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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...
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.
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 biophysica...
Over the last decade, high-sensitivity calorimetry has developed from a specialist method used mainly by dedicated experts to a major, commercially available tool in the arsenal directed at understanding molecular interactions and stability. Calorimeters have now become commonplace in bioscience laboratories. As a result, the number of those proficient in experimentation in this field has risen dramatically, as has the range of experiments to which these methods have been applied. Applications extend from studies in small molecule and solvent biophysics, through drug screening to whole cell assays. The technology has developed to include higher levels of sensitivity (and hence smaller sample...
Progress in Medicinal Chemistry
This book presents a first-hand account of the inner workings of the National Union of Mineworkers (NUM) in its confrontation with the Tory government during the Miners’ Strike of 1984/5 that changed the face of industrial relations in the UK forever. It charts the spirited defence against mine closures and the devastating aftermath, including the privatisation of British Coal, leading inexorably to the demise of the UK coal industry.
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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...
"High Throughput Screening (HTS) is one of several hit identification approaches that are part of a developing and evolving toolbox for the discovery of pharmaceutical start points. HTS remains one of the most successful approaches, and therefore an important foundation of drug discovery. In High Throughput Screening: Methods, Techniques and Applications, leading industrial and academic experts in screening and drug discovery explain key technologies and methods while demonstrating how they can be applied to successful hit identification. Describing both traditional and emerging methods in detail, this book provides an overview of these methods to the reader that will serve both those new to...