Medicinal chemistry is both science and art. The science of medicinal chemistry offers mankind one of its best hopes for improving the quality of life. The art of medicinal chemistry continues to challenge its practitioners with the need for both intuition and experience to discover new drugs. Hence sharing the experience of drug research is uniquely beneficial to the field of medicinal chemistry. Drug research requires interdisciplinary team-work at the interface between chemistry, biology and medicine. Therefore, the topic-related series Topics in Medicinal Chemistry covers all relevant aspects of drug research, e.g. pathobiochemistry of diseases, identification and validation of (emerging) drug targets, structural biology, drugability of targets, drug design approaches, chemogenomics, synthetic chemistry including combinatorial methods, bioorganic chemistry, natural compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions on the molecular level, structure-activity relationships, drug absorption, distribution, metabolism, elimination, toxicology and pharmacogenomics. In general, special volumes are edited by well known guest editors.

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 today's 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.

Vital information for discovering and optimizing new drugs "Understanding the data and the experimental details that support it has always been at the heart of good science and the assumption challenging process that leads from good science to drug discovery. This book helps medicinal chemists and pharmacologists to do exactly that in the realm of enzyme inhibitors." -Paul S. Anderson, PhD This publication provides readers with a thorough understanding of enzyme-inhibitor evaluation to assist them in their efforts to discover and optimize novel drug therapies. Key topics such as competitive, noncompetitive, and uncompetitive inhibition, slow binding, tight binding, and the use of Hill coefficients to study reaction stoichiometry are all presented. Examples of key concepts are presented with an emphasis on clinical relevance and practical applications. Targeted to medicinal chemists and pharmacologists, Evaluation of Enzyme Inhibitors in Drug Discovery focuses on the questions that they need to address: * What opportunities for inhibitor interactions with enzyme targets arise from consideration of the catalytic reaction mechanism? * How are inhibitors evaluated for potency, selectivity, and mode of action? * What are the advantages and disadvantages of specific inhibition modalities with respect to efficacy in vivo? * What information do medicinal chemists and pharmacologists need from their biochemistry and enzymology colleagues to effectively pursue lead optimization? Beginning with a discussion of the advantages of enzymes as targets for drug discovery, the publication then explores the reaction mechanisms of enzyme catalysis and the types of interactions that can occur between enzymes and inhibitory molecules that lend themselves to therapeutic use. Next are discussions of mechanistic issues that must be considered when designing enzyme assays for compound library screening and for lead optimization efforts. Finally, the publication delves into special forms of inhibition that are commonly encountered in drug discovery efforts, but can be easily overlooked or misinterpreted. This publication is designed to provide students with a solid foundation in enzymology and its role in drug discovery. Medicinal chemists and pharmacologists can refer to individual chapters as specific issues arise during the course of their ongoing drug discovery efforts.

Enzyme Inhibitors in Pharmacotherapy explores the role of enzyme inhibitors in treating chronic diseases and infections. It covers enzyme biology, inhibition mechanisms, and pharmacological applications. Featuring detailed discussions and illustrations, the book offers valuable insights for students and practitioners. Written for a global audience, it combines theoretical knowledge with practical drug development advancements.

Soybean protei ns are wi de 1 y used inhuman foods ina vari ety of forms, including baby formulas, flour, soy protein concentrates, soy protein isolates, soy sauces, textured soy fibers, and tofu. The presence of inhibitors of digestive enzymes in soy proteins impairs nutritional quality and possible safety of this impportant legume. Normal processing conditions based on the use of heat do not completely inactivate these inhibitors, so that residual amounts of plant protease inhibitors are consumed by animals and man. Inhibitors of digestive enzymes are present not only in legumes, such as soybeans, lima beans, and kidney beans, but also in nearly all plant foods, including cereals and potatoes, albeit in much smaller amounts. The antinutritional effects of inhibitors of proteolytic enzymes have been widely studied and can be ameliorated by processing and/or sulfur amino acid fortification. A more urgent concern is reports that rats fed diets containing even low levels of soybean-derived inhibitors, which are found in foods such as soy-based baby formulas, may develop over their lifespan pancreatic lesions leading eventually to neoplasia or tumor formation. On the other hand, recent stUdies suggest that certain enzyme inhibitors from plant foods may prevent cancer formation in other tissues. A key question, therefore, is whether inhibitors from plant foods constitute a human health hazard.

Chapter 10 focuses on the interaction of CN- with enzymes containing vanadium, manganese, non-heme iron, and zinc, and the inhibiting properties of this ligand, allowing its use as a probe. The reaction mechanism of the molybdenum hydroxylase xanthine oxidoreductase is revisited in Chapter 11; previously a molybdenum-carbon bond was postulated but now proof is presented against its formation. The terminating Chapter 12 reviews briefly the most popular computational approaches employed in theoretical studies of bioorganometallic species by providing detailed examples.

Extensively revised and updated, the new edition of the highly regarded Handbook of Proteolytic Enzymes is an essential reference for biochemists, biotechnologists and molecular biologists. Edited by world-renowned experts in the field, this comprehensive work provides detailed information on all known proteolytic enzymes to date. This two-volume set unveils new developments on proteolytic enzymes which are being investigatedin pharmaceutical research for such diseases as HIV, Hepatitis C, and the common cold. Volume I covers aspartic and metallo petidases while Volume II examines peptidases of cysteine, serine, threonine and unknown catalytic type. A CD-ROM accompanies the book containing fully searchable text, specialised scissile bond searches, 3-D color structures and much more. - The only comprehensive book on proteolytic enzymes - Includes 671 chapters, each written by experts in their field, on proteolytic enzymes from all groups of living organisms and the viruses, including those that are currently major targets of pharmaceutical research - Accompanying CD-ROM provides fully searchable text, 2D structures of peptidases in color and links directly to PubMed and MEROPS databases - Each chapter describes in detail the enzyme name, its history, activity and specificity, structural chemistry, preparation, biological aspects and distinguishing features - Over 1000 peptidases included

Originally, it was our intention to produce a single-volume book covering all aspects and approaches to the problem of specific inhibitors of respiratory viruses. However, as the work progressed it became obvious that certain chapters, because of the research interests of the authors, concentrated particularly on influenza viruses. It seemed logical therefore, to divide the book into two volumes, the first emphasizing influenza and the second concentrating on other viruses as well as discussing important general aspects of drug screening and clinical testing, although the second volume does have some chapters which deal mainly with influenza.

This book is the first to provide both a broad overview of the current methodologies being applied to drug design and in-depth analyses of progress in specific fields. It details state-of-the-art approaches to pharmaceutical development currently used by some of the world's foremost laboratories. The book features contributors from a variety of fields, new techniques, previously unpublished data, and extensive reference lists.

In this volume, the medicinal chemistry of the rapidly expanding family of retinoids, of promising semi-synthetic erythromycins and of the multifaceted amidines is reviewed. Another chapter continues the coverage of inorganic elements which have a medical role; recent studies on the various biological roles of manganese are also examined. Inhibition of enkephalin-degrading enzymes is reviewed, as are studies of the digitalis recognition site which are expected to lead to the development of more highly selective inotropic drugs. This work should be of value to medicinal chemists, pharmacists and pharmacologists. It should also be appreciated by all newcomers, as well as those who wish to be kept up to date with recent work on these topics.