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Structure-based drug discovery is a collection of methods that exploits the ability to determine and analyse the three dimensional structure of biological molecules. These methods have been adopted and enhanced to improve the speed and quality of discovery of new drug candidates. After an introductory overview of the principles and application of structure-based methods in drug discovery, this book then describes the essential features of the various methods. Chapters on X-ray crystallography, NMR spectroscopy, and computational chemistry and molecular modelling describe how these particular techniques have been enhanced to support rational drug discovery, with discussions on developments such as high throughput structure determination, probing protein-ligand interactions by NMR spectroscopy, virtual screening and fragment-based drug discovery. The concluding chapters complement the overview of methods by presenting case histories to demonstrate the major impact that structure-based methods have had on discovering drug molecules. Written by international experts from industry and academia, this comprehensive introduction to the methods and practice of structure-based drug discovery not only illustrates leading-edge science but also provides the scientific background for the non-expert reader. The book provides a balanced appraisal of what structure-based methods can and cannot contribute to drug discovery. It will appeal to industrial and academic researchers in pharmaceutical sciences, medicinal chemistry and chemical biology, as well as providing an insight into the field for recent graduates in the biomolecular sciences.
This book reviews the current strategies and challenges for the treatment of bacterial, fungal, parasitic and viral infectious diseases in developing countries. Contributing authors present expert analysis on the transmission, epidemiology, bacteriology, pathogenesis and treatment of Neglected Tropical Bacterial Diseases such as Leprosy, Buruli ulcer, and Trachoma. Particular attention is also given to current antifungal agents, their spectrum of activity, mode of action, limitations, and current challenges in antifungal therapy. The authors explore the medicinal chemistry efforts that gave rise to currently launched drugs and new anti-HIV agents, and they also highlight the latest vaccine and drug developments in the clinical management of the Ebola Virus Disease, ignited by the 2014-2016 outbreak. This work has an interdisciplinary appeal and will engage scholars and professionals in the burden of communicable diseases.
This book highlights how terpenoids act as biological messengers and can be used as medicine against liver disease, neurodegenerative disease, cancer, infectious disease, cardiovascular disease, and inflammatory diseases. It emphasizes the metabolic engineering approach of terpenoids production and their toxicity.
Drug development is very expensive and a fight against time. PET offers possibilities to speed up this process by adding unique in vivo information on pharmacokinetics/dynamics of a drug at an early stage. This information can help decision makers to move the drug in the drug development process or to decide to stop further developments. This unique and complete book highlights the different ways PET can be used and describes the latest trends in the various disciplines within nuclear medicine to further improve methodologies and increase the number of tools to accelerate drug development. Various topics within tracer development, instrumentation, data analysis and many clinical and preclinical topics are described by leading scientists from industry and academia.
This fully revised and updated third edition of Pharmaceutical Inhalation Aerosol Technology encompasses the scientific and technical foundation for the rationale, design, componentry, assembly and quality performance metrics of therapeutic inhalers in their delivery of pharmaceutical aerosols to treat symptoms or the underlying causes of disease. It focuses on the importance of pharmaceutical engineering as a foundational element of all inhaler products and their application to pulmonary drug delivery. The expanded scope considers previously unaddressed aspects of pharmaceutical inhalation aerosol technology and the patient interface by including aerosol delivery, lung deposition and clearance that are used as measures of effective dose delivery.
Pharmacology in Drug Discovery and Development: Understanding Drug Response, Second Edition, is an introductory resource illustrating how pharmacology can be used to furnish the tools necessary to analyze different drug behavior and trace this behavior to its root cause or molecular mechanism of action. The concepts discussed in this book allow for the application of more predictive pharmacological procedures aimed at increasing therapeutic efficacy that will lead to more successful drug development. Chapters logically build upon one another to show how to characterize the pharmacology of any given molecule and allow for more informed predictions of drug effects in all biological systems. New chapters are dedicated to the interdisciplinary drug discovery environment in both industry and academia, and special techniques involved in new drug screening and lead optimization. This edition has been fully revised to address the latest advances and research related to real time kinetic assays, pluridimensional efficacy, signaling bias, irreversible and chemical antagonism, allosterically-induced bias, pharmacokinetics and safety, target and pathway validation, and much more. With numerous valuable chapter summaries, detailed references, practical examples and case studies throughout, Dr. Kenakin successfully navigates a highly complex subject, making it accessible for students, professors, and new researchers working in pharmacology and drug discovery.
The use of biobased feedstocks and products produced from them are becoming increasingly established in the chemical industry. Significant advancements in processing, formulation, biotechnology, and chemical modification have enabled biobased materials to be used alongside petroleum hydrocarbon derived materials and provide additional performance capabilities. There is growing interest in biobased products in the scientific community, industry, and the public sector due to health and environmental issues, interest in sustainability, concerns about petroleum supply, and opportunities for new products and processes. The use of renewable raw materials is an important component of green chemistry. Following the green chemistry principle that a raw material or feedstock should be renewable rather than depleting whenever technically and economically practicable, and with demand for fuels and chemicals growing worldwide, biobased chemicals and processes are being implemented commercially. Renewable alternatives are playing an increasingly important role as basic resources for the production of energy and chemicals while enhancing human and environmental safety. Significant progress has been made, and is continuing, in developing and utilizing chemicals and materials using plant-based feedstocks as a viable and renewable replacement for petrochemicals. The driving forces supporting the growth of a biobased chemical industry segment and the global supply challenges that must be addressed are recognized. The chapters in this book provide examples of new developments and commercially promising biobased products.
This book describes the way that pharmaceutical projects and programs are currently managed, and offers views from many highly experienced practitioners from within the industry on future directions for drug program management. The book integrates portfolio, program, and project management processes as fundamental for effective and efficient drug product development. Contributing expert authors provide their view of how the projectization approach can be taken forward by the drug industry over the coming years.
This thesis mainly describes the development of a screening process for a mirror-image library of chiral natural products. It demonstrates how, by using mirror-image proteins for the screening of available natural products, unavailable mirror-image isomers of natural products can be screened in a mirror process. Moreover, as mirror-image isomers including target proteins and natural products are mainly prepared by means of chemical synthesis, the screening strategy presented here suggests the importance of organic chemistry. Natural products are commonly used as valuable resources for drug discovery. However, as they are mostly produced as single enantiomeric forms, researchers have tested o nly natural products bearing one stereochemistry available in nature. As natural products and their enantiomers have identical physicochemical properties and different biological activities, mirror-image isomers of natural products are promising candidates for novel medicinal resources. In an effort to identify anticancer agents from the mirror-image library, chemical protein syntheses of some target oncoproteins, MDM2, MDMX and Grb2, and their applications to the chemical array screening process were achieved. In the course of this process the NP843 enantiomer, which is the enantiomer of an -tocopherol derivative, was successfully identified as a novel MDM2-p53 interaction inhibitor. These results clearly show that a mirror-image library of chiral natural products represents an invaluable medicinal resource. Accordingly, the chemistry-based screening strategy described in this thesis will be of great interest to a broad range of chemists involved in natural product, medicinal, and synthetic chemistry.
This book reviews drug delivery systems as mechanisms to introduce therapeutic agents into the body to help or improve tissue function, and examines different drug delivery systems applied in various organs. To date, polymeric systems, ceramic particles or composites have been used in different applications such as injectable, coatings of implants, scaffolds, or implantable devices. Such systems should be able to retain the therapeutic agent and release it in uniform amounts at a specific time.
"A lot of hard-won knowledge is laid out here in a brief but informative way. Every topic is well referenced, with citations from both the primary literature and relevant resources from the internet." Review from Nature Chemical Biology Written by the founders of the SPARK program at Stanford University, this book is a practical guide designed for professors, students and clinicians at academic research institutions who are interested in learning more about the drug development process and how to help their discoveries become the novel drugs of the future. Often many potentially transformative basic science discoveries are not pursued because they are deemed `too early' to attract industry interest. There are simple, relatively cost-effective things that academic researchers can do to advance their findings to the point that they can be tested in the clinic or attract more industry interest. Each chapter broadly discusses an important topic in drug development, from preclinical work in assay design through clinical trial design, regulatory issues and marketing assessments. After the practical overview provided here, the reader is encouraged to consult more detailed texts on specific topics of interest. "I would actually welcome it if this book's intended audience were broadened even more. Younger scientists starting out in the drug industry would benefit from reading it and getting some early exposure to parts of the process that they'll eventually have to understand. Journalists covering the industry (especially the small startup companies) will find this book a good reality check for many an over-hopeful press release. Even advanced investors who might want to know what really happens in the labs will find information here that might otherwise be difficult to track down in such a concentrated form."
Fullerens, Graphenes and Nanotubes: A Pharmaceutical Approach shows how carbon nanomaterials are used in the pharmaceutical industry. While there are various books on the carbonaceous nanomaterials available on the market, none approach the subject from a pharmaceutical point-of-view. In this context, the book covers different applications of carbonaceous nanomaterials. Chapters examine different types of carbon nanomaterials and explore how they are used in such areas as cancer treatments, pulse sensing and prosthetics. Readers will find this book to be a valuable reference resource for those working in the areas of carbon materials, nanomaterials and pharmaceutical science.
This book details several important medicinal plants, their occurrence, plant compounds and their chemical structures, and pharmacological properties against various human diseases. It also gives information on isolation and structural elucidation of phytocompounds, bio-assays, metabolomic studies, and therapeutical applications of plant compounds.
This book compiles the fundamentals, applications and viable product strategies of biomimetic lipid membranes into a single, comprehensive source. It broadens its perspective to interdisciplinary realms incorporating medicine, biology, physics, chemistry, materials science, as well as engineering and pharmacy at large. The book guides readers from membrane structure and models to biophysical chemistry and functionalization of membrane surfaces. It then takes the reader through a myriad of surface-sensitive techniques before delving into cutting-edge applications that could help inspire new research directions. With more than half the world's drugs and various toxins targeting these crucial structures, the book addresses a topic of major importance in the field of medicine, particularly biosensor design, diagnostic tool development, vaccine formulation, micro/nano-array systems, and drug screening/development. Provides fundamental knowledge on biomimetic lipid membranes; Addresses some of biomimetic membrane types, preparation methods, properties and characterization techniques; Explains state-of-art technological developments that incorporate microfluidic systems, array technologies, lab-on-a-chip-tools, biosensing, and bioprinting techniques; Describes the integration of biomimetic membranes with current top-notch tools and platforms; Examines applications in medicine, pharmaceutical industry, and environmental monitoring.
Medicinal Chemistry, Second Edition provides a comprehensive, balanced introduction to this evolving, multi-disciplinary subject. The book carefully explains fundamental principles, assuming little in the way of prior knowledge. It opens with a broad overview of medicinal assuming little in the way of prior knowledge. It opens with a broad overview of medicinal chemistry followed by chapters that cover the principal methods used in drug design and the isolation of drugs from natural sources. subsequent chapters discuss more specialized aspects of medicinal chemistry and outline drug and analogue synthesis, development and production. Each chapter contains self-assessment questions, numerous examples and a wide variety of applications.
Building on the success of the first edition, the book has been completely redesigned to create a clearer, more logical presentation of the material. the text has been extensively revised and updated and includes two new chapters on drugs from natural sources, and drug development and production.
Medicinal chemistry, Second Edition will prove invaluable to students of chemistry, medicinal and pharmaceutical chemistry, pharmacy and pharmacology whose courses include medicinal chemistry units. Provides a comprehensive, accessible, clearly written introduction to medicinal chemistry Assumes little prior knowledge of biology and a familiarity with chemistry at first-year level Includes numerous examples of drugs and drug action Questions are provided at the end of each chapter, with answers at the end of the book Completely revised and updated to include many of the latest drugs and treatments
This book documents the long, still ongoing battle between the US Food and Drug Administration and the dietary supplement industry. It presents the complex, often subtle, and sometimes overlooked series of events that had a major impact on how dietary supplements are manufactured, marketed, sold, and used today. While the first few chapters focus on some background topics, the remaining chapters walk the reader through timeline of events, legislative actions, FDA proposed and final rules, and judicial decisions that led to our current dietary supplement regulatory framework. Interwoven in narrative are examples of the roles of science, social and public policy, politics, and popular media.
Hydrogels are crosslinked, macromolecular polymeric materials arranged in a three-dimensional network, which can absorb and retain large amounts of water. Hydrogels are commonly used in clinical practice and experimental medicine for a wide range of applications, including drug delivery, tissue engineering and regenerative medicine, diagnostics, cellular immobilization, separation of biomolecules or cells, and barrier materials to regulate biological adhesions. This book elucidates the underlying concepts and emerging applications of hydrogels and will provide key case studies and critical analysis of the existing research.
Formulation is a key step in the drug design process, where the active drug is combined with other substances that maximise the therapeutic potential, safety and stability of the final medicinal product. Modern formulation science deals with biologics as well as small molecules. Regulatory and quality demands, in addition to advances in processing technologies, result in growing challenges as well as possibilities for the field. Pharmaceutical Formulation provides an up to date source of information for all who wish to understand the principles and practice of formulation in the drug industry. The book provides an understanding of the links between formulation theory and the practicalities of processing in a commercial environment, giving researchers the knowledge to produce effective pharmaceutical products that can be approved and manufactured. The first chapters introduce readers to different dosage forms, including oral liquid products, topical products and solid dosage forms such as tablets and capsules. Subsequent chapters cover pharmaceutical coatings, controlled release drug delivery and dosage forms designed specifically for paediatric and geriatric patients. The final chapter provides an introduction to the vital role intellectual property plays in drug development. Covering modern processing methods and recent changes in the regulatory and quality demands of the industry, Pharmaceutical Formulation is an essential, up to date resource for students and researchers working in academia and in the pharmaceutical industry.
The editors have engaged leading scientists in the field to participate in the development of this book, which is envisioned as a "one of a kind" contribution to the field. The book is a comprehensive text that puts fundamental bioanalytical science in context with current practice, its challenges and ongoing developments. It expands on existing texts on the subject by covering regulated bioanalysis of both small and large molecule therapeutics from both a scientific and regulatory viewpoint. The content will be useful to a wide spectrum of readers: from those new to bioanalysis; to those developing their experience in the laboratory, or working in one of the many critical supporting roles; to seasoned practitioners looking for a solid source of information on this exciting and important discipline.
Biopharmaceuticals:Biochemistry and Biotechnology, Second Edition, provides a comprehensive, up-to-date overview of the science and medical applications of biopharmaceutical products.
Extensively revised and updated, the Second Edition of this highly successful textbook discusses the latest developments in the field, providing a greater focus on actual commercial products and how they are manufactured. Substantial new sections on detailing biopharmaceutical drug delivery and how advances in genomics and proteomics will impact upon (bio)pharmaceutical drug development are also included.
Reviews of Biopharmaceuticals:
‘Biopharmaceuticals: Biochemistry and Biotechnology contain(s) some very useful information and ultimately serves as a comprehensive introduction to both the biopharmaceutical industry and its role within the larger arena of pharmaceuticals. For those new to, or keen to be involved with biopharmaceuticals, the book will undoubtedly provide a solid grounding of not just the technology, but of the industry as a whole’ Pharmaceutical Technology Europe
‘This great compliment of scientific literature, is easy-to-read and understand, up-to-date as well as comprehensive,’ Bioseparation
‘Biopharmaceuticals……is well written and provides an excellent overview of the biotechnology industry….This book is an excellent and balanced source of information about the biotechnology industry’ FEBS Letters
Discovering & Developing Molecules with Optimal Drug-Like Properties provides a contemporary view on the latest research in the areathat will help readers benchmark current best practices, new research techniques and strategies, and understanding of informatics.Written with anunderlying theme of early collaboration opportunities between pharmaceutical and discovery sciences, emphasis is made ofpractical considerations, with the opportunities examined from a number of different perspectives to maximize utility to the reader. Questions like What properties of a molecule are important from a drug-like standpoint? and What are some of the new techniques and approaches that can be used to characterize and understand molecular properties relevant to molecule druggability? will be addressed in an objective scientific manner. The text covers: - in silico predictive tools - contemporary approaches to physiochemical measurements - case studies in lead optimization for drug-like properties - assessing the risk and challenges related to key physicochemical properties - design of molecules tailored for specific drug delivery approaches - the importance of phase discovery and selection on drug molecule development - use of physicochemical properties for preclinical formulation selection and early clinical formulations - new approaches to link physiochemical properties to formulation selection"
With chapters from highly skilled, experienced, and renowned scientists and researchers from around the globe, Dendrimers for Drug Delivery provides an abundance of information on dendrimers and their applications in the field of drug delivery. The volume begins with an introduction to dendrimers, summarizing dendrimer applications and the striking features of dendrimers. It goes on to present the details of usual properties, structure, classification, and methods of synthesis, with relevant examples. The toxicity of dendrimers is also discussed. The chapter authors provide an exhaustive amount of information about dendrimers and their biomedical applications, including biocompatibility and toxicity aspects, a very useful feature. This informative volume will be valuable resource that will help readers to create products derived from dendrimers and navigate through the regulatory, manufacturing, and quality control hurdles. It will be an important resource for researchers, scientists, upper-level students, and industry professionals.
In this book the authors present current research in the study of liposomes. Topics discusses in this compilation include liposome mediated malaria vaccine development; liposomal delivery of antimicrobial agents in advances in liposome research; trends on microfluidic liposome production through hydrodynamic flow-focusing and microdroplet techniques for gene delivery applications; liposomes as important drug carriers in cancer therapy; liposome application in the veterinary field; and design of liposomes with a pH-sensitive fluorescent dye and gramicidin channels for immune-sensing.
This second edition book explores breakthrough technologies in the field of drug target identification and validation. The volume emphasizes particularly revolutionary technologies, such as CRISPR-related screening, "big data," and in silico approaches, as well as in vivo applications of CRISPR and best uses of animal models in drug development. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Fully updated and authoritative, Target Identification and Validation in Drug Discovery: Methods and Protocols, Second Edition is an ideal guide for molecular and cellular biologists, pharmacologists, pathologists, bioinformaticians, clinical researchers, or investigators, as well as experts in other fields that need a quick overview of these state-of-the-art technologies.
This book illustrates the current state-of-the-art in histamine research, with a focus on the appropriate methodologies to investigate the pharmacological properties and the therapeutic exploitation of HRs and their ligands. In addition, the range of techniques described provides an introduction to complementary cross-methodological disciplines beyond these fields. This multi-disciplinary approach is required to define the `decision gates' that determine the development of more effective and safer therapeutic options for many forms of highly prevalent and debilitating diseases, such as asthma, dementias, dermatitis, and arthritis. Written for the Methods in Pharmacology and Toxicology series, chapters concentrate on practical, hands-on protocols from experts in the techniques. Authoritative and thorough, Histamine Receptors as Drug Targets seeks to aid pharmacologists, biochemists, drug discovery researchers, molecular biologists, chemists, toxicologists, lab scientists, medical doctors, principle investigators, research scientists, lab directors and technicians, as well as graduate students around the world in pursuing the study of this vital scientific area.
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