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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.
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.
Natural Products have been important sources of useful drugs from prehistoric times to the present. This book gives an overview about this field and provides important recent contributions to the discovery of new drugs generated by research on natural products. Total synthesis of natural products with interesting biological activities is paving the way for the preparation of new and improved analogs. The methods of combinatorial chemistry permit the selection of the best drug from a large number of candidates. Beyond synthesis and evaluation of organic molecules a number of new bioorganic methods are coming to the fore and will be discucced in this isue of the ERnst schering Research Foundation workshop proceedings.
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.
Metalloenzymes: From Bench to Bedside offers a thorough overview of metalloenzymes, spanning biochemical and structural features, pharmacology, and biotechnological applications. After a brief overview, international experts in the field discuss a wide range of magnesium, calcium, zinc, manganese, nickel, iron, copper, cadmium, molybdenum, and tungsten enzymes, along with catalytic roles within their active sites. With a uniform approach throughout, each chapter includes the structure and function of the enzyme, physiologic and pathologic roles, inhibitors and activators of the enzyme (and their design), and clinical agents or compounds applied in medicine and drug discovery. This book enables scientists across academia and industry to adopt ongoing metalloenzyme research, and continuous discovery of novel metalloenzymes, in new life science studies and clinical applications. - Examines a range of metalloenzymes, from biochemistry to pharmacology and drug design - Each chapter examines enzyme structure and function, physiologic and pathologic roles, inhibitors and activators, and clinical application - Features chapter contributions from international experts in the field
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Recent Advances in Micro- and Macroalgal Processing A comprehensive review of algae as novel and sustainable sources of algal ingredients, their extraction and processing This comprehensive text offers an in-depth exploration of the research and issues surrounding the consumption, economics, composition, processing and health effects of algae. With contributions from an international team of experts, the book explores the application of conventional and emerging technologies for algal processing. The book includes recent developments such as drying and milling technologies along with advancements in sustainable greener techniques. The text also highlights individual groups of compounds including polysaccharides, proteins, polyphenols, carotenoids, lipids and fibres from algae. The authors provide insightful reviews of the traditional and more recent applications of algae/algal extracts in food, feed, pharmaceutical and cosmetics products. Offering a holistic view of the various applications, the book looks at the economic feasibility, market trends and considerations, and health hazards associated with algae for industrial applications. This important book: Provides a comprehensive overview of algal biomolecules and the role of emerging processing technologies Explores the potential biological and health benefits of algae and their applications in food, pharmaceuticals and cosmetic products Includes a current review of algal bioactives and processing technologies for food and ingredient manufacturers Contains contributions from leading academic and industrial experts Written for food scientists, allied researchers and professional food technologists, Recent Advances in Micro- and Macroalgal Processing: Food and Health Perspectives offers a guide to the novel processing and extraction techniques for exploring and harnessing the immense potential of algae.
This book is a printed edition of the Special Issue "Impact of Bioactive Peptides on Human Health" that was published in Nutrients
Type 2 diabetes (T2D), also known as non-insulin-dependent diabetes mellitus (NIDDM), is a condition in which cells fail to respond to insulin properly. As the disease progresses, the body does not produce enough insulin. There are several classes of anti-diabetic medications available, including the oral agent metformin. This medication is recommended as first-line treatment for T2D, except for those patients with severe kidney or liver problems. This book discusses the molecular mechanism, pharmacokinetics, and uses of metformin, as well as presents information on adverse drug reactions, drug interactions, and the potential use of metformin in tuberculosis.
Presents the latest research and applications for a new, promising approach to fighting infectious diseases Enzybiotics is a promising way of fighting bacterial or fungal infectious diseases by using viruses or viral-derived lysins. Drawing from the fields of medicinal chemistry, microbiology, genetics, and biochemistry, this book presents the state of the science in enzybiotics research, fully exploring its emerging therapeutic applications. The book begins with four chapters that review the potential applications, possible advantages, and phylogeny of enzybiotics. Next, the book explores: A new approach to controlling infections using Gram-negative bacteria Bacteriophage holins and their membrane-disrupting activity Anti-staphylococcal lytic enzymes Membrane-targeted enzybiotics Design of phage cocktails for therapy from a host-range point of view Novel methods to identify new enzybiotics Genetically modified phages that deliver suicidal genes to target bacteria The authors, all active enzybiotics researchers, offer a variety of perspectives, the benefit of their own hands-on investigations, as well as a thorough review and analysis of the current literature. As more and more bacteria become resistant to antibiotics, the development of new disease-fighting agents has become essential. This book demonstrates the full potential of the emerging field of enzybiotics to control infectious diseases. Moreover, it will serve as a springboard for new research and the development of new therapeutics.