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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.
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.
Enzyme inhibitory agents are attractive because of their application in treating different ailments. The absence of enzymes produce a number of diseases. Medicinal plants are a rich source of producing secondary metabolites which showed broad-spectrum enzyme inhibitory potential. The position of enzyme inhibitors as new drugs is vast since these compounds have been used for the treatment of various physiological disorders. Bioactive secondary metabolites can deliver excellent pharmacophore patterns for drugs related to numerous illnesses. This book chapter is planned to document the enzyme inhibitory potential of natural compounds, medicinal plant extract, and its isolated compounds.
The past decade has seen the reappearance of natural products as a valuable source of potent therapeutics. Here, experts on bioactive natural products cover the full spectrum of clinically relevant enzymes that are known to be targeted by natural products. Key enzymes include acetylcholine esterase, angiotensin-I-converting enzyme, cyclooxygenase, dihydrofolate reductase, phospholipase A2, respiratory complexes, and many more. By connecting the diversity of medicinal natural product sources with their potential clinical applications, this volume serves as a companion for the medicinal chemist looking for innovative small molecule compounds as well as for pharmacologist interested in the clinical effects and mode of action of herbal and traditional medicines.
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.
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.
The application of biotechnology in the food sciences has led to an increase in food production and enhanced the quality and safety of food. Food biotechnology is a dynamic field and the continual progress and advances have not only dealt effectively with issues related to food security but also augmented the nutritional and health aspects of food. Advances in Food Biotechnology provides an overview of the latest development in food biotechnology as it relates to safety, quality and security. The seven sections of the book are multidisciplinary and cover the following topics: GMOs and food security issues Applications of enzymes in food processing Fermentation technology Functional food and nutraceuticals Valorization of food waste Detection and control of foodborne pathogens Emerging techniques in food processing Bringing together experts drawn from around the world, the book is a comprehensive reference in the most progressive field of food science and will be of interest to professionals, scientists and academics in the food and biotech industries. The book will be highly resourceful to governmental research and regulatory agencies and those who are studying and teaching food biotechnology.
This new book encompasses, in great detail, the most recent progress made in the isolation and separation of natural products. It covers antibiotics, marine and plant-derived substances, enzyme inhibitors and interferons. The most recent separation methodology is described. Although there is a bias toward antibiotics, it was done because this is still the largest natural products area of research.The fourteen chapters are written by experts in their respective fields. The first two chapters are largely devoted to new methodology applied to purification of a variety of compounds. They include an extensive review and new applications of counter-current chromatography and the newly emerging HPLC-photodiode array technology. Chapter 3 provides a review of affinity chromatography applied to the separation of antibiotics for the first time. Next are chapters on antimicrobials with an update on all the most recent &bgr;-lactam (after 1976) discoveries. A comprehensive review of a very important class of antiparasitic agents - the avermectins - follows. An update of isolation and purification of a variety of marine-derived compounds is next. The succeeding chapter is a comprehensive review of the most recent developments in isolation and purification of interferons. This is followed by a discussion of enzyme inhibitors and their isolation and purification and ties in with a chapter on plant-derived natural products, some of which are also in this same category. The final chapter is a futuristic essay indicating the isolation of minute amounts of natural products and the fascinating biological properties which they possess.The book has extensive isolation schemes, tables, figures and chemical structures. In many instances a short summary of the producing organism, brief chemical description and structure and biological activity of the compounds is presented. Detailed information of extraction, separation and purification techniques follow. Each chapter has an extensive bibliography and, where applicable, an appendix showing sources of materials and equipment. A detailed index to the subject matter is included at the end of the book.The book thus offers the reader: up-to-date reviews (including 1988) of specific topics in the natural products field not to be found elsewhere; information on new chromatographic methods and techniques described in sufficient detail to be utilized by investigators in this area of research; and extensive references to enable the serious researcher to pursue particular information. It will appeal to pharmaceutical and natural products researchers and is a valuable acquisition for university chemistry and biochemistry departments.
Hyaluronidase enzyme degrades hyaluronan, the primary component of the extracellular matrix found in connective tissues animals and on the surface of certain pathogenic bacteria. The degradation of hyaluronan is linked to a wide range of physiological and pathological process. Inhibiting the hyaluronidase enzyme is thus significant as an approach to treat a variety of diseases and health conditions such as anti-fertility, anti-tumor, antimicrobial, and anti-venom/toxin agents. HAase inhibitors of different chemical types have been identified include both synthetic compounds and constituents obtained from naturally sources. Plant natural products as HAase inhibitors are unique due to their structural features and diversity. Medicinal plants have historically been used as contraceptives, antidote for snakebites and to promote wound healing. In recent years, small molecules, particularly plant natural products (alkaloids, flavonoids, polyphenol and flavonoids, triterpenes and steroids) possessing potent HAase have been discovered. A number of plant species from various families, which have folk medicinal claims for these ailments (related to hyaluronan disturbances) were scientifically proven for their potential to block HAase enzymes.