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Lu Chuang Enzyme Inhibition in Drug Discovery and Development. The Good the Bad


The science and applied approaches of enzyme inhibition in drug discovery and development Offering a unique approach that includes both the pharmacologic and pharmaco-kinetic aspects of enzyme inhibition, Enzyme Inhibition in Drug Discovery and Development examines the scientific concepts and experimental approaches related to enzyme inhibition as applied in drug discovery and drug development. With chapters written by over fifty leading experts in their fields, Enzyme Inhibition in Drug Discovery and Development fosters a cross-fertilization of pharmacology, drug metabolism, pharmacokinetics, and toxicology by understanding the «good» inhibitions—desirable pharmacological effects—and «bad» inhibitions—drug–drug interactions and toxicity. The book discusses: The drug discovery process, including drug discovery strategy, medicinal chemistry, analytical chemistry, drug metabolism, pharmacokinetics, and safety biomarker assessment The manipulations of drug metabolizing enzymes and transporters as well as the negative consequences, such as drug–drug interactions The inhibition of several major drug target pathways, such as the GPCR pathway, the NFkB pathway, and the ion channel pathway Through this focused, single-source reference on the fundamentals of drug discovery and development, researchers in drug metabolism and pharmacokinetics (DMPK) will learn and appreciate target biology in drug discovery; discovery biologists and medicinal chemists will also broaden their understanding of DMPK.

17736.33 РУБ

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Robert A. Copeland Evaluation of Enzyme Inhibitors in Drug Discovery. A Guide for Medicinal Chemists and Pharmacologists


Offers essential guidance for discovering and optimizing novel drug therapies Using detailed examples, Evaluation of Enzyme Inhibitors in Drug Discovery equips researchers with the tools needed to apply the science of enzymology and biochemistry to the discovery, optimization, and preclinical development of drugs that work by inhibiting specific enzyme targets. Readers will applaud this book for its clear and practical presentations, including its expert advice on best practices to follow and pitfalls to avoid. This Second Edition brings the book thoroughly up to date with the latest research findings and practices. Updates explore additional forms of enzyme inhibition and special treatments for enzymes that act on macromolecular substrates. Readers will also find new discussions detailing the development and application of the concept of drug-target residence time. Evaluation of Enzyme Inhibitors in Drug Discovery begins by explaining why enzymes are such important drug targets and then examines enzyme reaction mechanisms. The book covers: Reversible modes of inhibitor interactions with enzymes Assay considerations for compound library screening Lead optimization and structure-activity relationships for reversible inhibitors Slow binding and tight binding inhibitors Drug-target residence time Irreversible enzyme inactivators The book ends with a new chapter exploring the application of quantitative biochemical principles to the pharmacologic evaluation of drug candidates during lead optimization and preclinical development. The Second Edition of Evaluation of Enzyme Inhibitors in Drug Discovery continues to offer a treatment of enzymology applied to drug discovery that is quantitative and mathematically rigorous. At the same time, the clear and simple presentations demystify the complex science of enzymology, making the book accessible to many fields— from pharmacology to medicinal chemistry to biophysics to clinical medicine.

11523.64 РУБ

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Arjun Singh Drug Discovery, Design & Development


Pharmaceutical Technology is versatile research area in the field of Drug Discovery, medicine, biotechnology, and pharmacology. Drug Discovery Technologies has been established to provide comprehensive overviews of all the major modern techniques, tools and technologies used in drug discovery and development technology. The major techniques and tools are used in drug discovery, drug design, clinical trial studies and thematic issues describing novel approaches and cutting edge technologies used in all stages of drug discovery. The Book addresses the multidimensional challenges of drug discovery science including integration issues of the drug discovery process. This Book is essential for all science students, biological scientists and researchers involved in drug discovery who wish to keep abreast of all the modern techniques and technologies used in drug discovery and development. The major topics of discussion related to drug, discovery and therapy will included in the next volume : Pharmaceutical Research & Development, Women's Health Drug Discovery & Therapy, Drug Discovery in Preclinical Research, Cardiovascular Drug Discovery & Therapy, Oncology, Process Chemistry and Drug.

4358 РУБ

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Varghese John BACE. Lead Target for Orchestrated Therapy of Alzheimers Disease


BACE inhibitors and their use in the treatment of Alzheimers Disease BACE (β-site of APP cleaving enzyme) is a critical component in Alzheimers Disease (AD), and the development of BACE inhibitors shows great potential as a therapy for the disease. BACE: Lead Target for Orchestrated Therapy of Alzheimers Disease covers virtually all aspects of BACE from initial identification, discovery of inhibitors, and challenges in clinical development, while providing a global understanding essential for productive and successful drug discovery. This book details the story of the discovery of BACE and its role in AD and comprehensively discusses: The development of BACE inhibitors as therapeutics for Alzheimers disease The research that led to the identification of BACE New BACE inhibitors currently being clinically tested ADME (absorption, distribution, metabolism, excretion) and clinical trial design—topics not addressed in current field literature Cutting-edge technology such as high-throughput screening, structure-based drug design, and QSAR in context of BACE inhibitors and Alzheimers drug discovery Other approaches to BACE inhibition based on interaction with the precursor protein APP By enhancing the readers understanding of the various aspects of the BACE drug-discovery process, this much-needed reference will serve as a key resource for all scientists involved in Alzheimers research—and inspire new approaches to treatment of AD.

10137.31 РУБ

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Wu-Kuang Yeh Enzyme Technologies. Pluripotent Players in Discovering Therapeutic Agent


Sets the stage for advances in drug discovery using the latest enzyme technology Reviewing new and emerging applications of enzyme technology in drug discovery, this book highlights some of the most promising areas of pharmaceutical and biotechnology research. It covers enzyme assay technology, utilization of enzymology for prodrug design, and the application of enzymes as therapeutic agents. Expert reviews highlight how our latest understanding of enzymology is used to develop new practical applications in drug discovery and design. Filled with case studies, Enzyme Technologies: Pluripotent Players in Discovering Therapeutic Agents enables readers to better understand the diverse functions of enzymes and master specific applications in drug discovery research. In addition to small molecule drug discovery, the book explores new developments in enzymes as therapeutic agents for genetic disorders. Section A, Enzymes – Essential Workhorses in Pharmaceutical Research, offers support in selecting the best enzyme targets for drug discovery, designing enzyme inhibitors for therapeutic agents, and evaluating selective enzyme inhibitors. Section B, Enzymes – Indispensable Tools for Improving Druggability, sets forth the principles alongside real-world examples of exploiting specific properties of enzymes to design successful prodrugs. Section C, Enzymes – Powerful Weapons for Correcting Natures Errors, provides new insights on applying enzymes as therapeutic agents or diagnostic tools to treat genetic disorders. Chapters are contributed by leading experts from around the world. Their contributions are based on a thorough review of the current literature as well as their own research. Reviewing our latest understanding of the nature of enzymes and their role in drug discovery, this book is recommended for researchers in pharmaceuticals and biotechnology as well as for researchers in enzymology, biochemistry, molecular biology, and medicinal chemistry.

12288.24 РУБ

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Binghe Wang Evaluation of Drug Candidates for Preclinical Development. Pharmacokinetics, Metabolism, Pharmaceutics, and Toxicology


Emphasizes the integration of major areas of drug discovery and their importance in candidate evaluation It is believed that selecting the «right» drug candidate for development is the key to success. In the last decade, pharmaceutical R&D departments have integrated pharmacokinetics and drug metabolism, pharmaceutics, and toxicology into early drug discovery to improve the assessment of potential drug compounds. Now, Evaluation of Drug Candidates for Preclinical Development provides a complete view and understanding of why absorption-distribution-metabolism-excretion-toxicology (ADMET) plays a pivotal role in drug discovery and development. Encompassing the three major interrelated areas in which optimization and evaluation of drug developability is most critical—pharmacokinetics and drug metabolism, pharmaceutics, and safety assessment—this unique resource encourages integrated thinking in drug discovery. The contributors to this volume: Cover drug transporters, cytochrome P-450 and drug-drug interactions, plasma protein binding, stability, drug formulation, preclinical safety assessment, toxicology, and toxicokinetics Address developability issues that challenge pharma companies, moving beyond isolated experimental results Reveal connections between the key scientific areas that are critical for successful drug discovery and development Inspire forward-thinking strategies and decision-making processes in preclinical evaluation to maximize the potential of drug candidates to progress through development efficiently and meet the increasing demands of the marketplace Evaluation of Drug Candidates for Preclinical Development serves as an introductory reference for those new to the pharmaceutical industry and drug discovery in particular. It is especially well suited for scientists and management teams in small- to mid-sized pharmaceutical companies, as well as academic researchers and graduate students concerned with the practical aspects related to the evaluation of drug developability.

9834.09 РУБ

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Mike Lee S. Oral Bioavailability Assessment. Basics and Strategies for Drug Discovery Development


Specifically geared to personnel in the pharmaceutical and biotechnology industries, this book describes the basics and challenges of oral bioavailability – one of the most significant hurdles in drug discovery and development. • Describes approaches to assess pharmacokinetics and how drug efflux and uptake transporters impact oral bioavailability • Helps readers reduce the failure rate of drug candidates when transitioning from the bench to the clinic during development • Explains how preclinical animal models – used in preclinical testing – and in vitro tools translate to humans, which is an underappreciated and complicated area of drug development • Includes chapters about pharmacokinetic modelling, the Biopharmaceutics Drug Disposition Classification System (BDDCS), and the Extended Clearance Classification System (ECCS) • Has tutorials for applying strategies to medicinal chemistry practices of drug discovery/development

13444.25 РУБ

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Binghe Wang Drug Design of Zinc-Enzyme Inhibitors. Functional, Structural, and Disease Applications


Brings together functional and structural informationrelevant to the design of drugs targeting zinc enzymes The second most abundant transition element in living organisms, zinc spans all areas of metabolism, with zinc-containing proteins offering both established and potential drug targets. Drug Design of Zinc-Enzyme Inhibitors brings together functional and structural information relevant to these zinc-containing targets. With up-to-date overviews of the latest developments field, this unique and comprehensive text enables readers to understand zinc enzymes and evaluate them in a drug design context. With contributions from the leaders of todays research, Drug Design of Zinc-Enzyme Inhibitors covers such key topics as: Major drug targets like carbonic anhydrases, matrix metalloproteinases, bacterial proteases, angiotensin-converting enzyme, histone deacetylase, and APOBEC3G Roles of recently discovered zinc-containing isozymes in cancer, obesity, epilepsy, pain management, malaria, and other conditions Cross reactivity of zinc-enzyme inhibitors and activators The extensive use of X-ray crystallography and QSAR studies for understanding zinc-containing proteins Clinical applications An essential resource for the discovery and development of new drug molecules, Drug Design of Zinc-Enzyme Inhibitors gives researchers, professionals, students, and academics the foundation to understand and work with zinc enzyme inhibitors and activators.

18975.74 РУБ

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Litwin Virginia Flow Cytometry in Drug Discovery and Development


This book covers the unique application of flow cytometry in drug discovery and development. The first section includes two introductory chapters, one on flow cytometry and one on biomarkers, as well as a chapter on recent advances in flow cytometry. The second section focuses on the unique challenges and added benefits associated with the use of flow cytometry in the drug development process. The third section contains a single chapter presenting an in depth discussion of validation considerations and regulatory compliance issues associated with drug development.

11008.48 РУБ

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Ekins Sean Drug Efficacy, Safety, and Biologics Discovery. Emerging Technologies Tools


Drug Efficacy, Safety, and Biologics Discovery: Emerging Technologies and Tools covers key emerging technologies in pharmaceutical R & D and how they have substantially impacted (or are currently impacting) drug discovery. The cross-disciplinary collaborations implicit in integrating these technologies with drug discovery operations will fuel the engine for future innovations. This book cuts across the multiple areas of drug discovery, each chapter authored by pioneers in that field, making for a broad appeal to the chemical and biological scientists and technologists involved in drug discovery and development.

11800.46 РУБ

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Urban Laszlo Predictive ADMET. Integrated Approaches in Drug Discovery and Development


This book helps readers integrate in silico, in vitro, and in vivo ADMET (absorption, distribution, metabolism, elimination and toxicity) and PK (pharmacokinetics) data with routine testing applications so that pharmaceutical scientists can diagnose ADMET problems and present appropriate recommendations to move drug discovery programs forward. The book introduces the current clinical practice for drug discovery and development along with the impact on early risk assessment; consolidates the tools and models to intelligently integrate existing in silico, in vitro and in vivo ADMET data; and demonstrates successful cases and lessons learned from real drug discovery and development. In short, it is a book aimed to provide a practical road map for drug discovery and development scientists to generate efficacious and safe drugs for unmet medical needs.

12275.65 РУБ

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Huang Xianhai Case Studies in Modern Drug Discovery and Development


Learn why some drug discovery and development efforts succeed . . . and others fail Written by international experts in drug discovery and development, this book sets forth carefully researched and analyzed case studies of both successful and failed drug discovery and development efforts, enabling medicinal chemists and pharmaceutical scientists to learn from actual examples. Each case study focuses on a particular drug and therapeutic target, guiding readers through the drug discovery and development process, including drug design rationale, structure-activity relationships, pharmacology, drug metabolism, biology, and clinical studies. Case Studies in Modern Drug Discovery and Development begins with an introductory chapter that puts into perspective the underlying issues facing the pharmaceutical industry and provides insight into future research opportunities. Next, there are fourteen detailed case studies, examining: All phases of drug discovery and development from initial idea to commercialization Some of todays most important and life-saving medications Drugs designed for different therapeutic areas such as cardiovascular disease, infection, inflammation, cancer, metabolic syndrome, and allergies Examples of prodrugs and inhaled drugs Reasons why certain drugs failed to advance to market despite major research investments Each chapter ends with a list of references leading to the primary literature. There are also plenty of tables and illustrations to help readers fully understand key concepts, processes, and technologies. Improving the success rate of the drug discovery and development process is paramount to the pharmaceutical industry. With this book as their guide, readers can learn from both successful and unsuccessful efforts in order to apply tested and proven science and technologies that increase the probability of success for new drug discovery and development projects.

11879.66 РУБ

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Walter Korfmacher A. Mass Spectrometry for Drug Discovery and Development


Facilitates the discovery and development of new, effective therapeutics With coverage of the latest mass spectrometry technology, this book explains how mass spectrometry can be used to enhance almost all phases of drug discovery and drug development, including new and emerging applications. The books fifteen chapters have been written by leading pharmaceutical and analytical scientists. Their contributions are based on a thorough review of the current literature as well as their own experience developing new mass spectrometry techniques to improve the ability to discover and develop new and effective therapeutics. Mass Spectrometry for Drug Discovery and Drug Development begins with an overview of the types of mass spectrometers that facilitate drug discovery and development. Next it covers: HPLC–high-resolution mass spectrometry for quantitative assays Mass spectrometry for siRNA Quantitative analysis of peptides Mass spectrometry analysis of biological drugs Applications that support medicinal chemistry investigations Mass spectrometry imaging and profiling Throughout the book, detailed examples underscore the growing role of mass spectrometry throughout the drug discovery and development process. In addition, images of mass spectra are provided to explain how results are interpreted. Extensive references at the end of each chapter guide readers to the primary literature in the field. Mass Spectrometry for Drug Discovery and Drug Development is recommended for readers in pharmaceutics, including medicinal chemists, analytical chemists, and drug metabolism scientists. All readers will discover how mass spectrometry can streamline and advance new drug discovery and development efforts.

10140.95 РУБ

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Young Daniel L. Systems Biology in Drug Discovery and Development


The first book to focus on comprehensive systems biology as applied to drug discovery and development Drawing on real-life examples, Systems Biology in Drug Discovery and Development presents practical applications of systems biology to the multiple phases of drug discovery and development. This book explains how the integration of knowledge from multiple sources, and the models that best represent that integration, inform the drug research processes that are most relevant to the pharmaceutical and biotechnology industries. The first book to focus on comprehensive systems biology and its applications in drug discovery and development, it offers comprehensive and multidisciplinary coverage of all phases of discovery and design, including target identification and validation, lead identification and optimization, and clinical trial design and execution, as well as the complementary systems approaches that make these processes more efficient. It also provides models for applying systems biology to pharmacokinetics, pharmacodynamics, and candidate biomarker identification. Introducing and explaining key methods and technical approaches to the use of comprehensive systems biology on drug development, the book addresses the challenges currently facing the pharmaceutical industry. As a result, it is essential reading for pharmaceutical and biotech scientists, pharmacologists, computational modelers, bioinformaticians, and graduate students in systems biology, pharmaceutical science, and other related fields.

10058.11 РУБ

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Rossi John J. RNA Interference. Application to Drug Discovery and Challenges Pharmaceutical Development


RNA Interference: Application to Drug Discovery and Challenges to Pharmaceutical Development provides a general overview of this rapidly emerging field, with a strong emphasis on issues and aspects that are important to a drug development team. The first part covers more general background of RNA interference and its application in drug discovery. In the second part, the book addresses siRNA (small interfering RNA), a pharmaceutically potent form, and its use and delivery in therapeutics along with manufacturing and delivery aspects.

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Practical Utility of Biomarkers in Drug Discovery and Development covers all aspects of biomarker research applied to drug discovery and development and contains state-of-the-art appraisals on the practical utility of genomic, biochemical, and protein biomarkers. Case histories and lessons from successful and unsuccessful applications of biomarkers are included along with key chapters on GLP validation, safety biomarkers and proteomics biomarkers. Regulatory agency perspectives and initiatives both in the US and internationally are also discussed.

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Leading experts illustrate how sophisticated computational data mining techniques can impact contemporary drug discovery and development In the era of post-genomic drug development, extracting and applying knowledge from chemical, biological, and clinical data is one of the greatest challenges facing the pharmaceutical industry. Pharmaceutical Data Mining brings together contributions from leading academic and industrial scientists, who address both the implementation of new data mining technologies and application issues in the industry. This accessible, comprehensive collection discusses important theoretical and practical aspects of pharmaceutical data mining, focusing on diverse approaches for drug discovery—including chemogenomics, toxicogenomics, and individual drug response prediction. The five main sections of this volume cover: A general overview of the discipline, from its foundations to contemporary industrial applications Chemoinformatics-based applications Bioinformatics-based applications Data mining methods in clinical development Data mining algorithms, technologies, and software tools, with emphasis on advanced algorithms and software that are currently used in the industry or represent promising approaches In one concentrated reference, Pharmaceutical Data Mining reveals the role and possibilities of these sophisticated techniques in contemporary drug discovery and development. It is ideal for graduate-level courses covering pharmaceutical science, computational chemistry, and bioinformatics. In addition, it provides insight to pharmaceutical scientists, principal investigators, principal scientists, research directors, and all scientists working in the field of drug discovery and development and associated industries.

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Sets forth the history, state of the science, and future directions of drug discovery Edited by Jie Jack Li and Nobel laureate E. J. Corey, two leading pioneers in drug discovery and medicinal chemistry, this book synthesizes great moments in history, the current state of the science, and future directions of drug discovery into one expertly written and organized work. Exploring all major therapeutic areas, the book introduces readers to all facets and phases of drug discovery, including target selection, biological testing, drug metabolism, and computer-assisted drug design. Drug Discovery features chapters written by an international team of pharmaceutical and medicinal chemists. Contributions are based on a thorough review of the current literature as well as the authors firsthand laboratory experience in drug discovery. The book begins with the history of drug discovery, describing groundbreaking moments in the field. Next, it covers such topics as: Target identification and validation Drug metabolism and pharmacokinetics Central nervous system drugs In vitro and in vivo assays Cardiovascular drugs Cancer drugs Each chapter features a case study, helping readers understand how science is put into practice throughout all phases of drug discovery. References at the end of each chapter serve as a gateway to groundbreaking original research studies and reviews in the field. Drug Discovery is ideal for newcomers to medicinal chemistry and drug discovery, providing a comprehensive overview of the field. Veterans in the field will also benefit from the perspectives of leading international experts in all aspects of drug discovery.

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Ross Stein L. Kinetics of Enzyme Action. Essential Principles for Drug Hunters


Few scientists have the knowledge to perform the studies that are necessary to discover and characterize enzyme inhibitors, despite the vested interest the pharmaceutical industry has in this field. Beginning with the most basic principles pertaining to simple, one-substrate enzyme reactions and their inhibitors, and progressing to a thorough treatment of two-substrate enzymes, Kinetics of Enzyme Action: Essential Principles for Drug Hunters provides biochemists, medicinal chemists, and pharmaceutical scientists with numerous case study examples to outline the tools and techniques necessary to perform, understand, and interpret detailed kinetic studies for drug discovery.

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Raimund Mannhold Biomolecular Simulations in Structure-Based Drug Discovery


A timely and topical survey of modern simulation tools and their applications in real-life drug discovery, allowing for better and quicker results in structure-based drug design. The first part of this practical guide for industry professionals describes common tools used in the biomolecular simulation of drugs and their targets. A critical analysis of the accuracy of the predictions, the integration of modeling with other experimental data combined with numerous case studies from different therapeutic fields enable users to quickly adopt these new methods for their current projects. The second part then shows how these tools can be applied to drug discovery and development projects. Modeling experts from the pharmaceutical industry and from leading academic institutions present real-life examples for important target classes such as GPCRs, kinases and amyloids as well as for common challenges in structure-based drug discovery. With its inclusion of novel methods and strategies for the modeling of drug-target interactions in the framework of real-life drug discovery and development, this application-oriented reference is tailor-made for medicinal chemists and those working in the pharmaceutical industry.

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