Evaluation of Enzyme Inhibitors in Drug Discovery

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Publisher : John Wiley & Sons
ISBN 13 : 0471723266
Total Pages : 295 pages
Book Rating : 4.4/5 (717 download)

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Book Synopsis Evaluation of Enzyme Inhibitors in Drug Discovery by : Robert A. Copeland

Download or read book Evaluation of Enzyme Inhibitors in Drug Discovery written by Robert A. Copeland and published by John Wiley & Sons. This book was released on 2005-04-01 with total page 295 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.

Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters

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Publisher : Elsevier Science
ISBN 13 : 0128200189
Total Pages : 708 pages
Book Rating : 4.1/5 (282 download)

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Book Synopsis Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters by : Shuguang Ma

Download or read book Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters written by Shuguang Ma and published by Elsevier Science. This book was released on 2020-07-24 with total page 708 pages. Available in PDF, EPUB and Kindle. Book excerpt: Identification and Quantification of Drugs, Metabolites, Drug Metabolizing Enzymes, and Transporters, Second Edition, is completely updated to provide an overview of the last decade's numerous advances in analytical technologies for detection and quantification of drugs, metabolites, and biomarkers. This new edition goes beyond LC-MS and features all-new chapters on how to evaluate drug absorption, distribution, metabolism, and excretion, potential for hepatic and renal toxicity, immunogenicity of biotherapeutics and translational tools for predicting human dosage, safety and efficacy of small molecules and biologics. This book will be an important handbook and desk reference for pharmacologists, toxicologists, clinical scientists, and students interested in the fields of pharmacology, biochemistry, and drug metabolism. Four sections in the book with 24 chapters give readers an overview of state-of-the-art techniques for identifying and quantifying drugs, metabolites and biomarkers, including a chapter on new approaches for quantification of enzymes and transporters in different tissues Focuses on the role of drug metabolism enzymes, transporters in disposition and drug-drug interactions, as well as strategies for evaluating drug metabolism and safety using advanced liver and kidney models. Discussions on immunogenicity risks of biologics and their evaluation methods have been included Includes several chapters on advanced translational sciences to predict human dosage, pharmacokinetics and efficacy for small molecules and biotherapeutics All chapters are written by experts with a wide range of practical experience from the industry and academia

Metabolism of Drugs and Other Xenobiotics

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Publisher : John Wiley & Sons
ISBN 13 : 352732903X
Total Pages : 755 pages
Book Rating : 4.5/5 (273 download)

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Book Synopsis Metabolism of Drugs and Other Xenobiotics by : Pavel Anzenbacher

Download or read book Metabolism of Drugs and Other Xenobiotics written by Pavel Anzenbacher and published by John Wiley & Sons. This book was released on 2012-05-29 with total page 755 pages. Available in PDF, EPUB and Kindle. Book excerpt: A practice-oriented desktop reference for medical professionals, toxicologists and pharmaceutical researchers, this handbook provides systematic coverage of the metabolic pathways of all major classes of xenobiotics in the human body. The first part comprehensively reviews the main enzyme systems involved in biotransformation and how they are orchestrated in the body, while parts two to four cover the three main classes of xenobiotics: drugs, natural products, environmental pollutants. The part on drugs includes more than 300 substances from five major therapeutic groups (central nervous system, cardiovascular system, cancer, infection, and pain) as well as most drugs of abuse including nicotine, alcohol and "designer" drugs. Selected, well-documented case studies from the most important xenobiotics classes illustrate general principles of metabolism, making this equally useful for teaching courses on pharmacology, drug metabolism or molecular toxicology. Of particular interest, and unique to this volume is the inclusion of a wide range of additional xenobiotic compounds, including food supplements, herbal preparations, and agrochemicals.

Evaluation of Enzyme Inhibitors in Drug Discovery

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Author :
Publisher : John Wiley & Sons
ISBN 13 : 111854028X
Total Pages : 588 pages
Book Rating : 4.1/5 (185 download)

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Book Synopsis Evaluation of Enzyme Inhibitors in Drug Discovery by : Robert A. Copeland

Download or read book Evaluation of Enzyme Inhibitors in Drug Discovery written by Robert A. Copeland and published by John Wiley & Sons. This book was released on 2013-01-31 with total page 588 pages. Available in PDF, EPUB and Kindle. Book excerpt: Offers essential guidance for discovering and optimizing novel drug therapies Using detailed examples, Evaluation of Enzyme Inhibitors in Drug Discovery equips researchers with the tools needed to apply the science of enzymology and biochemistry to the discovery, optimization, and preclinical development of drugs that work by inhibiting specific enzyme targets. Readers will applaud this book for its clear and practical presentations, including its expert advice on best practices to follow and pitfalls to avoid. This Second Edition brings the book thoroughly up to date with the latest research findings and practices. Updates explore additional forms of enzyme inhibition and special treatments for enzymes that act on macromolecular substrates. Readers will also find new discussions detailing the development and application of the concept of drug-target residence time. Evaluation of Enzyme Inhibitors in Drug Discovery begins by explaining why enzymes are such important drug targets and then examines enzyme reaction mechanisms. The book covers: Reversible modes of inhibitor interactions with enzymes Assay considerations for compound library screening Lead optimization and structure-activity relationships for reversible inhibitors Slow binding and tight binding inhibitors Drug-target residence time Irreversible enzyme inactivators The book ends with a new chapter exploring the application of quantitative biochemical principles to the pharmacologic evaluation of drug candidates during lead optimization and preclinical development. The Second Edition of Evaluation of Enzyme Inhibitors in Drug Discovery continues to offer a treatment of enzymology applied to drug discovery that is quantitative and mathematically rigorous. At the same time, the clear and simple presentations demystify the complex science of enzymology, making the book accessible to many fields— from pharmacology to medicinal chemistry to biophysics to clinical medicine.

Enzymes and Their Inhibitors

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Author :
Publisher : CRC Press
ISBN 13 : 0203414586
Total Pages : 325 pages
Book Rating : 4.2/5 (34 download)

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Book Synopsis Enzymes and Their Inhibitors by : H. John Smith

Download or read book Enzymes and Their Inhibitors written by H. John Smith and published by CRC Press. This book was released on 2004-11-29 with total page 325 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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

Enzyme Kinetics in Drug Metabolism

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Publisher : Humana
ISBN 13 : 9781627037570
Total Pages : 0 pages
Book Rating : 4.0/5 (375 download)

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Book Synopsis Enzyme Kinetics in Drug Metabolism by : Swati Nagar

Download or read book Enzyme Kinetics in Drug Metabolism written by Swati Nagar and published by Humana. This book was released on 2014-02-13 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug metabolism and transport are very important facets within the discipline of pharmaceutical sciences, with enzyme kinetic concepts utilized regularly in characterizing and modeling the disposition and elimination of drugs. Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications focuses on very practical aspects of applying kinetic principles to drug metabolizing enzymes and transporters. Divided into five convenient sections, topics include the fundamental principles of enzyme kinetics, the kinetics of oxidative and conjugative drug metabolizing enzymes and drug transporters, modeling approaches for both drug metabolizing enzymes and transporters including novel systems biology approaches, understanding of variability both experimental and interindividual (pharmacogenomic), and case studies that provide real life examples of applying these principles. Written in the successful Methods in Molecular Biology series format, chapters include introductions to their respective topics especially suitable for the novice, in some cases step-by-step, readily reproducible protocols, and insights to help with troubleshooting and avoiding known pitfalls with extensive cross referencing to assist in learning. Authoritative and easily accessible, Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications serves as a very practical teaching tool for novice, non-mathematically trained scientists interested in these fundamental concepts and as an aid for their supervisors in teaching these principles.

Drug Metabolism in Diseases

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Publisher : Academic Press
ISBN 13 : 0128029633
Total Pages : 296 pages
Book Rating : 4.1/5 (28 download)

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Book Synopsis Drug Metabolism in Diseases by : Wen Xie

Download or read book Drug Metabolism in Diseases written by Wen Xie and published by Academic Press. This book was released on 2016-09-12 with total page 296 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug Metabolism in Diseases is a comprehensive reference devoted to the current state of research on the impact of various disease states on drug metabolism. The book contains valuable insights into mechanistic effects and examples of how to accurately predict drug metabolism during these different pathophysiological states. Each chapter clearly presents the effects of changes in drug metabolism and drug transporters on pharmacokinetics and disposition. This is a unique and useful approach for all those involved in drug discovery and development, and for clinicians and researchers in drug metabolism, pharmacology, and clinical pharmacology. - Written and edited by leaders in drug metabolism from academia and industry - Covers important topics, such as pharmacogenomics, drug metabolism in transplant patients, xenobiotic receptors, drug metabolism in geriatric and pediatric populations, and more - Highlights topics of importance in drug discovery and development, and for safe and effective drug use in the clinic

Structural Biology in Drug Discovery

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Author :
Publisher : John Wiley & Sons
ISBN 13 : 1118900502
Total Pages : 1437 pages
Book Rating : 4.1/5 (189 download)

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Book Synopsis Structural Biology in Drug Discovery by : Jean-Paul Renaud

Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1437 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins

Drug Metabolism and Pharmacokinetics Quick Guide

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Publisher : Springer Science & Business Media
ISBN 13 : 1441956298
Total Pages : 222 pages
Book Rating : 4.4/5 (419 download)

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Book Synopsis Drug Metabolism and Pharmacokinetics Quick Guide by : Siamak Cyrus Khojasteh

Download or read book Drug Metabolism and Pharmacokinetics Quick Guide written by Siamak Cyrus Khojasteh and published by Springer Science & Business Media. This book was released on 2011-04-07 with total page 222 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug Metabolism and Pharmacokinetics Quick Guide covers a number of aspects of drug assessment at drug discovery and development stages, topics such as pharmacokinetics, absorption, metabolism, enzyme kinetics, drug transporters, drug interactions, drug-like properties, assays and in silico calculations. It covers key concepts, with useful tables on physiological parameters (eg. blood flow to organs in x-species, expression and localization of enzymes and transporters), chemical structure, nomenclature, and moieties leading to bioactivation (with examples). Overall it includes a number of key topics useful at the drug discovery stage, which would serve as a quick reference with several examples from the literature to illustrate the concept.

Pharmaceutical Enzymes

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Publisher : CRC Press
ISBN 13 : 9780824793753
Total Pages : 408 pages
Book Rating : 4.7/5 (937 download)

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Book Synopsis Pharmaceutical Enzymes by : Albert Lauwers

Download or read book Pharmaceutical Enzymes written by Albert Lauwers and published by CRC Press. This book was released on 1997-07-15 with total page 408 pages. Available in PDF, EPUB and Kindle. Book excerpt: This well-integrated, one-of-a-kind resource offers comprehensive, interdisciplinary analyses of the entire pharmaceutical enzyme field-from molecular biology to clinical pharmacology. Highlights practical, previously unpublished information, immediately useful in industry and academic institutions! Emphasizing pharmacology and clinical impact, Pharmaceutical Enzymes discusses robust methods of measurement and evaluation reviews current knowledge on the bioavailability of pharmaceutical enzymes presents different chemical approaches to tailoring enzymes for the improvement of therapeutic effectiveness provides a step-by-step approach to molecular modeling describes recently introduced pharmaceutical products, including glucocerebrosidase for the treatment of Gaucher's disease and deoxyribonuclease for cystic fibrosis furnishes unique laboratory guidelines for the testing and quality control of pharmaceutical enzymes and more! With over 1200 bibliographic citations, figures, and tables, Pharmaceutical Enzymes is an indispensable, day-to-day reference for pharmacologists, enzymologists, microbiologists, organic and medicinal chemists and biochemists, biophysicists, biotechnologists, molecular and membrane biologists, immunologists, physiologists, pharmaceutical development managers, regulatory affairs personnel, and graduate-level students in these disciplines.

Microsomes and Drug Oxidations

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Publisher : Elsevier
ISBN 13 : 1483159086
Total Pages : 805 pages
Book Rating : 4.4/5 (831 download)

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Book Synopsis Microsomes and Drug Oxidations by : Volker Ullrich

Download or read book Microsomes and Drug Oxidations written by Volker Ullrich and published by Elsevier. This book was released on 2013-10-22 with total page 805 pages. Available in PDF, EPUB and Kindle. Book excerpt: Microsomes and Drug Oxidations is a record of the proceedings of the Third International Symposium on Microsomes and Drug Oxidations, held in Berlin, Germany in July 1976. The compendium provides an overview of knowledge on the oxidative metabolism of drugs, carcinogens, and various other environmental chemicals. Topics discussed include lipid structure of liver microsomal membranes; interactions between cytochrome p-450 and nadphcytochrome p-450 reductase in the microsomal membrane; impact of drug monoxygenases in clinical pharmacology; and the manner in which oxygen participates in mixed-function oxidation reactions. Pharmacologists, toxicologists, biochemists, and researchers in the pharmaceutical industry will find the book highly insightful.

Hydrolysis in Drug and Prodrug Metabolism

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Publisher : John Wiley & Sons
ISBN 13 : 9783906390253
Total Pages : 808 pages
Book Rating : 4.3/5 (92 download)

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Book Synopsis Hydrolysis in Drug and Prodrug Metabolism by : Bernard Testa

Download or read book Hydrolysis in Drug and Prodrug Metabolism written by Bernard Testa and published by John Wiley & Sons. This book was released on 2003-08 with total page 808 pages. Available in PDF, EPUB and Kindle. Book excerpt: Many drugs and other xenobiotics (e.g., preservatives, insecticides, and plastifiers) contain hydrolyzable moieties such as ester or amide groups. In biological media, such foreign compounds are, therefore, important substrates for hydrolytic reactions catalyzed by hydrolases or proceeding non-enzymatically. Despite their significance, until now, no book has been dedicated to hydrolysis and hydrolases in the metabolism of drugs and other xenobiotics. This work fills a gap in the literature and reviews metabolic reactions of hydrolysis and hydarion from the point of views of enzymes, substrates, and reactions.

Drug Design of Zinc-Enzyme Inhibitors

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Publisher : John Wiley & Sons
ISBN 13 : 9780470508152
Total Pages : 1040 pages
Book Rating : 4.5/5 (81 download)

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Book Synopsis Drug Design of Zinc-Enzyme Inhibitors by : Claudiu T. Supuran

Download or read book Drug Design of Zinc-Enzyme Inhibitors written by Claudiu T. Supuran and published by John Wiley & Sons. This book was released on 2009-10-22 with total page 1040 pages. Available in PDF, EPUB and Kindle. Book excerpt: Brings together functional and structural informationrelevant to the design of drugs targeting zinc enzymes The second most abundant transition element in living organisms, zinc spans all areas of metabolism, with zinc-containing proteins offering both established and potential drug targets. Drug Design of Zinc-Enzyme Inhibitors brings together functional and structural information relevant to these zinc-containing targets. With up-to-date overviews of the latest developments field, this unique and comprehensive text enables readers to understand zinc enzymes and evaluate them in a drug design context. With contributions from the leaders of today's research, Drug Design of Zinc-Enzyme Inhibitors covers such key topics as: Major drug targets like carbonic anhydrases, matrix metalloproteinases, bacterial proteases, angiotensin-converting enzyme, histone deacetylase, and APOBEC3G Roles of recently discovered zinc-containing isozymes in cancer, obesity, epilepsy, pain management, malaria, and other conditions Cross reactivity of zinc-enzyme inhibitors and activators The extensive use of X-ray crystallography and QSAR studies for understanding zinc-containing proteins Clinical applications An essential resource for the discovery and development of new drug molecules, Drug Design of Zinc-Enzyme Inhibitors gives researchers, professionals, students, and academics the foundation to understand and work with zinc enzyme inhibitors and activators.

Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays

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Publisher : Springer
ISBN 13 : 9783642252396
Total Pages : 0 pages
Book Rating : 4.2/5 (523 download)

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Book Synopsis Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays by : H. Gerhard Vogel

Download or read book Drug Discovery and Evaluation: Safety and Pharmacokinetic Assays written by H. Gerhard Vogel and published by Springer. This book was released on 2013-02-27 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: -A landmark in the continuously changing world of drugs -Essential reading for scientists and managers in the pharmaceutical industry involved in drug finding, drug development and decision making in the development process -Of use for government institutions and committees working on official guidelines for drug evaluation worldwide

Drug-Induced Liver Injury

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Publisher : Academic Press
ISBN 13 : 0128173173
Total Pages : 290 pages
Book Rating : 4.1/5 (281 download)

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Book Synopsis Drug-Induced Liver Injury by :

Download or read book Drug-Induced Liver Injury written by and published by Academic Press. This book was released on 2019-07-13 with total page 290 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug-Induced Liver Injury, Volume 85, the newest volume in the Advances in Pharmacology series, presents a variety of chapters from the best authors in the field. Chapters in this new release include Cell death mechanisms in DILI, Mitochondria in DILI, Primary hepatocytes and their cultures for the testing of drug-induced liver injury, MetaHeps an alternate approach to identify IDILI, Autophagy and DILI, Biomarkers and DILI, Regeneration and DILI, Drug-induced liver injury in obesity and nonalcoholic fatty liver disease, Mechanisms of Idiosyncratic Drug-Induced Liver Injury, the Evaluation and Treatment of Acetaminophen Toxicity, and much more. - Includes the authority and expertise of leading contributors in pharmacology - Presents the latest release in the Advances in Pharmacology series

Holland-Frei Cancer Medicine

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Publisher : John Wiley & Sons
ISBN 13 : 111900084X
Total Pages : 2004 pages
Book Rating : 4.1/5 (19 download)

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Book Synopsis Holland-Frei Cancer Medicine by : Robert C. Bast, Jr.

Download or read book Holland-Frei Cancer Medicine written by Robert C. Bast, Jr. and published by John Wiley & Sons. This book was released on 2017-03-10 with total page 2004 pages. Available in PDF, EPUB and Kindle. Book excerpt: Holland-Frei Cancer Medicine, Ninth Edition, offers a balanced view of the most current knowledge of cancer science and clinical oncology practice. This all-new edition is the consummate reference source for medical oncologists, radiation oncologists, internists, surgical oncologists, and others who treat cancer patients. A translational perspective throughout, integrating cancer biology with cancer management providing an in depth understanding of the disease An emphasis on multidisciplinary, research-driven patient care to improve outcomes and optimal use of all appropriate therapies Cutting-edge coverage of personalized cancer care, including molecular diagnostics and therapeutics Concise, readable, clinically relevant text with algorithms, guidelines and insight into the use of both conventional and novel drugs Includes free access to the Wiley Digital Edition providing search across the book, the full reference list with web links, illustrations and photographs, and post-publication updates

Enzyme Inhibitors and Activators

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Author :
Publisher : BoD – Books on Demand
ISBN 13 : 9535130579
Total Pages : 270 pages
Book Rating : 4.5/5 (351 download)

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Book Synopsis Enzyme Inhibitors and Activators by : Murat Şentürk

Download or read book Enzyme Inhibitors and Activators written by Murat Şentürk and published by BoD – Books on Demand. This book was released on 2017-03-29 with total page 270 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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.