Download or read book Drug Receptor Thermodynamics written by Robert B. Raffa and published by Wiley. This book was released on 2001-06-08 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug-Receptor Thermodynamics is the first book to provide in depth coverage of principles and applications of thermodynamic drug-receptor interactions. The book starts from familiar points, making thermodynamics accessible to anyone interested in how drugs work. The ideas presented cover general principles as well as laying the groundwork for new ways of examining drug action. * covers an area of increasing interest and relevance in the field of drug design and discovery * excellent explanation of why thermodynamics is at the heart of drug action * contributions from many of the worlds leading experts in the field Anyone interested in drug receptor interaction will find something of use in this book. It will be of particular relevance for pharmacologists, health science researchers and medicinal chemists.

Download or read book Thermodynamics and Kinetics of Drug Binding written by György Keserü and published by John Wiley & Sons. This book was released on 2015-03-09 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: This practical reference for medicinal and pharmaceutical chemists combines the theoretical background with modern methods as well as applications from recent lead finding and optimization projects. Divided into two parts on the thermodynamics and kinetics of drug-receptor interaction, the text provides the conceptual and methodological basis for characterizing binding mechanisms for drugs and other bioactive molecules. It covers all currently used methods, from experimental approaches, such as ITC or SPR, right up to the latest computational methods. Case studies of real-life lead or drug development projects are also included so readers can apply the methods learned to their own projects. Finally, the benefits of a thorough binding mode analysis for any drug development project are summarized in an outlook chapter written by the editors.

Download or read book Thermodynamics of Pharmaceutical Systems written by Kenneth A. Connors and published by John Wiley & Sons. This book was released on 2010-01-22 with total page 379 pages. Available in PDF, EPUB and Kindle. Book excerpt: Designed for pharmacy students Now updated for its Second Edition, Thermodynamics of Pharmaceutical Systems provides pharmacy students with a much-needed introduction to the mathematical intricacies of thermodynamics in relation to practical laboratory applications. Designed to meet the needs of the contemporary curriculum in pharmacy schools, the text makes these connections clear, emphasizing specific applications to pharmaceutical systems including dosage forms and newer drug delivery systems. Students and practitioners involved in drug discovery, drug delivery, and drug action will benefit from Connors' and Mecozzi's authoritative treatment of the fundamentals of thermodynamics as well as their attention to drug molecules and experimental considerations. They will appreciate, as well, the significant revisions to the Second Edition. Expanding the book's scope and usefulness, the new edition: Explores in greater depth topics most relevant to the pharmacist such as drug discovery and drug delivery, supramolecular chemistry, molecular recognition, and nanotechnologies Moves the popular review of mathematics, formerly an appendix, to the front of the book Adds new textual material and figures in several places, most notably in the chapter treating noncovalent chemical interactions Two new appendices provide ancillary material that expands on certain matters bordering the subject of classical thermodynamics Thermodynamics need not be a mystery nor confined to the realm of mathematical theory. Thermodynamics of Pharmaceutical Systems, Second Edition demystifies for students the profound thermodynamic applications in the laboratory while also serving as a handy resource for practicing researchers.

Download or read book Carbonic Anhydrase as Drug Target written by Daumantas Matulis and published by Springer. This book was released on 2019-05-21 with total page 353 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book offers deep insights into the thermodynamics and molecular structures of the twelve catalytically active isoforms of human carbonic anhydrase (CA) with a particular focus on inhibitor binding for drug design. X-ray crystallographic structures in combination with enzyme kinetic testing provide information on the interaction of CAs and their inhibitors, knowledge which is crucial for rational drug design. CAs are zinc carrying enzymes that catalyse the reversible interconversion of carbon dioxide and bicarbonate and are involved in numerous cellular processes. They are therefore a common target for drugs. The suppression of CA activities through inhibitory compounds has found application for example in diuretics and in glaucoma therapy. In this book methods used to determine binding thermodynamics of inhibitory compounds (Isothermal titration calorimetry, Fluorescent thermal shift assay/differential scanning fluorimetry and others) will be compared in detail. Also types and chemical synthesis of CA inhibitors, the use of antibodies against CAs as well as inhibitor application in animals are discussed.

Download or read book Structure based Drug Design written by John E. Ladbury and published by Landes Bioscience. This book was released on 1997 with total page 206 pages. Available in PDF, EPUB and Kindle. Book excerpt:

Download or read book Pharmacological Aspects of Molecular Recognition written by F. S. Dukhovich and published by Nova Publishers. This book was released on 2005 with total page 230 pages. Available in PDF, EPUB and Kindle. Book excerpt: In the monograph, recognition of the receptors by drugs is described as a complex phenomenon that has not been yet entirely understood. The description of molecular structure information necessary to achieve specific receptors without getting lost among huge amounts of non-specific acceptors is present. Various examples of receptor' binding features for narcotic analgetics, neuroleptics, tranquilisators, ligands of acetylcholine receptors are also included. The three stages of drug interaction with acceptors are considered, namely, distant stage, stage of orientation of the molecule on the acceptor, stage of molecule fixation. Kinetics and thermodynamics of these stages as well as factors preventing drug binding to non-specific acceptors are described. Some considerations concerning methods of changing activity and selectivity of drugs are given. Literature information needed for analysis of molecular mechanisms of interactions between drugs and receptors is present.

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 Applied Biophysics for Drug Discovery written by Donald Huddler and published by John Wiley & Sons. This book was released on 2017-10-02 with total page 148 pages. Available in PDF, EPUB and Kindle. Book excerpt: Applied Biophysics for Drug Discovery is a guide to new techniques and approaches to identifying and characterizing small molecules in early drug discovery. Biophysical methods are reasserting their utility in drug discovery and through a combination of the rise of fragment-based drug discovery and an increased focus on more nuanced characterisation of small molecule binding, these methods are playing an increasing role in discovery campaigns. This text emphasizes practical considerations for selecting and deploying core biophysical method, including but not limited to ITC, SPR, and both ligand-detected and protein-detected NMR. Topics covered include: • Design considerations in biophysical-based lead screening • Thermodynamic characterization of protein-compound interactions • Characterizing targets and screening reagents with HDX-MS • Microscale thermophoresis methods (MST) • Screening with Weak Affinity Chromatography • Methods to assess compound residence time • 1D-NMR methods for hit identification • Protein-based NMR methods for SAR development • Industry case studies integrating multiple biophysical methods This text is ideal for academic investigators and industry scientists planning hit characterization campaigns or designing and optimizing screening strategies.

Download or read book Drug Acceptor Interactions written by Niels Bindslev and published by CRC Press. This book was released on 2017-02-10 with total page 847 pages. Available in PDF, EPUB and Kindle. Book excerpt: Drug-Acceptor Interactions: Modeling theoretical tools to test and evaluate experimental equilibrium effects suggests novel theoretical tools to test and evaluate drug interactions seen with combinatorial drug therapy. The book provides an in-depth, yet controversial, exploration of existing tools for analysis of dose-response studies at equilibrium or steady state. The book is recommended reading for post-graduate students and researchers engaged in the study of systems biology, networks, and the pharmacodynamics of natural or industrial drugs, as well as for medical clinicians interested in drug application and combinatorial drug therapy. Even people without mathematical skills will be able to follow the pros and cons of reaction schemes and their related distribution equations. Chapter 9 is a hands-on guide for software to plot, fit and analyze one’s own data.

Download or read book Thermodynamics of Pharmaceutical Systems written by Kenneth A. Connors and published by Wiley-Liss. This book was released on 2002-09-17 with total page 362 pages. Available in PDF, EPUB and Kindle. Book excerpt: Studies of thermodynamics often fail to demonstrate how the mathematical intricacies of the subject relate to practical laboratory applications. Thermodynamics of Pharmaceutical Systems makes these connections clear, emphasizing specific applications to pharmaceutical systems in a study created specifically for contemporary curriculums at colleges of pharmacy. Students investigating drug discovery, drug delivery, and drug action will benefit from Kenneth Connors’s authoritative treatment of the fundamentals of thermodynamics as well as his attention to drug molecules and experimental considerations. An extensive appendix that reviews the mathematics needed to master the pharmacy curriculum proves an invaluable reference. Connors divides his one-of-a-kind text into three sections: Basic Thermodynamics, Thermodynamics of Physical Processes, and Thermodynamics of Chemical Processes; chapters include: Energy and the First Law of Thermodynamics The Entropy Concept Phase Transformations Solubility Acid-Base Equilibria Noncovalent Binding Equilibria Thermodynamics need not be a mystery nor be confined to the realm of mathematical theory. Thermodynamics of Pharmaceutical Systems introduces students of pharmacy to the profound thermodynamic applications in the laboratory while also serving as a handy resource for practicing researchers.

Download or read book A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics written by Pier Andrea Borea and published by Springer Science & Business Media. This book was released on 2009-12-01 with total page 324 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book, with its 16 chapters, documents the present state of knowledge of the adenosine A receptor. It covers a wide range of information, including data from 3 studies of theoretical, molecular and cellular pharmacology, signal transduction, integrative physiology, new drug discoveries and clinical applications. It fills an important gap in the literature since no alternative source of such information is currently available. Although the A receptor is increasingly being recognized for 3 its increasing number of biological roles throughout the body and many A receptor 3 ligands have proven useful in elucidating peripheral and central pathologies, many issues remain unresolved. Moreover, research activity in this field continues to grow exponentially, resulting in a constant flow of new information. The chapters in this book cover both basic science and the relevant applications and provide an authoritative account of the current status of the field. They have enabled my goal as editor to make “A Adenosine Receptors from Cell Biology to Pharmacology and 3 Therapeutics” an up to date, scientifically excellent, reference source, attractive to basic and clinical scientists alike, a reality. Detailed understanding of the physico-chemical aspects and molecular biology of the A receptor provides a solid basis for its future development as a target for 3 adenosine-based pharmacotherapies (Chapters 2 and 3).

Download or read book Thermodynamics and Kinetics of Drug Binding written by György Keserü and published by John Wiley & Sons. This book was released on 2015-08-17 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: This practical reference for medicinal and pharmaceutical chemists combines the theoretical background with modern methods as well as applications from recent lead finding and optimization projects. Divided into two parts on the thermodynamics and kinetics of drug-receptor interaction, the text provides the conceptual and methodological basis for characterizing binding mechanisms for drugs and other bioactive molecules. It covers all currently used methods, from experimental approaches, such as ITC or SPR, right up to the latest computational methods. Case studies of real-life lead or drug development projects are also included so readers can apply the methods learned to their own projects. Finally, the benefits of a thorough binding mode analysis for any drug development project are summarized in an outlook chapter written by the editors.

Download or read book Thermodynamics of Membrane Receptors and Channels written by Meyer B. Jackson and published by CRC Press. This book was released on 1992-11-18 with total page 454 pages. Available in PDF, EPUB and Kindle. Book excerpt: Thermodynamics of Membrane Receptors and Channels synthesizes a wealth of new information regarding the biophysics of membrane proteins. New insights provided by molecular genetics, single channel recording, and high resolution structural techniques are discussed from a conceptual perspective. Basic theoretical topics are introduced, developed, and then extensively illustrated with recent results from the literature or data from the authors' own laboratories. Theoretical and experimental information is incorporated into in-depth discussions of ion permeation mechanisms, ion channel and receptor conformational changes, aggregate activity of complexes of lipids and proteins, and how coupling is achieved between different energy modes in the many transduction systems residing in biomembranes. Thermodynamics of Membrane Receptors and Channels will be valuable both as a learning aid and a reference for biophysicists, neuroscientists, cell biologists, physiologists, and other researchers investigating any aspects of biomembranes.

Download or read book Pharmaceutical Amorphous Solid Dispersions written by Ann Newman and published by John Wiley & Sons. This book was released on 2015-03-09 with total page 502 pages. Available in PDF, EPUB and Kindle. Book excerpt: Providing a roadmap from early to late stages of drug development, this book overviews amorphous solid dispersion technology – a leading platform to deliver poorly water soluble drugs, a major hurdle in today’s pharmaceutical industry. • Helps readers understand amorphous solid dispersions and apply techniques to particular pharmaceutical systems • Covers physical and chemical properties, screening, scale-up, formulation, drug product manufacture, intellectual property, and regulatory considerations • Has an appendix with structure and property information for polymers commonly used in drug development and with marketed drugs developed using the amorphous sold dispersion approach • Addresses global regulatory issues including USA regulations, ICH guidelines, and patent concerns around the world

Download or read book Fragment Based Drug Discovery written by Steven Howard and published by Royal Society of Chemistry. This book was released on 2015-07-03 with total page 314 pages. Available in PDF, EPUB and Kindle. Book excerpt: Fragment-based drug discovery is a rapidly evolving area of research, which has recently seen new applications in areas such as epigenetics, GPCRs and the identification of novel allosteric binding pockets. The first fragment-derived drug was recently approved for the treatment of melanoma. It is hoped that this approval is just the beginning of the many drugs yet to be discovered using this fascinating technique. This book is written from a Chemist's perspective and comprehensively assesses the impact of fragment-based drug discovery on a wide variety of areas of medicinal chemistry. It will prove to be an invaluable resource for medicinal chemists working in academia and industry, as well as anyone interested in novel drug discovery techniques.

Download or read book Introduction to Biomolecular Energetics written by Irving Klotz and published by Elsevier. This book was released on 2012-12-02 with total page 153 pages. Available in PDF, EPUB and Kindle. Book excerpt: Introduction to Biomolecular Energetics Including Ligand-Receptor Interactions focuses on the concepts of energetics and their biological applications, including the study of ligand-receptor interactions. The book provides quantitative calculations and addresses topics that have become more prominent in the biochemical and related sciences in recent years, including the first and second laws of thermodynamics, the concept of entropy, free energy or chemical potential, group-transfer potential, physicochemical behavior, and enzyme kinetics. This volume is organized into 10 chapters, and it begins with an overview of the scope of energetics and two general approaches to the field: the classical or phenomenological approach and the statistical-molecular approach. The chapters that follow explore the concepts of energy and entropy in the context of the first and second laws of thermodynamics, along with the relationships between work, heat, energy and entropy as an index of exhaustion. The discussion then shifts to the free energy function and general procedures for computing standard free energies. The book also introduces the reader to the fundamental relationship between chemical potential (free energy) and concentration; high-energy bond and the concept of group-transfer potential; the use of thermodynamic methods in the analysis of physicochemical behavior; and statistical thermodynamics. The final chapter examines the number of ligands that are bound by the receptor entity, how strongly the ligands are held, and the molecular nature of the forces of ligand-receptor interaction. This book will be of interest to biologists and those who want to understand the principles of energetics governing biochemical changes.

Download or read book Protein Ligand Interactions written by Hans-Joachim Böhm and published by John Wiley & Sons. This book was released on 2006-03-06 with total page 262 pages. Available in PDF, EPUB and Kindle. Book excerpt: The lock-and-key principle formulated by Emil Fischer as early as the end of the 19th century has still not lost any of its significance for the life sciences. The basic aspects of ligand-protein interaction may be summarized under the term 'molecular recognition' and concern the specificity as well as stability of ligand binding. Molecular recognition is thus a central topic in the development of active substances, since stability and specificity determine whether a substance can be used as a drug. Nowadays, computer-aided prediction and intelligent molecular design make a large contribution to the constant search for, e. g., improved enzyme inhibitors, and new concepts such as that of pharmacophores are being developed. An up-to-date presentation of an eternally young topic, this book is an indispensable information source for chemists, biochemists and pharmacologists dealing with the binding of ligands to proteins.