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In silico identification of noncompetitive inhibitors targeting an uncharacterized allosteric site of falcipain Computer Science, Medicine. Journal of Computer-Aided Molecular Design. Molecular Pharmacology. View 2 excerpts, cites methods. Kinetic Behavior of Enzyme Inhibitors. This chapter describes the modes of action of various reversible and irreversible enzyme inhibitors as well as the approaches for rationally designing high-affinity inhibitors, based on the inferred … Expand.
High performance enzyme kinetics of turnover, activation and inhibition for translational drug discovery. Expert opinion on drug discovery. View 2 excerpts, cites background. Journal of biomolecular screening.
The book discusses: The drug discovery process, including drug discovery strategy, medicinal chemistry, analytical chemistry, drug metabolism, pharmacokinetics, and safety biomarker assessment The manipulations of drug metabolizing enzymes Sets the stage for advances in drug discovery using the latest enzyme technology Reviewing new and emerging applications of enzyme technology in drug discovery, this book highlights some of the most promising areas of pharmaceutical and How are inhibitors properly evaluated for potency, selectivity, and mode of action'?
The text begins with a chapter that describes the advantages of enzymes as targets for drug discovery and some of the unique opportunities for drug Alpha-glucosidase Inhibitors: Clinically Promising Candidates for Anti-diabetic Drug Discovery presents information that researchers can use to address a whole host of promising leads for the development of novel, oral, anti-diabetic drugs This book provides a comprehensive and up-to-date coverage of the relationship between drug metabolism enzymes and transporters on drug toxicity, along with methods to investigate their role on adverse drug reactions.
This reference book contains a comprehensive selection of the most frequently used assays for reliably detecting pharmacological effects of potential drugs, including tests for cardiovascular, analgesic, psychotropic, metabolic, endocrine, It covers enzyme assay technology, utilization of enzymology for prodrug design, and the application of enzymes as therapeutic agents.
Expert reviews highlight how our latest understanding of enzymology is used to develop new practical applications in drug discovery and design. Filled with case studies, Enzyme Technologies: Pluripotent Players in Discovering Therapeutic Agents enables readers to better understand the diverse functions of enzymes and master specific applications in drug discovery research. In addition to small molecule drug discovery, the book explores new developments in enzymes as therapeutic agents for genetic disorders.
Section A, Enzymes — Essential Workhorses in Pharmaceutical Research, offers support in selecting the best enzyme targets for drug discovery, designing enzyme inhibitors for therapeutic agents, and evaluating selective enzyme inhibitors.
Section B, Enzymes — Indispensable Tools for Improving Druggability, sets forth the principles alongside real-world examples of exploiting specific properties of enzymes to design successful prodrugs. Section C, Enzymes — Powerful Weapons for Correcting Nature's Errors, provides new insights on applying enzymes as therapeutic agents or diagnostic tools to treat genetic disorders.
Chapters are contributed by leading experts from around the world. Their contributions are based on a thorough review of the current literature as well as their own research.
Reviewing our latest understanding of the nature of enzymes and their role in drug discovery, this book is recommended for researchers in pharmaceuticals and biotechnology as well as for researchers in enzymology, biochemistry, molecular biology, and medicinal chemistry.
Alpha-glucosidase Inhibitors: Clinically Promising Candidates for Anti-diabetic Drug Discovery presents information that researchers can use to address a whole host of promising leads for the development of novel, oral, anti-diabetic drugs with improved efficacy and fewer side effects. This book provides a comprehensive and up-to-date coverage of the relationship between drug metabolism enzymes and transporters on drug toxicity, along with methods to investigate their role on adverse drug reactions.
Unites both the metabolism and transporter components of drug toxicity — two aspects not normally connected and the latter often neglected Familiarizes readers with the mechanism and species differences in drug metabolizing enzymes and transporters Discusses promising approaches to accurately predict human drug toxicity via the incorporation of human drug metabolism in toxicity evaluation.
This reference book contains a comprehensive selection of the most frequently used assays for reliably detecting pharmacological effects of potential drugs, including tests for cardiovascular, analgesic, psychotropic, metabolic, endocrine, respiratory, renal, and immunomodulatory activities. Each of the over assays comprises a detailed protocol with the purpose and rationale of the method, a description of the experimental procedure, a critical assessment of the results and their pharmacological and clinical relevance, and pertinent references.
Identification of specific tests is facilitated by the enclosed CD-ROM which allows for a quick and full text research.
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