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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.
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
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.
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.
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Plants produce a vast number of bioactive compounds with different chemical scaffolds, which modulate a diverse range of molecular targets and are used as drugs for treating numerous diseases. Most present-day medicines are derived either from plant compounds or their derivatives, and plant compounds continue to offer limitless reserves for the discovery of new medicines. While different classes of plant compounds, like phenolics, flavonoids, saponins and alkaloids, and their potential pharmacological applications are currently being explored, their curative mechanisms are yet to be understood in detail. This book is divided into 2 volumes and offers detailed information on plant-derived bioactive compounds, including recent research findings. Volume 1, Plant-derived Bioactives: Chemistry and Mode of Action, discusses the chemistry of highly valued plant bioactive compounds and their mode of actions at the molecular level. Volume 2, Plant-derived Bioactives: Production, Properties and Therapeutic Applications, explores the sources, biosynthesis, production, biological properties and therapeutic applications of plant bioactives. Given their scope, these books are valuable resources for members of the scientific community wishing to further explore various medicinal plants and the therapeutic applications of their bioactive compounds. They appeal to scholars, teachers and scientists involved in plant product research, and facilitate the development of innovative new drugs.
Established almost 30 years ago, Methods in Microbiology is the most prestigious series devoted to techniques and methodology in the field. Now totally revamped, revitalized, with a new format and expanded scope, Methods in Microbiology will continue to provide you with tried and tested, cutting-edge protocols to directly benefit your research. - Focuses on the methods most useful for the microbiologist interested in the way in which bacteria cause disease - Includes section devoted to 'Approaches to characterising pathogenic mechanisms' by Stanley Falkow - Covers safety aspects, detection, identification and speciation - Includes techniques for the study of host interactions and reactions in animals and plants - Describes biochemical and molecular genetic approaches - Essential methods for gene expression and analysis - Covers strategies and problems for disease control