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 Enzyme Inhibitors in Pharmacotherapy written by Dr Bukata B. Bukar and published by Exceller Books. This book was released on with total page 1139 pages. Available in PDF, EPUB and Kindle. Book excerpt: Enzyme Inhibitors in Pharmacotherapy explores the role of enzyme inhibitors in treating chronic diseases and infections. It covers enzyme biology, inhibition mechanisms, and pharmacological applications. Featuring detailed discussions and illustrations, the book offers valuable insights for students and practitioners. Written for a global audience, it combines theoretical knowledge with practical drug development advancements.

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 Enzyme Inhibitors as Drugs written by Merton Sandler and published by . This book was released on 1980 with total page 285 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Enzyme Inhibitors as Drugs written by Merton Sandler and published by . This book was released on 1980 with total page 304 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 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.

Download or read book Improved Non Steroid Anti Inflammatory Drugs COX 2 Enzyme Inhibitors written by Sir John R. Vane and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 249 pages. Available in PDF, EPUB and Kindle. Book excerpt: In 1971, Vane proposed that the mechanism of action of the aspirin-like drugs was through their inhibition of prostaglandin biosynthesis. Since then, there has been intense interest in the interaction between this diverse group of inhibitors and the enzyme known as cyclooxygenase (COX). It exists in two isoforms, COX-l and COX-2 (discovered some 5 years ago). Over the last two decades several new drugs have reached the market based on COX-l enzyme screens. Elucidation of the three-dimensional structure of COX-l has provided a new understanding for the actions of COX inhibitors. The constitutive isoform of COX, COX-l has clear physiological functions. Its activation leads, for instance, to the production of prostacyclin which when released by the endothelium is anti-thrombogenic and anti-atherosclerotic, and in the gastric mucosa is cyto protective. COX-l also generates prostaglandins in the kidney, where they help to maintain blood flow and promote natriuresis. The inducible isoform, COX-2, was discovered through its activity being increased in a number of cells by pro inflammatory stimuli. A year or so later, COX-2 was identified as a distinct isoform encoded by a different gene from COX-I. COX-2 is induced by inflammatory stimuli and by cytokines in migratory and other cells. Thus the anti-inflammatory actions of non-steroid anti-inflammatory drugs (NSAIDs) may be due to the inhibition of COX-2, whereas the unwanted side-effects such as irritation of the stomach lining and toxic effects on the kidney are due to inhibition of the constitutive enzyme, COX-I.

Download or read book Design of Enzyme Inhibitors as Drugs written by Merton Sandler and published by Oxford University Press, USA. This book was released on 1989 with total page 844 pages. Available in PDF, EPUB and Kindle. Book excerpt: A collection of essays examining the major target enzymes and their inhibitors. The underlying physical and chemical processes of enzyme inhibition, the principles of inhibitor design using computer-based techniques, and clinical applications are described.

Download or read book Advances in Studies on Enzyme Inhibitors As Drugs written by Satya Prakash Gupta and published by Nova Science Publishers. This book was released on 2017 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book which is edited by eminent scientist Satya P. Gupta, covers the most recent development on design and discovery of the most useful drugs acting against several life threatening diseases such as cancer, viral infections and many others in two volumes. All of these drugs are based on inhibitions of various enzymes. Most human diseases are found to be associated with the overexpression of the enzymes. The book presents the structural aspects of various enzymes, their active sites, and the structural requirements of chemicals for strong interactions with enzymes. Volume One contains twelve chapters related to enzyme inhibitors acting as anticancer and antiviral drugs (each written by highly acclaimed authors), and Volume Two contains ten chapters on enzyme inhibitors acting against miscellaneous diseases written by equally competent authors. The book may be an asset for drug industries, research organisations, and individual researchers.

Download or read book Atkinson s Principles of Clinical Pharmacology written by Shiew-Mei Huang and published by Academic Press. This book was released on 2021-10-16 with total page 764 pages. Available in PDF, EPUB and Kindle. Book excerpt: Atkinson’s Principles of Clinical Pharmacology, Fourth Edition is the essential reference on the pharmacologic principles underlying the individualization of patient therapy and contemporary drug development. This well-regarded survey continues to focus on the basics of clinical pharmacology for the development, evaluation and clinical use of pharmaceutical products while also addressing the most recent advances in the field. Written by leading experts in academia, industry, clinical and regulatory settings, the fourth edition has been thoroughly updated to provide readers with an ideal reference on the wide range of important topics impacting clinical pharmacology. Presents the essential knowledge for effective practice of clinical pharmacology Includes a new chapter and extended discussion on the role of personalized and precision medicine in clinical pharmacology Offers an extensive regulatory section that addresses US and international issues and guidelines Provides extended coverage of earlier chapters on transporters, pharmacogenetics and biomarkers, along with further discussion on "Phase 0" studies (microdosing) and PBPK

Download or read book Advances in Studies on Enzyme Inhibitors as Drugs Volume 2 Miscellaneous Drugs written by Satya P. Gupta and published by . This book was released on 2017 with total page 341 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Advances in Studies on Enzyme Inhibitors As Drugs written by Satya Prakash Gupta and published by Nova Science Publishers. This book was released on 2017 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book which is edited by eminent scientist Satya P. Gupta, covers the most recent development on design and discovery of the most useful drugs acting against several life threatening diseases such as cancer, viral infections and many others in two volumes. All of these drugs are based on inhibitions of various enzymes. Most human diseases are found to be associated with the overexpression of the enzymes. The book presents the structural aspects of various enzymes, their active sites, and the structural requirements of chemicals for strong interactions with enzymes. Volume One contains twelve chapters related to enzyme inhibitors acting as anticancer and antiviral drugs (each written by highly acclaimed authors), and Volume Two contains ten chapters on enzyme inhibitors acting against miscellaneous diseases written by equally competent authors. The book may be an asset for drug industries, research organisations, and individual researchers.

Download or read book Natural Products as Enzyme Inhibitors written by Vijay L. Maheshwari and published by Springer Nature. This book was released on 2022-05-03 with total page 287 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book provides an overview of the latest developments and future challenges in enzyme inhibitor research. It discusses the general enzyme inhibitory principles and mechanisms in enzyme activity regulation and application of enzyme inhibitors in different areas and sectors. The major areas of applications of enzyme inhibitors covered in this book are human health management, agriculture, food processing and research, which leads to drug discovery or enzyme activity mechanisms. The book also identifies the gaps in the existing knowledge and opens up new research ideas in this important area. Currently, most enzyme inhibitors are reported to inhibit various classes of enzymes. These enzyme inhibitors are the focus of the scientific community because they may answer an increasing array of questions in the research area of biological sciences, including biochemistry, medicine, physiology, pharmacy, agriculture, ecology etc. It also serves as a useful tool in the study of enzyme structures and reaction mechanisms and in the development of technologies in agriculture, food processing, and health management. Chapters in this book cover topics such as plant-derived inhibitors of serine proteases, pancreatic lipase (PL) inhibitors from indigenous medicinal plants, amylase inhibitors and their applications in agriculture and food processing industries and advances in silico techniques used in the study of enzyme inhibitors. The book will serve as a valuable resource for students and researchers in Life Sciences, agriculture, medicine, food processing, and allied industries.

Download or read book Description and Analysis of the VA National Formulary written by Institute of Medicine and published by National Academies Press. This book was released on 2000-10-03 with total page 280 pages. Available in PDF, EPUB and Kindle. Book excerpt: The VA National Formulary generated controversy, which motivated congressional scrutiny and a directive to the VA to commission this report reviewing the experience with the National Formulary and formulary system. This Institute of Medicine committee was pleased to assist the Congress with this review, in part because the committee saw in the VHA example an opportunity to understand and anticipate problems that all publicly funded programs are likely to encounter in this new age of pharmaceuticals. The Congress asked the committee to review the restrictiveness of the National Formulary, its impact on the costs and quality of care in the VHA, and how it compared to formularies and drug management practices in the private sector and in other public programs, especially Medicaid. Detailed in the pages that follow, the committee's findings and conclusions on these questions are, the committee believes, highly instructive, though not always in the ways that we anticipated.

Download or read book Biopharmaceutics and Pharmacokinetics Considerations written by and published by Academic Press. This book was released on 2021-07-07 with total page 754 pages. Available in PDF, EPUB and Kindle. Book excerpt: Biopharmaceutics and Pharmacokinetics Considerations examines the history of biopharmaceutics and pharmacokinetics. The book provides a biopharmaceutics and pharmacokinetics approach to addressing issues in formulation development and ethical considerations in handling animals. Written by experts in the field, this volume within the Advances in Pharmaceutical Product Development and Research series deepens understanding of biopharmaceutics and pharmacokinetics within drug discovery and drug development. Each chapter delves into a particular aspect of this fundamental field to cover the principles, methodologies and technologies employed by pharmaceutical scientists, researchers and pharmaceutical industries to study the chemical and physical properties of drugs and the biological effects they produce. Examines the most recent developments in biopharmaceutics and pharmacokinetics for pharmaceutical sciences Covers the principles, methodologies and technologies of biopharmaceutics and pharmacokinetics Focuses on the pharmaceutical sciences, but also encompasses aspects of toxicology, neuroscience, environmental sciences and nanotechnology