As research progresses and information continues to proliferate in the field of molecular design for therapeutic use, there is a need for a reference that brings current theory and proven practice together in a how-to volume. This reference guides scientists new to the field on how to design small molecules that interact with critical protein targets. The chapters condense useful material into a manageable format which is carefully organized and presented. It offers an essential resource for a variety of chemists in academia, and the biotech and pharmaceutical industries, as well as professionals in complementary fields.

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

Burger’s Medicinal Chemistry, Drug Discovery and Development Explore the freshly updated flagship reference for medicinal chemists and pharmaceutical professionals The newly revised eighth edition of the eight-volume Burger’s Medicinal Chemistry, Drug Discovery and Development is the latest installment in this celebrated series covering the entirety of the drug development and discovery process. With the addition of expert editors in each subject area, this eight-volume set adds 35 chapters to the extensive existing chapters. New additions include analyses of opioid addiction treatments, antibody and gene therapy for cancer, blood-brain barrier, HIV treatments, and industrial-academic collaboration structures. Along with the incorporation of practical material on drug hunting, the set features sections on drug discovery, drug development, cardiovascular diseases, metabolic diseases, immunology, cancer, anti-Infectives, and CNS disorders. The text continues the legacy of previous volumes in the series by providing recognized, renowned, authoritative, and comprehensive information in the area of drug discovery and development while adding cutting-edge new material on issues like the use of artificial intelligence in medicinal chemistry. Included: Volume 1: Methods in Drug Discovery, edited by Kent D. Stewart Volume 2: Discovering Lead Molecules, edited by Kent D. Stewart Volume 3: Drug Development, edited by Ramnarayan S. Randad and Michael Myers Volume 4: Cardiovascular, Endocrine, and Metabolic Diseases, edited by Scott D. Edmondson Volume 5: Pulmonary, Bone, Immunology, Vitamins, and Autocoid Therapeutic Agents, edited by Bryan H. Norman Volume 6: Cancer, edited by Barry Gold and Donna M. Huryn Volume 7: Anti-Infectives, edited by Roland E. Dolle Volume 8: CNS Disorders, edited by Richard A. Glennon Perfect for research departments in the pharmaceutical and biotechnology industries, Burger’s Medicinal Chemistry, Drug Discovery and Development can be used by graduate students seeking a one-stop reference for drug development and discovery and deserves its place in the libraries of biomedical research institutes, medical, pharmaceutical, and veterinary schools.

This timely guide to kinase inhibitor drug development is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Edited by the pioneers in the field, on the drug development side this ready reference discusses classical medicinal chemistry approaches as well as current chemical genomics strategies. On the clinical side, both current and future therapeutic application areas for kinase inhibitor drugs are addressed, with a strong focus on oncology drugs. Backed by recent clinical experience with first-generation drugs in the battle against various forms of cancer, this is crucial reading for medicinal, pharmaceutical and biochemists, molecular biologists, and oncologists, as well as those working in the pharmaceutical industry.

Principles of Tumors: A Translational Approach to Foundations, Second Edition, provides a concise summary of translational/interdisciplinary topics on the various aspects of tumors, especially abnormalities in their cells, their causes and effects on patients. Topics discussed include how genomic abnormalities in tumors may result from the actions of carcinogens and how genomic changes determine the cell biological/morphological abnormalities in tumor cell populations. In addition, the relationships between tumor cell genomics and therapeutic outcomes are described. There are also supporting appendices on general bioscience, including the principles of histology (the cells and tissues of the body), genetics, pathology, radiology and pharmacology. This book gives a thorough, detailed, yet concise account of the main bioscience, clinical and therapeutic aspects of tumors. It emphasizes the translational aspects of research into tumors with extensive discussions of interdisciplinary issues. The content in this book will be invaluable for researchers and clinicians involved in collaborative projects where it is necessary to understand fundamental issues in other branches of biomedicine. - Presents content that has been totally updated with the most recent developments of the field, including new chapters on tumor imaging exams, new surgical techniques, immunotherapy, gene therapy, and several novel therapies using natural and synthetic compounds - Presents translational approaches for every topic to improve conceptual insights for new research projects - Covers a broad range of subjects, making it easier for the reader to understand related fields - Includes diagrams for complex topics to aid in understanding for non-specialists

Chemogenomics brings together the most powerful concepts in modern chemistry and biology, linking combinatorial chemistry with genomics and proteomics. This first reference devoted to the topic covers all stages of the early drug discovery process, from target selection to compound library and lead design. With the combined expertise of 20 research groups from academia and leading pharmaceutical companies, this is a must-have for every drug developer and medicinal chemist applying the powerful methods of chemogenomics to speed up the drug discovery process.

""Frontiers in Medicinal Chemistry" is an Ebook series devoted to the review of areas of important topical interest to medicinal chemists and others in allied disciplines. "Frontiers in Medicinal Chemistry" covers all the areas of medicinal chemistry, incl"

This book brings together drug design practitioners, all leaders in their field, who are actively advancing the field of quantitative methods to guide drug discovery, from structure-based design to empirical statistical models - from rule-based approaches to toxicology to the fields of bioinformatics and systems biology. The aim of the book is to show how various facets of the drug discovery process can be addressed in a quantitative fashion (ie: numerical analysis to enable robust predictions to be made). Each chapter includes a brief review of the topic showing the historical development of quantitative approaches, a survey/summary of the current state-of-the-art, a selection of well chosen examples with some worked through and an appreciation of what problems remain to be overcome as well as an indication of how the field may develop. After an overview of quantitative approaches to drug design the book describes the development of concepts of "drug-like properties", of quantitative structure-activity relationships and molecular modelling, and in particular, structure-based design approaches to guide lead optimisation. How to manage and describe chemical structures, underpins all quantitative approaches to drug design and these are described in the following chapters. The next chapter covers the value of a quantitative approach, and also the challenge which is to describe the confidence in any prediction, and methods to assess predictive model quality. The later chapters describe the application of quantitative approaches to describing and optimising potency, selectivity, drug metabolism and pharmacokinetic properties and toxicology, and the design of chemical libraries to feed the screening approaches to lead generation that underpin modern drug discovery. Finally the book describes the impact of bioinformatics, current status of predicting ligand affinity direct from the protein structure, and the application of quantitative approaches to predicting environmental risk. The book provides a summary of the current state-of-the-art in quantitative approaches to drug design, and future opportunities, but it also provides inspiration to drug design practitioners to apply careful design, to make best use of the quantitative methods that are available, while continuing to improve them. Drug discovery still relies heavily on random screening and empirical screening cascades to identify leads and drugs and the process has many failures to deliver only a small handful of drugs. With the rapidly escalating costs of drug discovery and development together with spiralling delivery, quantitative approaches hold the promise of shifting the balance of success, to enable drug discovery to maintain its economic viability.

The insights following the wake of the Human Genome project are radically influencing our understanding of the molecular basis of life, health and disease. The improved accuracy and precision of clinical diagnostics is also beginning to have an impact on therapeutics in a fundamental way. This book is suitable for undergraduate medical students, as part of their basic sciences training, but is also relevant to interested under- and postgraduate science and engineering students. It serves as an introductory text for medical registrars in virtually all specialties, and is also of value to the General Practitioner wishing to keep up to date, especially in view of the growing, internet-assisted public knowledge of the field. There is a special focus on the application of molecular medicine in Africa and in developing countries elsewhere.

This is an innovative textbook for undergraduates as well as postgraduates offering basic knowledge of biology. Its aim is to provide state-of-the-art information about this developing science that has the potential to replace existing biological approaches to study genes and proteins. The chapters are explained in a concise yet detailed manner, including ample cross-references, references to literature and databases, tables and illustrations. The book's sound approach to this intricately complex field makes it an exceptional resource for further exploration into biochemistry, molecular biology, genomics and drug designing fields. Abundant learning features make this book the ideal teaching and learning tool. KEY FEATURES • Illustrations to bolster understanding of complex biochemical relations • Tables for quick access to precise data • Extensive end-of-chapter exercises and references • The most basic details furnished for those who are new to biology • User-friendly, Internet-based bioinformatics tools that allow researchers to extract information from databases and analyze it • Analysis of one software tool discussed in each chapter step-by-step from entering the input till interpretation of the results This is an in-depth textbook written for the biologist who wants a thorough understanding of the popular bioinformatics programs and molecular databases currently in use. It provides a broad, application-oriented overview of this technology.