Download or read book Enzymes as Targets for Drug Design written by Michael Palfreyman and published by Elsevier. This book was released on 2012-12-02 with total page 282 pages. Available in PDF, EPUB and Kindle. Book excerpt: Enzymes as Targets for Drug Design is a collection of scientific discussions related to enzyme inhibitors that show the many facets of the drug discovery process from the basic sciences through clinical applications. Topics include the biogenesis of phosphatidylinositol glycosyl membrane proteins, structure and catalytic function of ADP-ribose polymerase (ADPRT), and modulation of the dopaminergic system in cardiovascular therapeutics. The therapeutic utility of selected enzyme-activated irreversible inhibitors, the role of proteinases in the fibrosis of systemic sclerosis, and therapeutic opportunities in eicosanoid biosynthesis are also discussed. This book consists of 18 chapters and begins with examples of enzymes whose activities have recently been elucidated, or for which newer insights have been gleaned, but which do not yet have selective or potent inhibitors. The second part provides examples of enzymes where inhibitors have been identified but it is still not clear whether or not such an enzymatic blockade will be therapeutically beneficial. The final section describes clinical studies of newer, and not so new, enzyme inhibitors that are clearly of therapeutic importance. The therapeutic activity of monoamine oxidase inhibitors and the associated clinical issues are considered. This book is intended for clinicians as well as basic scientists in biochemistry, chemistry, pharmacology, and cell biology.
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.
Download or read book Enzymes as Drugs written by John S. Holcenberg and published by John Wiley & Sons. This book was released on 1981 with total page 546 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Therapeutic Enzymes Function and Clinical Implications written by Nikolaos Labrou and published by Springer Nature. This book was released on 2019-09-03 with total page 388 pages. Available in PDF, EPUB and Kindle. Book excerpt: Therapeutic enzymes exhibit fascinating features and opportunities, and represent a significant and promising subcategory of modern biopharmaceuticals for the treatment of several severe diseases. Research and drug developments efforts and the advancements in biotechnology over the past twenty years have greatly assisted the introduction of efficient and safe enzyme-based therapies for a range of both rare and common disorders. The introduction and regulatory approval of twenty different recombinant enzymes has enabled effective enzyme-replacement therapy. This volume aims to overview these therapeutic enzymes, focusing in particular on more recently approved enzymes produced by recombinant DNA technology. This volume is composed of four sections. Section 1 provides an overview of the production process and biochemical characterization of therapeutic enzymes, while Section 2 focuses upon the engineering strategies and delivery methods of therapeutic enzymes. Section 3 highlights the clinical applications of approved therapeutic enzymes, including aspects on their structure, indications and mechanisms of action. Together with information on these mechanisms, safety and immunogenicity issues and various adverse events of the recombinant enzymes used for therapy are discussed. Section 4, provides discussion on the prospective and future developments of new therapeutic enzymes. This book is aimed at academics, researchers and students undertaking advanced undergraduate/postgraduate programs in the biopharmaceutical/biotechnology area who wish to gain a comprehensive understanding of enzyme-based therapeutic molecules.
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.
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
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
Download or read book Enzymes and Drug Action written by J. L. Mongar and published by . This book was released on 1962 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Enzyme Inhibition in Drug Discovery and Development written by Chuang Lu and published by John Wiley & Sons. This book was released on 2010-01-26 with total page 878 pages. Available in PDF, EPUB and Kindle. Book excerpt: The science and applied approaches of enzyme inhibition in drug discovery and development Offering a unique approach that includes both the pharmacologic and pharmaco-kinetic aspects of enzyme inhibition, Enzyme Inhibition in Drug Discovery and Development examines the scientific concepts and experimental approaches related to enzyme inhibition as applied in drug discovery and drug development. With chapters written by over fifty leading experts in their fields, Enzyme Inhibition in Drug Discovery and Development fosters a cross-fertilization of pharmacology, drug metabolism, pharmacokinetics, and toxicology by understanding the "good" inhibitions—desirable pharmacological effects—and "bad" inhibitions—drug–drug interactions and toxicity. 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 and transporters as well as the negative consequences, such as drug–drug interactions The inhibition of several major drug target pathways, such as the GPCR pathway, the NFkB pathway, and the ion channel pathway Through this focused, single-source reference on the fundamentals of drug discovery and development, researchers in drug metabolism and pharmacokinetics (DMPK) will learn and appreciate target biology in drug discovery; discovery biologists and medicinal chemists will also broaden their understanding of DMPK.
Download or read book Enzymes and Drugs written by Serge Kirkiacharian and published by John Wiley & Sons. This book was released on 2024-07-23 with total page 228 pages. Available in PDF, EPUB and Kindle. Book excerpt: Enzyme dysfunction, an essential catalyst for the smooth running of biochemical reactions and the maintenance of vital processes, is at the root of many pathologies that have paved the way for the development of numerous drugs. Aimed at pharmacists, biologists, biochemists, doctors, veterinarians, medicinal chemists and students from a wide range of disciplines, Enzymes and Drugs brings together, for the first time, extensive documentation highlighting the relationships between a large number of drugs and enzymes. The book also highlights new prospects for therapeutic discoveries offered by enzyme targeting. Numerous applications have been developed thanks to strategies for studying enzyme inhibition or activation, as well as the development of allosteric effectors, presented with their advantages and disadvantages. Various rare diseases, known as "orphan" diseases, have resulted from enzyme deficiency or absence. For their treatment, the introduction of substitute enzymes has led to major therapeutic advances.
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.
Download or read book Drugs and Enzymes written by Bernard B. Brodie and published by Elsevier. This book was released on 2013-10-22 with total page 519 pages. Available in PDF, EPUB and Kindle. Book excerpt: Second International Pharmacological Meeting, Volume 4: Drugs and Enzymes is a collection of papers presented at the Second International Pharmacological Meeting on August 20-23, 1963. This volume is organized into two sections encompassing 41 chapters. The first section discusses the relationship between biochemical effects of drugs in vitro and their pharmacological effect in vivo. This section specifically examines the correlation between the action of substances on isolated smooth muscle and on the central nervous system, as well as the behavior of a centrally-acting drug and enzyme in the ion movement in the system. The second section surveys the biochemical mechanisms of drug toxicity. Considerable chapters in this section are devoted to the effect of drug toxicity, such as altered drug metabolism, enzyme induction, morphological changes, hepatic effects, and photosensitivity. This book will prove useful to pharmacologists, neurologists, biochemists, and researchers who are interested the fields of drugs and drug toxicity.
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 1367 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
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.
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.
Download or read book Enzyme and Transporter Based Drug Drug Interactions written by K. Sandy Pang and published by Springer Science & Business Media. This book was released on 2009-12-17 with total page 742 pages. Available in PDF, EPUB and Kindle. Book excerpt: Germination of the thought of "Enzymatic- and Transporter-Based Drug-Drug Interactions: Progress and Future Challenges" Proceedings came about as part of the annual meeting of The American Association of Pharmaceutical Scientists (AAPS) that was held in San Diego in November of 2007. The attendance of workshop by more than 250 pharmaceutical scientists reflected the increased interest in the area of drug-drug interactions (DDIs), the greater focus of PhRMA, academia, and regulatory agencies, and the rapid pace of growth in knowledge. One of the aims of the workshop was to address the progress made in quantitatively predicting enzyme- and transporter-based DDIs as well as highlighted areas where such predictions are poor or areas that remain challenging for the future. Because of the serious clinical implications, initiatives have arisen from the FDA (http://www.fda.gov/cber/gdlns/interactstud.htm) to highlight the importance of enzyme- and transporter-based DDIs. During the past ten to fifteen years, we have come to realize that transporters, in addition to enzymes, play a vital role in drug elimination. Such insight has been possible because of the continued growth in PK-ADME (pharmacokinetics-absorption-distribution-metabolism-excretion) knowledge, fueled by further advances in molecular biology, greater availability of human tissues, and the development of additional and sophisticated model systems and sensitive assay methods for studying drug metabolism and transport in vitro and in vivo. This has sparked an in-depth probing into mechanisms surrounding DDIs, resulting from ligand-induced changes in nuclear receptors, as well as alterations in transporter and enzyme expression and function. Despite such advances, the in vitro and in vivo study of drug interactions and the integration of various data sets remain challenging. Therefore, it has become apparent that a proceeding that serves to encapsulate current strategies, approaches, methods and applications is necessary. As Editors, we have assembled a number of opinion leaders and asked them to contribute chapters surrounding these issues. Many of these are the original Workshop speakers whereas others had been selected specially to contribute on topics related to basic and applied information that had not been covered in other reference texts on DDI. The resulting tome, entitled Enzyme- and Transporter-Based Drug Interactions: Progress and Future Challenges, comprises of four sections. Twenty-eight chapters covering various topics and perspectives related to the subject of metabolic and transporter-based drug-drug interactions are presented.
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
