H. John Smith - Böcker

A high proportion of drugs currently coming to market exert their action in the body by inhibition of a target enzyme involved in a particular body function or in a bacterium, protozoon, or virus causing an infection. This book extends the previous volume in providing a comprehensive coverage of more recently recognised target enzymes and their known inhibitors, and within this framework of knowledge demonstrates how the drug designer uses all available information to develop a specific therapeutic agent. Drug design is an interdisciplinary art and the text illustrates the pathway followed from the initial design concept and synthesis of an inhibitor through its in vitro and in vivo assessments to clinical trial, a process involving chemists, biochemists, pharmacologies, and clinicians.

Focusing on the development of enzyme inhibitors as therapeutic drugs, Enzymes and Their Inhibitors: Drug Development provides a concise overview of the chemistry of major types of enzymes and their inhibitors. The opening chapters introduce readers to the structure, functions, mechanisms, and kinetics of enzymes, including their use as disease markers, analytical reagents, and in industrial processes. Subsequent chapters discuss the different types of enzyme inhibitors and the principles involved in developing them into effective drugs. This outstanding text, also valuable as a professional reference, will be useful to all students of pharmacology and medicinal chemistry.

Cellular proteinases and their physiological role in normal and disease states have been the subject of great interest over recent decades. At present, specific protease inhibitors are exploited both as tools in unraveling the role of individual proteinases in particular cellular processes and for the development of chemotherapeutic agents for the treatment of various disorders. Proteinase and Peptidase Inhibition presents updated progress reports on the characterization of a wide range of cellular proteinases whose inhibitors may hold the key to the development of new drugs. Introductory chapters deal with the broad enzyme classes, inhibitor types and regulatory mechanisms governing proteinase activity. The target enzymes themselves, together with all aspects of their inhibition and inhibitor design, are comprehensively described. The classification of target enzymes by structural similarity, rather than by pharmacological effects, provides a new and coherent platform for understanding how inhibition of different targets can lead to the same therapeutic outcomes. This is a valuable reference book that will appeal to both academic and industrial researchers in the fields of medicinal chemistry, drug design and development, pharmacology, biochemistry, and molecular and cell biology.

Cellular proteinases and their physiological role in normal and disease states have been the subject of great interest over recent decades. At present, specific protease inhibitors are exploited both as tools in unraveling the role of individual proteinases in particular cellular processes and for the development of chemotherapeutic agents for the treatment of various disorders. Proteinase and Peptidase Inhibition presents updated progress reports on the characterization of a wide range of cellular proteinases whose inhibitors may hold the key to the development of new drugs. Introductory chapters deal with the broad enzyme classes, inhibitor types and regulatory mechanisms governing proteinase activity. The target enzymes themselves, together with all aspects of their inhibition and inhibitor design, are comprehensively described. The classification of target enzymes by structural similarity, rather than by pharmacological effects, provides a new and coherent platform for understanding how inhibition of different targets can lead to the same therapeutic outcomes. This is a valuable reference book that will appeal to both academic and industrial researchers in the fields of medicinal chemistry, drug design and development, pharmacology, biochemistry, and molecular and cell biology.

Advances in knowledge and technology have revolutionized the process of drug development, making it possible to design drugs for a given target or disease. Building on the foundation laid by the previous three editions, Smith and Williams’ Introduction to the Principles of Drug Design and Action, Fourth Edition includes the latest information on topics such as gene therapy, computer-aided design, and molecular techniques including proteomics. Using real-world examples that illustrate the principles of drug design, the author explores the discovery of lead compounds and their manipulation in the production of non-toxic, metabolically stable drug candidates that will interact with target receptors in a predicted fashion.See what’s new in the Fourth Edition: Fully updates and expands the contents Coverage of agonists and antagonists of neuro-transmitters Information on the design of stable peptide-like drugs The human genome and its impact on drug discovery and development Advances in therapy and pharmacokinetics Adopting a from-the-bench-to-the-marketplace approach, the book provides a thorough grounding in rational drug design. It emphasizes principles and elucidates a framework for basic drug design into which current and, more importantly, future drugs will fit.

Focusing on the development of enzyme inhibitors as therapeutic drugs, Enzymes and Their Inhibitors: Drug Development provides a concise overview of the chemistry of major types of enzymes and their inhibitors. The opening chapters introduce readers to the structure, functions, mechanisms, and kinetics of enzymes, including their use as disease markers, analytical reagents, and in industrial processes. Subsequent chapters discuss the different types of enzyme inhibitors and the principles involved in developing them into effective drugs. This outstanding text, also valuable as a professional reference, will be useful to all students of pharmacology and medicinal chemistry.