kinetics of enzyme action essential principles for drug hunters

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Kinetics Of Enzyme Action

Author : Ross L. Stein
ISBN : 1118084403
Genre : Science
File Size : 66. 85 MB
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Few scientists have the knowledge to perform the studies that are necessary to discover and characterize enzyme inhibitors, despite the vested interest the pharmaceutical industry has in this field. Beginning with the most basic principles pertaining to simple, one-substrate enzyme reactions and their inhibitors, and progressing to a thorough treatment of two-substrate enzymes, Kinetics of Enzyme Action: Essential Principles for Drug Hunters provides biochemists, medicinal chemists, and pharmaceutical scientists with numerous case study examples to outline the tools and techniques necessary to perform, understand, and interpret detailed kinetic studies for drug discovery.

The Organic Chemistry Of Drug Design And Drug Action

Author : Richard B. Silverman
ISBN : 9780123820310
Genre : Medical
File Size : 74. 78 MB
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The Organic Chemistry of Drug Design and Drug Action, Third Edition, represents a unique approach to medicinal chemistry based on physical organic chemical principles and reaction mechanisms that rationalize drug action, which allows reader to extrapolate those core principles and mechanisms to many related classes of drug molecules. This new edition includes updates to all chapters, including new examples and references. It reflects significant changes in the process of drug design over the last decade and preserves the successful approach of the previous editions while including significant changes in format and coverage. This text is designed for undergraduate and graduate students in chemistry studying medicinal chemistry or pharmaceutical chemistry; research chemists and biochemists working in pharmaceutical and biotechnology industries. Updates to all chapters, including new examples and references Chapter 1 (Introduction): Completely rewritten and expanded as an overview of topics discussed in detail throughout the book Chapter 2 (Lead Discovery and Lead Modification): Sections on sources of compounds for screening including library collections, virtual screening, and computational methods, as well as hit-to-lead and scaffold hopping; expanded sections on sources of lead compounds, fragment-based lead discovery, and molecular graphics; and deemphasized solid-phase synthesis and combinatorial chemistry Chapter 3 (Receptors): Drug-receptor interactions, cation-π and halogen bonding; atropisomers; case history of the insomnia drug suvorexant Chapter 4 (Enzymes): Expanded sections on enzyme catalysis in drug discovery and enzyme synthesis Chapter 5 (Enzyme Inhibition and Inactivation): New case histories: for competitive inhibition, the epidermal growth factor receptor tyrosine kinase inhibitor, erlotinib and Abelson kinase inhibitor, imatinib for transition state analogue inhibition, the purine nucleoside phosphorylase inhibitors, forodesine and DADMe-ImmH, as well as the mechanism of the multisubstrate analog inhibitor isoniazid for slow, tight-binding inhibition, the dipeptidyl peptidase-4 inhibitor, saxagliptin Chapter 7 (Drug Resistance and Drug Synergism): This new chapter includes topics taken from two chapters in the previous edition, with many new examples Chapter 8 (Drug Metabolism): Discussions of toxicophores and reactive metabolites Chapter 9 (Prodrugs and Drug Delivery Systems): Discussion of antibody–drug conjugates

Simulating Enzyme Reactivity

Author : Inaki Tunon
ISBN : 9781782624295
Genre : Science
File Size : 61. 22 MB
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Exploring the theories, methodologies and applications in simulations of enzymatic reactions, this book is a great resource for postgraduate students and researchers.

A Practical Guide To Continuous Delivery

Author : Eberhard Wolff
ISBN : 9780134691541
Genre : Computers
File Size : 77. 70 MB
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Using Continuous Delivery, you can bring software into production more rapidly, with greater reliability. A Practical Guide to Continuous Delivery is a 100% practical guide to building Continuous Delivery pipelines that automate rollouts, improve reproducibility, and dramatically reduce risk. Eberhard Wolff introduces a proven Continuous Delivery technology stack, including Docker, Chef, Vagrant, Jenkins, Graphite, the ELK stack, JBehave, and Gatling. He guides you through applying these technologies throughout build, continuous integration, load testing, acceptance testing, and monitoring. Wolff’s start-to-finish example projects offer the basis for your own experimentation, pilot programs, and full-fledged deployments. A Practical Guide to Continuous Delivery is for everyone who wants to introduce Continuous Delivery, with or without DevOps. For managers, it introduces core processes, requirements, benefits, and technical consequences. Developers, administrators, and architects will gain essential skills for implementing and managing pipelines, and for integrating Continuous Delivery smoothly into software architectures and IT organizations. Understand the problems that Continuous Delivery solves, and how it solves them Establish an infrastructure for maximum software automation Leverage virtualization and Platform as a Service (PAAS) cloud solutions Implement build automation and continuous integration with Gradle, Maven, and Jenkins Perform static code reviews with SonarQube and repositories to store build artifacts Establish automated GUI and textual acceptance testing with behavior-driven design Ensure appropriate performance via capacity testing Check new features and problems with exploratory testing Minimize risk throughout automated production software rollouts Gather and analyze metrics and logs with Elasticsearch, Logstash, Kibana (ELK), and Graphite Manage the introduction of Continuous Delivery into your enterprise Architect software to facilitate Continuous Delivery of new capabilities

Evaluation Of Enzyme Inhibitors In Drug Discovery

Author : Robert A. Copeland
ISBN : 9781118540282
Genre : Science
File Size : 81. 16 MB
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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.

Enzyme Kinetics Catalysis And Control

Author : Daniel L. Purich
ISBN : 9780123809254
Genre : Science
File Size : 45. 52 MB
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Far more than a comprehensive treatise on initial-rate and fast-reaction kinetics, this one-of-a-kind desk reference places enzyme science in the fuller context of the organic, inorganic, and physical chemical processes occurring within enzyme active sites. Drawing on 2600 references, Enzyme Kinetics: Catalysis & Control develops all the kinetic tools needed to define enzyme catalysis, spanning the entire spectrum (from the basics of chemical kinetics and practical advice on rate measurement, to the very latest work on single-molecule kinetics and mechanoenzyme force generation), while also focusing on the persuasive power of kinetic isotope effects, the design of high-potency drugs, and the behavior of regulatory enzymes. Historical analysis of kinetic principles including advanced enzyme science Provides both theoretical and practical measurements tools Coverage of single molecular kinetics Examination of force generation mechanisms Discussion of organic and inorganic enzyme reactions

Introduction To Enzyme And Coenzyme Chemistry

Author : T. D. H. Bugg
ISBN : 9781118348994
Genre : Science
File Size : 37. 92 MB
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Enzymes are giant macromolecules which catalyse biochemical reactions. They are remarkable in many ways. Their three-dimensional structures are highly complex, yet they are formed by spontaneous folding of a linear polypeptide chain. Their catalytic properties are far more impressive than synthetic catalysts which operate under more extreme conditions. Each enzyme catalyses a single chemical reaction on a particular chemical substrate with very high enantioselectivity and enantiospecificity at rates which approach “catalytic perfection”. Living cells are capable of carrying out a huge repertoire of enzyme-catalysed chemical reactions, some of which have little or no precedent in organic chemistry. The popular textbook Introduction to Enzyme and Coenzyme Chemistry has been thoroughly updated to include information on the most recent advances in our understanding of enzyme action, with additional recent examples from the literature used to illustrate key points. A major new feature is the inclusion of two-colour figures, and the addition of over 40 new figures of the active sites of enzymes discussed in the text, in order to illustrate the interplay between enzyme structure and function. This new edition provides a concise but comprehensive account from the perspective of organic chemistry, what enzymes are, how they work, and how they catalyse many of the major classes of enzymatic reactions, and will continue to prove invaluable to both undergraduate and postgraduate students of organic, bio-organic and medicinal chemistry, chemical biology, biochemistry and biotechnology.

Fragment Based Drug Discovery

Author : Daniel A. Erlanson
ISBN : 9783527337750
Genre : Medical
File Size : 74. 89 MB
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From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets.

Aggregation Of Therapeutic Proteins

Author : Wei Wang
ISBN : 1118043588
Genre : Medical
File Size : 65. 20 MB
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This book gives pharmaceutical scientists an up-to-date resource on protein aggregation and its consequences, and available methods to control or slow down the aggregation process. While significant progress has been made in the past decade, the current understanding of protein aggregation and its consequences is still immature. Prevention or even moderate inhibition of protein aggregation has been mostly experimental. The knowledge in this book can greatly help pharmaceutical scientists in the development of therapeutic proteins, and also instigate further scientific investigations in this area. This book fills such a need by providing an overview on the causes, consequences, characterization, and control of the aggregation of therapeutic proteins.

Applications Of Microdialysis In Pharmaceutical Science

Author : Tung-Hu Tsai
ISBN : 1118011287
Genre : Medical
File Size : 38. 88 MB
Format : PDF
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Discover new and emerging applications for microdialysis in drug evaluation Microdialysis is a highly valuable sampling tool that can be used in vivo to measure free, unbound analyte concentrations located in interstitial and extracellular spaces. This book explores the full range of clinical applications for microdialysis, focusing on its use in different organ and tissue systems for pharmacokinetic and pharmacodynamic studies. Readers gain a full understanding of the underlying science of microdialysis, current techniques and practices, as well as its many applications in pharmaceutical research. Applications of Microdialysis in Pharmaceutical Science starts with an introduction to basic principles and then covers analytical considerations, pharmacodynamic and pharmacokinetic studies, clinical aspects, and special applications. Topics include: Role of microdialysis in drug development, including crucial sampling considerations and applications for nervous system diseases Continuous measurement of glucose concentrations in diabetics Applications for clinical evaluation and basic research on organ systems, including monitoring exogenous and endogenous compounds in the lungs Pharmacokinetic and pharmacodynamic evaluation of anticancer drugs Comparison of microdialysis with imaging approaches to evaluate in vivo drug distribution Special applications of microdialysis in studies of cell culture assays, drug-drug interactions, and environmental monitoring Throughout the book, readers will find simple models that clarify complex concepts and easy-to-follow examples that guide them through key applications in pharmaceutical research. In short, this book enables pharmaceutical researchers to take full advantage of microdialysis techniques for the preclinical and clinical evaluation of drugs and much more.

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