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Building on the success of the previous editions, the Textbook of Drug Design and Discovery, Fifth Edition, has been thoroughly revised and updated to provide a complete source of information on all facets of drug design and discovery for students of chemistry, pharmacy, pharmacology, biochemistry, and medicine. The information is presented in an up-to-date review form with an underlying and fundamental focus on the educational aspects. Beginning with an introduction to drug design and discovery, the first eight chapters cover molecular recognition, ligand-based drug design, and biostructure-based drug design. The authors also discuss drug-like properties and decision making in medicinal chemistry, chemical biology, natural products in drug discovery, and in vivo imaging in drug discovery. The middle six chapters provide an overview of peptide and protein drug design, prodrugs in drug design and development, and enzyme inhibitors. The authors also go through receptors (structure, function, and pharmacology), ion channels (structure and function), and neurotransmitter transporters (structure, function, and drug binding). The following chapters address important neurotransmitter systems, GABA and glutamic acid receptors and transporter ligands, acetylcholine, histamine, dopamine and serotonin, and opioid and cannabinoid receptors. The book concludes with an examination of neglected diseases, anticancer agents, tyrosine kinase receptors, and antibiotics.
The molecular biological revolution and the mapping of the human genome continue to provide new challenges and opportunities for drug research and design. Future medicinal chemists and drug designers must have a firm background in a number of related scientific disciplines in order to understand the conversion of new insight into lead structures and subsequently into drug candidates. Classroom tested and student approved, Textbook of Drug Design and Discovery, Fourth Edition describes the manner in which medicinal chemists utilize the various fields upon which they draw and the specific strategies they employ to advance promising molecules into clinical use for the treatment of disease. This text integrates a number of related scientific disciplines, including advanced synthetic chemistry, computational chemistry, biochemistry, structural biology, and molecular pharmacology, to provide current and comprehensive information on all aspects of drug design and discovery. Extensively revised, new topics in the fourth edition include: Biostructure-based and ligand-based drug design Chemical biology Natural products Imaging Neurotransmitter transporters Opioid and cannabinoid receptors Hypnotics Neglected diseases Immunomodulating agents Antibiotics The first part of the book covers general aspects, methods, and principles for drug design and discovery, and the second part covers specific targets and diseases. The text contains more than 300 color figures and 24 tables for rapid assimilation. Each chapter includes references for further study. Most chapters also provide the background and history needed to provide a context for students, as well as conclusions that summarize the points most relevant to emerging areas of research in drug design.
This volume provides an introduction to medicinal chemistry. It covers basic principles and background, and describes the general tactics and strategies involved in developing an effective drug.
This title demonstrates how advanced formulation designs and delivery technologies can be used to improve drug efficacy and treatment outcomes in particular therapeutic categories or disease states. It discusses nanoparticle systems for cancer treatments, and also presents cutting edge immono-regulation agents for transplantation and the local targeting of drugs, especially poorly water soluble drugs to provide enhanced therapeutic outcomes. In addition, this title highlights areas of therapy showing the most promise for improvement in clinical outcomes via advanced formulation design.
Practical Bioinformatics is specifically designed for biology majors, with a heavy emphasis on the steps required to perform bioinformatics analysis to answer biological questions. It is written for courses that have a practical, hands-on element and contains many exercises (for example, database searches, protein analysis, data interpretation) to complement the straightforward and practical topics. The chapters are focused on DNA, RNA, and protein sequence analysis‹frequently performed subsets of the field of bioinformatics‹taking the reader through the commonly asked question Ðwhat can I learn about this sequence?Ó A special note to established scientists: new genomic sequences are being published at an accelerating pace. Although new technology has led to unprecedented accuracy of the sequence, incomplete and challenging assemblies along with imperfect predictive methods are still generating gene models that require verification. With the sequence analysis skills learned from this book, features such as missing exons and incorrect termini can be easily recognized and more accurate gene models can be constructed.
The Organic Chemistry of Drug Design and Drug Action, Third Edition, represents a unique approach to medicinal chemistry based on physical organic chemical principles and reaction mechanisms that rationalize drug action, which allows reader to extrapolate those core principles and mechanisms to many related classes of drug molecules. This new edition includes updates to all chapters, including new examples and references. It reflects significant changes in the process of drug design over the last decade and preserves the successful approach of the previous editions while including significant changes in format and coverage. This text is designed for undergraduate and graduate students in chemistry studying medicinal chemistry or pharmaceutical chemistry; research chemists and biochemists working in pharmaceutical and biotechnology industries. Updates to all chapters, including new examples and references Chapter 1 (Introduction): Completely rewritten and expanded as an overview of topics discussed in detail throughout the book Chapter 2 (Lead Discovery and Lead Modification): Sections on sources of compounds for screening including library collections, virtual screening, and computational methods, as well as hit-to-lead and scaffold hopping; expanded sections on sources of lead compounds, fragment-based lead discovery, and molecular graphics; and deemphasized solid-phase synthesis and combinatorial chemistry Chapter 3 (Receptors): Drug-receptor interactions, cation-π and halogen bonding; atropisomers; case history of the insomnia drug suvorexant Chapter 4 (Enzymes): Expanded sections on enzyme catalysis in drug discovery and enzyme synthesis Chapter 5 (Enzyme Inhibition and Inactivation): New case histories: for competitive inhibition, the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib and Abelson kinase inhibitor, imatinib for transition state analogue inhibition, the purine nucleoside phosphorylase inhibitors, forodesine and DADMe-ImmH, as well as the mechanism of the multisubstrate analog inhibitor isoniazid for slow, tight-binding inhibition, the dipeptidyl peptidase-4 inhibitor, saxagliptin Chapter 7 (Drug Resistance and Drug Synergism): This new chapter includes topics taken from two chapters in the previous edition, with many new examples Chapter 8 (Drug Metabolism): Discussions of toxicophores and reactive metabolites Chapter 9 (Prodrugs and Drug Delivery Systems): Discussion of antibody–drug conjugates
The Practice of Medicinal Chemistry fills a gap in the list of available medicinal chemistry literature. It is a single-volume source on the practical aspects of medicinal chemistry. Considered ""the Bible"" by medicinal chemists, the book emphasizes the methods that chemists use to conduct their research and design new drug entities. It serves as a practical handbook about the drug discovery process, from conception of the molecules to drug production. The first part of the book covers the background of the subject matter, which includes the definition and history of medicinal chemistry, the measurement of biological activities, and the main phases of drug activity. The second part of the book presents the road to discovering a new lead compound and creating a working hypothesis. The main parts of the book discuss the optimization of the lead compound in terms of potency, selectivity, and safety. The Practice of Medicinal Chemistry can be considered a ""first-read"" or ""bedside book"" for readers who are embarking on a career in medicinal chemistry. NEW TO THIS EDITION: * Focus on chemoinformatics and drug discovery * Enhanced pedagogical features * New chapters including: - Drug absorption and transport - Multi-target drugs * Updates on hot new areas: NEW! Drug discovery and the latest techniques NEW! How potential drugs can move through the drug discovery/ development phases more quickly NEW! Chemoinformatics

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