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The introduction of combinatorial chemistry technology has increased the amount of compounds generated in a year from 50 to 2000. Conventional analytical approaches simply cannot keep up. These circumstances have caused drug discovery to take on the shape of a bottleneck, like traffic through a toll booth. In order to break the bottleneck, a corres
Backed by leading authorities, this is a professional guide to successful compound screening in pharmaceutical research and chemical biology, including the chemoinformatic tools needed for correct data evaluation. Chapter authors from leading pharmaceutical companies as well as from Harvard University discuss such factors as chemical genetics, binding, cell-based and biochemical assays, the efficient use of compound libraries and data mining using cell-based assay results. For both academics and professionals in the pharma and biotech industries working on small molecule screening.
High Throughput Bioanalytical Sample Preparation: Methods and Automation Strategies is an authoritative reference on the current state-of-the-art in sample preparation techniques for bioanalysis. This book focuses on high throughput (rapid productivity) techniques and describes exactly how to perform and automate these methodologies, including useful strategies for method development and optimization. A thorough review of the literature is included within each of these chapters describing high throughput sample preparation techniques: protein removal by precipitation; equilibrium dialysis and ultrafiltration; liquid-liquid extraction; solid-phase extraction; and various on-line techniques. The text begins with an introductory overview of the role of bioanalysis in pharmaceutical drug development. Fundamental understanding of the strategies for sample preparation is reinforced next, along with essential concepts in extraction chemistry. Several chapters introduce and discuss microplates, accessory products and automation devices. Particular strategies for efficient use of automation within a bioanalytical laboratory are also presented. The subject material then reviews protein precipitation, liquid-liquid extraction, solid-phase extraction and various on-line sample preparation approaches. The book concludes with information on recent advances in sample preparation, such as solid-phase extraction in a card format and higher density extraction plates. Important objectives that can be accomplished when the strategies presented in this book are followed include: improved efficiency in moving discovery compounds to preclinical status with robust analytical methods; return on investment in automation for sample preparation; and improved knowledge and expertise of laboratory staff. · Shows the reader exactly how to perform modern bioanalytical sample preparation techniques, complete with detailed strategies · Thorough literature review and summary of published information · Detailed discussion and examples of the method development process
High throughput screening remains a key part of early stage drug and tool compound discovery, and methods and technologies have seen many fundamental improvements and innovations over the past 20 years. This comprehensive book provides a historical survey of the field up to the current state-of-the-art. In addition to the specific methods, this book also considers cultural and organizational questions that represent opportunities for future success. Following thought-provoking foreword and introduction from Professor Stuart Schreiber and the editors, chapters from leading experts across academia and industry cover initial considerations for screening, methods appropriate for different goals in small molecule discovery, newer technologies that provide alternative approaches to traditional miniaturization procedures, and practical aspects such as cost and resourcing. Within the context of their historical development, authors explain common pitfalls and their solutions. This book will serve as both a practical reference and a thoughtful guide to the philosophy underlying technological change in such a fast-moving area for postgraduates and researchers in academia and industry, particularly in the areas of chemical biology, pharmacology, structural biology and assay development.
Furnishing the latest interdisciplinary information on the most important and frequently the only investigational system available for discovery programs that address the effects of small molecules on newly discovered enzyme and receptor targets emanating from molecular biology, this timely resource facilitates the transition from classical to high throughput screening (HTS) systems and provides a solid foundation for the implementation and development of HTS in bio-based industries and associated academic environments.
"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 the field and expert scientists alike. High Throughput Screening: Methods, Techniques and Applications provides readers with an outline of key elements in the areas of assay development, detailed descriptions of a range of both biochemical and cell-based screening methodologies and strategies, as well as highlighting important steps in data analysis. By describing the basic principles of methods commonly used in HTS, High Throughput Screening: Methods, Techniques and Applications provides an illuminating introduction to HTS, capturing established good practice within the field, thereby imparting both the industrial and academic researcher with the knowledge required to work effectively in both today's and the hit identification laboratories of the future"--
This concise, self-contained and cohesive book focuses on commonly used and recently developed methods for designing and analyzing high-throughput screening (HTS) experiments from a statistically sound basis. Combining ideas from biology, computing and statistics, the author explains experimental designs and analytic methods that are amenable to rigorous analysis and interpretation of RNAi HTS experiments. The opening chapters are carefully presented to be accessible both to biologists with training only in basic statistics and to computational scientists and statisticians with basic biological knowledge. Biologists will see how new experiment designs and rudimentary data-handling strategies for RNAi HTS experiments can improve their results, whereas analysts will learn how to apply recently developed statistical methods to interpret HTS experiments.
HIGH THROUGHPUT ANALYSIS FOR FOOD SAFETY MEETS FSMA REQUIREMENTS WITH THE LATEST ADVANCES IN HIGH-THROUGHPUT SCREENING High-Throughput Analysis for Food Safety addresses the fundamental concepts involved in the rapid screening for contaminants, including residual veterinary drugs, proteins, metals, hormones, pesticides, and adulterants. Addressing the need for—and requirements of—rapid screening tests, the book includes discussions of regulations and compliance issues from perspectives of both domestic and global industry and government contributors. The latest developments and most common techniques are focused on, with an emphasis on the applicability of both stand-alone mass spectrometry methods and coupled techniques. Beginning with a review of high-throughput analysis basics, the authors conduct a full exploration of mass spectrometry applications allowing readers to: Survey GC-MS, LC-MS, stand-alone MS, and tandem MS methods in foodanalysis and contaminant screening Review quality control standards, method validation, and ongoing analyticalcontrol Examine the current methods used to detect veterinary medicinal productresidues in food, as well as future directionsRecent Recent incidents around the globe have turned the food industry toward high-throughput analysis, and the Food Safety Modernization Act has made it a legal requirement in the US. This resource provides an in-depth discussion of the latest advances in methods and instrumentation.
High Throughput Analysis for Early Drug Discovery offers concise and unbiased presentations by synthetic and analytical chemists who have been involved in creating and moving the field of combinatorial chemistry into the academic and industrial mainstream. Since the synthetic method often dictates the appropriate types of analysis, each chapter or section begins with a description of the synthesis approach and its advantages. The description of various combinatorial and high-throughput parallel synthesis techniques provide a relevant point of entry for synthetic chemists who need to set up appropriate characterisation methods for his/her organisation. This is an invaluable resource for all organic and analytical chemists in the pharmaceutical, agrochemical, and biotechnology fields who are either involved in, or beginning to investigate combinatorial techniques to increase overall efficiency and productivity. First reference to focus on the analytical side of synthesis
Here in a single source is a complete spectrum of ideas on the development of new anticancer drugs. Containing concise reviews of multidisciplinary fields of research, this book offers a wealth of ideas on current and future molecular targets for drug design, including signal transduction, the cell division cycle, and programmed cell death. Detailed descriptions of sources for new drugs and methods for testing and clinical trial design are also provided. - One work that can be consulted for all aspects of anticancer drug development - Concise reviews of research fields, combined with practical scientific detail, written by internationally respected experts - A wealth of ideas on current and future molecular targets for drug design, including signal transduction, the cell division cycle, and programmed cell death - Detailed descriptions of the sources of new anticancer drugs, including combinatorial chemistry, phage display, and natural products - Discussion of how new drugs can be tested in preclinical systems, including the latest technology of robotic assay systems, cell culture, and experimental animal techniques - Hundreds of references that allow the reader to access relevant scientific and medical literature - Clear illustrations, some in color, that provide both understanding of the field and material for teaching