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This book, a part of the series Studies in Medicinal Chemistry, details the biological inhibitors that reflect drug discovery in treating human diseases, including cardiovascular, nervous, inflammatory, hormonal and metabolic processes. Compounds for fungal diseases and HIV/AIDS are also covered.
This book provides an overview of the latest developments and future challenges in enzyme inhibitor research. It discusses the general enzyme inhibitory principles and mechanisms in enzyme activity regulation and application of enzyme inhibitors in different areas and sectors. The major areas of applications of enzyme inhibitors covered in this book are human health management, agriculture, food processing and research, which leads to drug discovery or enzyme activity mechanisms. The book also identifies the gaps in the existing knowledge and opens up new research ideas in this important area. Currently, most enzyme inhibitors are reported to inhibit various classes of enzymes. These enzyme inhibitors are the focus of the scientific community because they may answer an increasing array of questions in the research area of biological sciences, including biochemistry, medicine, physiology, pharmacy, agriculture, ecology etc. It also serves as a useful tool in the study of enzyme structures and reaction mechanisms and in the development of technologies in agriculture, food processing, and health management. Chapters in this book cover topics such as plant-derived inhibitors of serine proteases, pancreatic lipase (PL) inhibitors from indigenous medicinal plants, amylase inhibitors and their applications in agriculture and food processing industries and advances in silico techniques used in the study of enzyme inhibitors. The book will serve as a valuable resource for students and researchers in Life Sciences, agriculture, medicine, food processing, and allied industries.
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.
Over the recent years, medicinal chemistry has become responsible for explaining interactions of chemical molecule processes such that many scientists in the life sciences from agronomy to medicine are engaged in medicinal research. This book contains an overview focusing on the research area of enzyme inhibitor and activator, enzyme-catalyzed biotransformation, usage of microbial enzymes, enzymes associated with programmed cell death, natural products as potential enzyme inhibitors, protease inhibitors from plants in insect pest management, peptidases, and renin-angiotensin system. The book provides an overview on basic issues and some of the recent developments in medicinal science and technology. Especially, emphasis is devoted to both experimental and theoretical aspect of modern medicine. The primary target audience for the book includes students, researchers, chemists, molecular biologists, medical doctors, pharmacologists, and professionals who are interested in associated areas. The textbook is written by international scientists with expertise in biochemistry, enzymology, molecular biology, and genetics, many of which are active in biochemical and pharmacological research. I would like to acknowledge the authors for their contribution to the book. We hope that the textbook will enhance the knowledge of scientists in the complexities of some medical approaches; it will stimulate both professionals and students to dedicate part of their future research in understanding relevant mechanisms and applications of pharmacology.
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 mar
This book, a part of the series Studies in Medicinal Chemistry, details the biological inhibitors that reflect drug discovery in treating human diseases, including cardiovascular, nervous, inflammatory, hormonal and metabolic processes. Compounds for fungal diseases and HIV/AIDS are also covered.
Metabolic inhibitors and receptor antagonists are indispensable tools for the molecular life scientist. By blocking specific enzymes or receptor-mediated signal transduction cascades, they simplify the analysis of complex cellular processes especially when it is essential to demonstrate that a process of interest is functionally linked to a particular enzyme or receptor. From antibiotics to statins, modern medicine relies on the reliability and ease-of-use of enzyme- and receptor-directed inhibitors and antagonists.The Inhibitor Index is a comprehensive, curated compendium of over 7,800 enzyme inhibitors and receptor antagonists, including many toxins, poisons, and metabolic uncouplers.
Metabolic Inhibitors: A Comprehensive Treatise, Volume I focuses on the properties of inhibitors of metabolic processes or enzyme systems. The book explores a wide range of substances that interfere with (and usually retard) metabolic and enzymic processes, emphasizing the inhibitor rather than the metabolic or enzymic system that is affected. Organized into 15 chapters, this volume begins with a historical overview of research on the mode of action of biological inhibitors, touching on the principle of competitive inhibition by structural analogues. The book then turns to the concept of a competitive enzymic relationship by growth inhibitory analogues and their corresponding amino acids; the metabolic inhibitory effects of polypeptides and proteins; and the use of pentoses as analogues in carbohydrate metabolism. The reader is also introduced to the metabolic inhibitory effects of fatty acids; the intermediary metabolism of phospholipids; and the inhibition of purine and pyrimidine analogues. The remaining chapters discuss the role of nucleic acids and nucleoproteins in the regulation of cellular metabolism and the inhibition of amino acid decarboxylases, cholesterol, and steroid biosynthesis. This book will be of value to biochemists, advanced students, medical research workers, and research workers in the various fields of biological chemistry, as well as those working in the microbiological, botanical, and other agricultural fields.
Metabolic Inhibitors: A Comprehensive Treatise, Volume II charts the major advances that have been made in understanding metabolic inhibition and inhibitors. The book explores the inhibition of enzymes, such as catechol amines, acetylcholinesterases, and succinic dehydrogenases, as well as inhibitors of processes ranging from gas transport to photosynthesis, nitrogen fixation, nitrification, and oxidative phosphorylation. Organized into 23 chapters, this volume begins with a discussion on the biosynthesis of nicotinamide adenine dinucleotide and dinucleotide analogues. The reader is then introduced to the biochemical significance and mode of action of antibiotics; substances interfering with the biogenesis and metabolism of catechol amines; and inhibition of enzyme activities by thioarsenites. Some chapters focus on mercaptide-forming agents, biological alkylating agents, organophosphates, and carbamates, while others examine the metabolic inhibitory effects of quinones, fungicides, and surface active agents. The book also considers the effects of anesthetics, depressants, and tranquilizers on cerebral metabolism, and then concludes with a chapter on inhibition caused by radiation. This book is a valuable resource for biochemists, advanced students, medical research workers, and research workers in the fields of biological chemistry, microbiology, botany, and agriculture.
This book provides an overview of the world market of therapeutic enzymes and enzyme inhibitors, rare diseases, orphan drugs, the costs of drug development and therapies, and enzymes in downstream processing of pharmaceuticals. It discusses carbonic anhydrase inhibitors and their multiple drug interactions, carboxylesterase inhibitors for pharmaceutical applications, employment of inhibitors for the treatment of neurodegenerative diseases, use of engineered proteins, bioactive peptides, and fibrinolytic enzymes for thrombolytic therapy, and enzymes important for the design and development of new drugs/drug metabolites such as aldehyde oxidases and cytochrome P450 enzymes and the role the latter play in vascular biology and pathophysiology. The treatment of cancer is explored in connection with enzymatic amino acid deprivation therapies and new drugs that act as chemical degraders of oncogenic proteins. The book also introduces the resistance mechanisms of cancer. Furthermore, it provides an insight into the relationship between pathological conditions of cardiovascular disease and oxidative stress. The text also focuses on the potential use of nanoparticles as carriers for enzymes with medical relevance, computer-aided drug design for the identification of multi-target directed ligands, and the development of improved therapeutics through a glycan-“designer” approach. It concludes with an introduction to the chemoenzymatic synthesis of drugs.