The Handbook of Assay Development in Drug Discovery describes all the tools currently available for performing various assay techniques. Featuring troubleshooting advice for common problems from experienced assay developers, the vendor community, and scientists in the pharmaceutical industry, the book presents descriptions of methods, laboratory guidelines and protocols used to perform such methods, specific examples of each assay system, and troubleshooting tools. Designed as a guide to running an assay from start to finish, this is an ideal bench top companion for scientists involved in drug discovery screening, lead profiling, therapeutic target evaluation, and assay development and implementation.

The development of suitable assays, the integration of appropriate technology, and the effective management of the essential infrastructure are all critical to the success of any high-throughput screening (HTS) endeavor. However, few scientists have the multidisciplinary experience needed to control all aspects of an HTS drug discovery project. A Practical Guide to Assay Development and High-Throughput Screening in Drug Discovery integrates the experience of diverse experts who offer fundamental and practical guidance across numerous situations. The book first discusses assay developments for important target classes such as protein kinases and phosphatases, proteases, nuclear receptors, G protein-coupled receptors, ion channels, and heat shock proteins. It next examines assay developments for cell viability, apoptosis, and infectious diseases. The contributors explore the application of emerging technologies and systems, including image-based high content screening, RNA interference, and primary cells. Finally, they discuss the essential components of the integrated HTS process, such as screening automation, compound library management, the screening of natural products from botanical sources, and screening informatics. Designed to motivate researchers to bring further advances to the field, this volume provides practical guidance on how to initiate, validate, optimize, and manage a bioassay intended to screen large collections of compounds. Drawing on the knowledge from experts actively involved in assay development and HTS, this is a resource that is both comprehensive and focused.

A presentation of screening techniques, modern technologies, and high-capacity instrumentation for increased productivity in the development and discovery of new drugs, chemical compounds, and targeted delivery of pharmaceuticals. It contains practical applications and examples of strategies in cell-based and cell-free screens as well as homogeneous, fluorescence, chemiluminescence, and radioactive-based technologies.

Discover how biomarkers can boost the success rate of drug development efforts As pharmaceutical companies struggle to improve the success rate and cost-effectiveness of the drug development process, biomarkers have emerged as a valuable tool. This book synthesizes and reviews the latest efforts to identify, develop, and integrate biomarkers as a key strategy in translational medicine and the drug development process. Filled with case studies, the book demonstrates how biomarkers can improve drug development timelines, lower costs, facilitate better compound selection, reduce late-stage attrition, and open the door to personalized medicine. Biomarkers in Drug Development is divided into eight parts: Part One offers an overview of biomarkers and their role in drug development. Part Two highlights important technologies to help researchers identify new biomarkers. Part Three examines the characterization and validation process for both drugs and diagnostics, and provides practical advice on appropriate statistical methods to ensure that biomarkers fulfill their intended purpose. Parts Four through Six examine the application of biomarkers in discovery, preclinical safety assessment, clinical trials, and translational medicine. Part Seven focuses on lessons learned and the practical aspects of implementing biomarkers in drug development programs. Part Eight explores future trends and issues, including data integration, personalized medicine, and ethical concerns. Each of the thirty-eight chapters was contributed by one or more leading experts, including scientists from biotechnology and pharmaceutical firms, academia, and the U.S. Food and Drug Administration. Their contributions offer pharmaceutical and clinical researchers the most up-to-date understanding of the strategies used for and applications of biomarkers in drug development.

This reference book contains a comprehensive selection of the most frequently used assays for reliably detecting pharmacological effects of potential drugs, including tests for cardiovascular, analgesic, psychotropic, metabolic, endocrine, respiratory, renal, and immunomodulatory activities. Each of the over 700 assays comprises a detailed protocol with the purpose and rationale of the method, a description of the experimental procedure, a critical assessment of the results and their pharmacological and clinical relevance, and pertinent references. Identification of specific tests is facilitated by the enclosed CD-ROM which allows for a quick and full text research. An appendix with guidelines and legal regulations for animal experiments in various countries will help to plan these experiments properly in accordance with the welfare of laboratory animals.

This unique volume traces the critically important pathway by which a "molecule" becomes an "anticancer agent. " The recognition following World War I that the administration of toxic chemicals such as nitrogen mustards in a controlled manner could shrink malignant tumor masses for relatively substantial periods of time gave great impetus to the search for molecules that would be lethal to specific cancer cells. Weare still actively engaged in that search today. The question is how to discover these "anticancer" molecules. Anticancer Drug Development Guide: Preclinical Screening, Clinical Trials, and Approval, Second Edition describes the evolution to the present of preclinical screening methods. The National Cancer Institute's high-throughput, in vitro disease-specific screen with 60 or more human tumor cell lines is used to search for molecules with novel mechanisms of action or activity against specific phenotypes. The Human Tumor Colony-Forming Assay (HTCA) uses fresh tumor biopsies as sources of cells that more nearly resemble the human disease. There is no doubt that the greatest successes of traditional chemotherapy have been in the leukemias and lymphomas. Since the earliest widely used in vivo drug screening models were the murine L 1210 and P388 leukemias, the community came to assume that these murine tumor models were appropriate to the discovery of "antileukemia" agents, but that other tumor models would be needed to discover drugs active against solid tumors.

This comprehensive, practical guide presents an explanation of the latest techniques and methods in drug discovery, including: Genomics, proteomics, high-throughput screening, and systems biology Summaries of how these techniques and methods are used to discover new central nervous system agents, antiviral agents, respiratory drugs, oncology drugs, and more Specific approaches to drug discovery, including problems that are encountered, solutions to these problems, and limitations of various methods and techniques.