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Author | : Michael Palfreyman |
Publisher | : Elsevier |
Total Pages | : 282 |
Release | : 2012-12-02 |
Genre | : Medical |
ISBN | : 0323140483 |
Download Enzymes as Targets for Drug Design Book in PDF, ePub and Kindle
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.
Author | : Robert A. Copeland |
Publisher | : John Wiley & Sons |
Total Pages | : 295 |
Release | : 2005-04-01 |
Genre | : Science |
ISBN | : 0471723266 |
Download Evaluation of Enzyme Inhibitors in Drug Discovery Book in PDF, ePub and Kindle
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.
Author | : John S. Holcenberg |
Publisher | : John Wiley & Sons |
Total Pages | : 546 |
Release | : 1981 |
Genre | : Enzymes |
ISBN | : |
Download Enzymes as Drugs Book in PDF, ePub and Kindle
Author | : Nikolaos Labrou |
Publisher | : Springer Nature |
Total Pages | : 388 |
Release | : 2019-09-03 |
Genre | : Science |
ISBN | : 981137709X |
Download Therapeutic Enzymes: Function and Clinical Implications Book in PDF, ePub and Kindle
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.
Author | : Donald J. Abraham |
Publisher | : |
Total Pages | : |
Release | : 2021 |
Genre | : Drug development |
ISBN | : 9781119821519 |
Download Burger's Medicinal Chemistry, Drug Discovery and Development Book in PDF, ePub and Kindle
"Burger's is a flagship reference source for medicinal chemists and pharmaceutical professionals. This updated and expanded 8th edition has been thoroughly revised and improved to incorporate the concepts of drug hunting along with its existing coverage of the entire process of drug discovery and development. Bringing in a new and expert editorial board, this new edition updates existing chapters and adds 35 new ones, with topics including: opioid addiction treatments, antibody and gene therapy for cancer, blood-brain barrier, HIV treatments, and industrial-academic collaboration structures"--
Author | : J. L. Mongar |
Publisher | : John Wiley & Sons |
Total Pages | : 581 |
Release | : 2009-09-16 |
Genre | : Medical |
ISBN | : 0470716762 |
Download Enzymes and Drug Action Book in PDF, ePub and Kindle
The Novartis Foundation Series is a popular collection of the proceedings from Novartis Foundation Symposia, in which groups of leading scientists from a range of topics across biology, chemistry and medicine assembled to present papers and discuss results. The Novartis Foundation, originally known as the Ciba Foundation, is well known to scientists and clinicians around the world.
Author | : H. John Smith |
Publisher | : CRC Press |
Total Pages | : 325 |
Release | : 2004-11-29 |
Genre | : Medical |
ISBN | : 0203414586 |
Download Enzymes and Their Inhibitors Book in PDF, ePub and Kindle
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
Author | : Serge Kirkiacharian |
Publisher | : John Wiley & Sons |
Total Pages | : 228 |
Release | : 2024-07-23 |
Genre | : Science |
ISBN | : 1786309394 |
Download Enzymes and Drugs Book in PDF, ePub and Kindle
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.
Author | : Bernard B. Brodie |
Publisher | : Elsevier |
Total Pages | : 519 |
Release | : 2013-10-22 |
Genre | : Medical |
ISBN | : 1483223515 |
Download Drugs and Enzymes Book in PDF, ePub and Kindle
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.
Author | : Chuang Lu |
Publisher | : John Wiley & Sons |
Total Pages | : 878 |
Release | : 2010-01-26 |
Genre | : Medical |
ISBN | : 0470538945 |
Download Enzyme Inhibition in Drug Discovery and Development Book in PDF, ePub and Kindle
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.