rare diseases are described. For this 4th edition, all existing chapters have been revised and completely updated. A large number of assays were added. Sections that have been specifically enlarged include - Pharmacological assays in thrombosis and haemostasis, - Antidiabetic activity (includes completely new chapters such as Biochemical Methods in Diabetology), - Anti-atherosclerotic activity. New chapters are added such as Auditory Pharmacology, Oncology Activity, Stem Cells, Omics, Personalized Medicine, etc.
The first edition of this handbook was a tremendous success,
collating the scientific literature on this topic that had
otherwise been rather limited and scattered throughout numerous
journals and patents. The result was a comprehensive resource that
addresses the preparation, selection, and use of pharmaceutically
active salts, examining the opportunities for increased efficacy
and improved drug delivery provided by the selection of an optimal
salt. This second, revised edition is designed to meet the
continued interest in both the topic and the book.
This third volume in the successful 'Drug Discovery in Infectious
Diseases' series is the first to deal with drug discovery in
helminthic infections in human and animals. The result is a broad
overview of different drug target evaluation methods, including
specific examples of successful drug development against
helminthes, and with a whole section devoted to vaccine
Edited by two renowned medicinal chemists who have pioneered the development of personalized therapies in their respective fields, this authoritative analysis of what is already possible is the first of its kind, and the only one to focus on drug development issues. Numerous case studies from the first generation of "personalized drugs" are presented, highlighting the challenges and opportunities for pharmaceutical development. While the majority of these examples are taken from the field of cancer treatment, other key emerging areas, such as neurosciences and inflammation, are also covered. With its careful balance of current and future approaches, this handbook is a prime knowledge source for every drug developer, and one that will remain up to date for some time to come. From the content: * Discovery of Predictive Biomarkers for Anticancer Drugs * Discovery and Development of Vemurafenib * Targeting Basal-Cell Carcinoma * G-Quadruplexes as Therapeutic Targets in Cancer * From Human Genetics to Drug Candidates: An Industrial Perspective on LRRK2 Inhibition as a Treatment for Parkinson's Disease * Therapeutic Potential of Kinases in Asthma * DNA Damage Repair Pathways and Synthetic Lethality * Medicinal Chemistry in the Context of the Human Genome and many more
Written by the pioneers of Viagra, the first blockbuster PDE
This is the first resource to provide researchers in academia and
industry with an urgently needed update on drug intervention
against trypanosomatides. As such, it
This first systematic treatment of the concept and practice of scaffold hopping shows the tricks of the trade and provides invaluable guidance for the reader's own projects. The first section serves as an introduction to the topic by describing the concept of scaffolds, their discovery, diversity and representation, and their importance for finding new chemical entities. The following part describes the most common tools and methods for scaffold hopping, whether topological, shape-based or structure-based. Methods such as CATS, Feature Trees, Feature Point Pharmacophores (FEPOPS), and SkelGen are discussed among many others. The final part contains three fully documented real-world examples of successful drug development projects by scaffold hopping that illustrate the benefits of the approach for medicinal chemistry. While most of the case studies are taken from medicinal chemistry, chemical and structural biologists will also benefit greatly from the insights presented here.
The first professional reference on this highly relevant topic, for drug developers, pharmacologists and toxicologists. The authors provide more than a systematic overview of computational tools and knowledge bases for drug metabolism research and their underlying principles. They aim to convey their expert knowledge distilled from many years of experience in the field. In addition to the fundamentals, computational approaches and their applications, this volume provides expert accounts of the latest experimental methods for investigating drug metabolism in four dedicated chapters. The authors discuss the most important caveats and common errors to consider when working with experimental data. Collating the knowledge gained over the past decade, this practice-oriented guide presents methods not only used in drug development, but also in the development and toxicological assessment of cosmetics, functional foods, agrochemicals, and additives for consumer goods, making it an invaluable reference in a variety of disciplines.
Filling an obvious gap in the scientific literature, this
practice-oriented reference is the first to tie together the
working knowledge of large
The first of the two volumes is divided into three parts. Part One
begins by introducing xenobiotics in the broad context of
physiological metabolism, and continues with an overview of the
processes of drug disposition and metabolism. It then goes on to
summarize the macroscopic and microscopic locations of drug
metabolism in animals and humans. This is followed by an
introduction to the all-important issue of the consequences of drug
and xenobiotic metabolism, providing an initial overview of
pharmacokinetic, pharmacological and toxicological consequences.
The last chapter examines drug metabolism in the context of drug
research, with a focus on medicinal chemistry.
NMR in Pharmaceutical Sciences is intended to be a comprehensive source of information for the many individuals that utilize MR in studies of relevance to the pharmaceutical sector. The book is intended to educate and inform those who develop and apply MR approaches within the wider pharmaceutical environment, emphasizing the toolbox that is available to spectroscopists and radiologists. This book is structured on the key processes in drug discovery, development and manufacture, but underpinned by an understanding of fundamental NMR principles and the unique contribution that NMR (including MRI) can provide. After an introductory chapter, which constitutes an overview, the content is organised into five sections. The first section is on the basics of NMR theory and relevant experimental methods. The rest follow a sequence based on the chronology of drug discovery and development, firstly 'Idea to Lead' then 'Lead to Drug Candidate', followed by 'Clinical Development', and finally 'Drug Manufacture'. The thirty one chapters cover a vast range of topics from analytical chemistry, including aspects involved in regulatory matters and in the prevention of fraud, to clinical imaging studies. Whilst this comprehensive volume will be essential reading for many scientists based in pharmaceutical and related industries, it should also be of considerable value to a much wider range of academic scientists whose research is related to the various aspects of pharmaceutical R for them it will supply vital understanding of pharmaceutical industrial concerns and the basis of key decision making processes. About eMagRes Handbooks eMagRes (formerly the Encyclopedia of Magnetic Resonance) publishes a wide range of online articles on all aspects of magnetic resonance in physics, chemistry, biology and medicine. The existence of this large number of articles, written by experts in various fields, is enabling the publication of a series of eMagRes Handbooks on specific areas of NMR and MRI. The chapters of each of these handbooks will comprise a carefully chosen selection of eMagRes articles. In consultation with the eMagRes Editorial Board, the eMagRes handbooks are coherently planned in advance by specially-selected Editors, and new articles are written to give appropriate complete coverage. The handbooks are intended to be of value and interest to research students, postdoctoral fellows and other researchers learning about the scientific area in question and undertaking relevant experiments, whether in academia or industry. Have the content of this handbook and the complete content of eMagRes at your fingertips! Visit: www.wileyonlinelibrary.com/ref/eMagRes
A practice-oriented desktop reference for medical professionals,
toxicologists and pharmaceutical researchers, this handbook
Written for drug developers rather than computer scientists, this monograph adopts a systematic approach to mining scientifi c data sources, covering all key steps in rational drug discovery, from compound screening to lead compound selection and personalized medicine. Clearly divided into four sections, the first part discusses the different data sources available, both commercial and non-commercial, while the next section looks at the role and value of data mining in drug discovery. The third part compares the most common applications and strategies for polypharmacology, where data mining can substantially enhance the research effort. The final section of the book is devoted to systems biology approaches for compound testing. Throughout the book, industrial and academic drug discovery strategies are addressed, with contributors coming from both areas, enabling an informed decision on when and which data mining tools to use for one's own drug discovery project.
Most of the antibiotics now in use have been discovered more or
less by chance, and their mechanisms of action have only been
elucidated after their discovery. To meet the medical need for
next-generation antibiotics, a more rational approach to antibiotic
development is clearly needed.
Filling a real knowledge gap, this handbook and ready reference is
both modern and forward-looking in its emphasis on the "bench to
bedside" translational approach to drug development.
In this comprehensive two-volume resource on the topic senior lead generation medicinal chemists present a coherent view of the current methods and strategies in industrial and academic lead generation. This is the first book to combine both standard and innovative approaches in comparable breadth and depth, including several recent successful lead generation case studies published here for the first time. Beginning with a general discussion of the underlying principles and strategies, individual lead generation approaches are described in detail, highlighting their strengths and weaknesses, along with all relevant bordering disciplines like e.g. target identification and validation, predictive methods, molecular recognition or lead quality matrices. Novel lead generation approaches for challenging targets like DNA-encoded library screening or chemical biology approaches are treated here side by side with established methods as high throughput and affinity screening, knowledge- or fragment-based lead generation, and collaborative approaches. Within the entire book, a very strong focus is given to highlight the application of the presented methods, so that the reader will be able to learn from real life examples. The final part of the book presents several lead generation case studies taken from different therapeutic fields, including diabetes, cardiovascular and respiratory diseases, neuroscience, infection and tropical diseases. The result is a prime knowledge resource for medicinal chemists and for every scientist involved in lead generation.
This book presents basic and extensive information on the physiological and pathological significance of the protein-modifying enzymes, transglutaminases, which are involved in multiple biological events by catalyzing a unique and important posttranslational modification reaction, cross-linking of proteins, and interacting with a large number of proteins inside and outside of cells. Although several of their essential physiological roles have been revealed, many unknown and so far not fully understood functions have remained. In humans, there are eight active isozymes having distinct tissue and subcellular distribution patterns with different substrates and physiological roles. Accordingly, aberrant regulation of the enzyme reactions or expression may lead to or has been implicated in various pathologies including neurodegeneration, fibrosis, cancer, inflammation, celiac disease, and hemostasis disorders.To provide those who are new to the field with basic knowledge and recent information on transglutaminase structures and reactions, the mechanism by which transglutaminases modify substrate proteins and their contributions to multiple biological phenomena as well as disease phenotypes, the publication of the present transglutaminase book was planned, to consist of review articles by 17 expert investigators working in this exciting area of research. The book contains detailed information related to several transglutaminases from aspects in chemical and cellular biology, medical sciences, and biotechnology that will also supply starting points for drug discovery. Although many prominent findings have been published in recent years, this type of comprehensive review book has been missing in the scientific literature. This volume will be useful for investigators who either currently work on or will start addressing transglutaminase-related research, and beyond that, for a broad audience in the scientific community.
Cost-effective manufacturing of biopharmaceutical products is rapidly gaining in importance, while healthcare systems across the globe are looking to contain costs and improve efficiency. To adapt to these changes, industries need to review and streamline their manufacturing processes. This two volume handbook systematically addresses the key steps and challenges in the production process and provides valuable information for medium to large scale producers of biopharmaceuticals. It is divided into seven major parts: - Upstream Technologies - Protein Recovery - Advances in Process Development - Analytical Technologies - Quality Control - Process Design and Management - Changing Face of Processing With contributions by around 40 experts from academia as well as small and large biopharmaceutical companies, this unique handbook is full of first-hand knowledge on how to produce biopharmaceuticals in a cost-effective and quality-controlled manner.
A textbook which is both comprehensive and comprehensible and that offers easy but scientifically sound reading to both students and professionals Now in its 12th edition in its native German, Voigt's Pharmaceutical Technology is an interdisciplinary textbook covering the fundamental principles of pharmaceutical technology. Available for the first time in English, this edition is produced in full colour throughout, with a concise, clear structure developed after consultation with students, instructors and researchers. This book: Features clear chapter layouts and easily digestible content Presents novel trends, devices and processes Discusses classical and modern manufacturing processes Covers all formulation principles including tablets, ointments, capsules, nanosystems and biopharmaceutics Takes account of legal requirements for both qualitative and quantitative composition Addresses quality assurance considerations Uniquely relates contrasting international pharmacopeia from EU, US and Japan to formulation principles Includes examples and text boxes for quicker data assimilation Written for both students studying pharmacy and industry professionals in the field as well as toxicologists, biochemists, medical lab technicians, Voigt's Pharmaceutical Technology is the essential resource for understanding the various aspects of pharmaceutical technology.
Born out of a project of the IUPAC's committee on Medicinal
Chemistry and Drug Development, this reference addresses past and
current strategies for successful drug analog development,
extending the previously published volume by nine new analog
classes and eight case studies. Like its precursor, this volume
also contains a general section discussing universally applicable
strategies for analog discovery and development. Spanning a wide
range of therapeutic fields and chemical classes, the two volumes
together constitute the first systematic approach to drug analog
The past decade has seen the reappearance of natural products as a valuable source of potent therapeutics. Here, experts on bioactive natural products cover the full spectrum of clinically relevant enzymes that are known to be targeted by natural products. Key enzymes include acetylcholine esterase, angiotensin-I-converting enzyme, cyclooxygenase, dihydrofolate reductase, phospholipase A2, respiratory complexes, and many more. By connecting the diversity of medicinal natural product sources with their potential clinical applications, this volume serves as a companion for the medicinal chemist looking for innovative small molecule compounds as well as for pharmacologist interested in the clinical effects and mode of action of herbal and traditional medicines.
The discovery and use of medicines is just as fascinating a human scientific endeavor as space flight or the tracing of human evolution. It is also the everyday task of hundreds of thousands of pharmacists, pharmaceutical chemists and researchers worldwide. Based on his profound knowledge of past and present paradigms in the development of medicines, Enrique Ravina takes the reader from the very beginnings of pharmacology to the multibillion-dollar business it represents today. Recounting the often spectacular successes and failures of innovative drugs as well as the people who discovered them, he brings abstract science to life in anecdotal form. For anyone with a more than superficial interest in the science of drugs and all those interested in knowing how drugs have been developed, how they have reached us, and became part of our daily life. This book is beautifully illustrated, containing many rare and historical photographs of drugs and their discoverers, and abounds with references to the primary literature, listing seminal publications alongside more modern reviews for readers seeking further details. With a Foreword by Hugo Kubinyi
This book gives a comprehensive overview about medicinal inorganic chemistry. Topics like targeting strategies, mechanism of action, Pt-based antitumor drugs, radiopharmaceuticals are covered in detail and offer the reader an in-depth overview about this important topic.
Advances in biotechnology have provided scientists with an increasing number of biopharmaceuticals such as novel peptide and protein drugs as well as nucleic acid based drugs for gene therapy. However, successful delivery of these biopharmaceuticals is a major challenge because their molecular properties lead to poor physical and chemical stability in the body and limited membrane permeability. Therefore researchers are developing a range of new delivery technologies and materials to enable these new drugs to be delivered intact to their target sites.
"Delivery Technologies for Biopharmaceuticals" describes strategies to overcome the main barriers for successful delivery of therapeutic peptides, proteins, and nucleic acid-based drugs or vaccines related to the site of administration and the target site. Many of the approaches described are reported in formulations in current clinical trials as well as in marketed products. Contents include:
challenges in delivery of biopharmaceuticalsnovel formulation approaches for peptide and protein injectablesnon-viral chemical vectors and viral technology for delivery of nucleic acid based drugsimmune response, adjuvants and delivery systems for vaccinesseveral examples of delivery systems for different biopharmaceuticalsa critical assessment of delivery technologies for biopharmaceuticals
"Delivery Technologies for Biopharmaceuticals" is an essential single-volume introduction to the technologies used by researchers to ensure efficient delivery of this exciting new class of drugs. It will be of value to researchers and students working in drug delivery, formulation, biopharmaceuticals, medicinal chemistry, and new materials development.
With contributions from biotechnologists and bioengineers, this ready reference describes the state of the art in industrial biopharmaceutical production, with a strong focus on continuous processes. Recent advances in single-use technology as well as application guidelines for all types of biopharmaceutical products, from vaccines to antibodies, and from bacterial to insect to mammalian cells are covered. The efficiency, robustness, and quality control of continuous production processes for biopharmaceuticals are reviewed and compared to traditional batch processes for a range of different production systems.
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