The goal of an activity-directed isolation process is to isolate bioactive compounds which may provide structural leads of therapeutic importance. Whereas the traditional process of drug development is long and expensive, simple and rapid bioassays can serve as the starting point for drug discovery. This book presents a range of "bench top" bioassa
Bioassay Methods in Natural Product Research and Drug Development contains the proceedings from the Phytochemical Society of Europe's very successful symposium on this topic, held August 24-27, 1997 in Uppsala, Sweden. In this volume, leading academic and industrial scientists discuss novel methods for assaying natural products to find new structure-activity relationships. Of key importance in this process is the availability and reliability of specific bioassay methods, but chapters also discuss chemical and biological diversity and how to dereplicate natural product extracts to increase efficiency in lead discovery. Anti-tumor, HIV-inhibitory, antiprotozoal, anti-infective and immunomodulatory natural products are discussed. Various industrial projects are presented for the first time. This volume bridges the gap between academic and industrial research and scientists, and should be required reading in drug companies and faculties of pharmacy, as well as serving scientists in pharmacognosy, pharmacology, phytochemistry, natural products and drug discovery.
This comprehensive and useful handbook represents a definitive up-to-date compendium of key in vitro bioassay methods that are employed to quantify and validate the anticancer activity of a drug candidate before it makes its way in to animal or clinical trials. In Vitro Bioassay Techniques for Anticancer Drug Discovery and Development covers the screening and evaluation of potential drug candidates in a wide category of anticancer assays demonstrating the specific ways in which various pharmaceutical bioassays interpret the activity of drug molecules. The major emphasis of the book is to present those bioassays which can be readily set up and practiced in any laboratory with limited funds, facilities or technical know-how.
The definitive compendium of bioassay procedures and applications A virtual encyclopedia of key bioassay protocols, this up-to-date, essential resource reviews the methods and applications of bioassays that quantify drug activity and evaluate the validity of pharmacological models. Demonstrating the specific ways in which various pharmaceutical bioassays interpret the activity of drug molecules, the book covers the evaluation and screening of drug compounds in a wide spectrum of therapeutic categories. Throughout, the authors use various models to link experimental observations with findings that clarify the effect of drug compounds on cellular biology and measure the pharmacological activity of chemical substances. This provides an important technological platform for successful drug research and clinical therapy, making Pharmaceutical Bioassays an ideal sourcebook for pharmacologists, pharmaceutical and medical researchers, analytical chemists, toxicologists, and students. Just as a fundamental knowledge of pharmaceutical bioassays is vital to understanding how bioactive agents and new drugs are defined, discovered, and developed, so too is this indispensable reference, which: Offers a complete reference on pharmaceutical bioassays and their specific applications in the assessment of therapies for cancer, Alzheimer’s, diabetes, epilepsy, inflammation, antimalarials, pharmacogenomics, and other major therapeutic areas Covers bioassays that measure toxicity, including those for chemical toxicity and hepatoxicity—a particularly significant consideration in the development of safe and tolerable medications Highlights clinically relevant methods, ideas, and techniques to support any pharmaceutical researcher Suggests guidelines and systems to enhance communication between pharmacologists, chemists, and biologists Provides an informative analysis of pharmaceutical bioassay technologies and lab applications
A Comprehensive Guide to Toxicology in Preclinical Drug Development is designed for toxicologists who need a thorough understanding of the drug development process. This multi-contributed reference will provide a detailed picture of the complex and highly interrelated activities of preclinical toxicology in both small molecules and biologics --
Improving and Accelerating Therapeutic Development for Nervous System Disorders is the summary of a workshop convened by the IOM Forum on Neuroscience and Nervous System Disorders to examine opportunities to accelerate early phases of drug development for nervous system drug discovery. Workshop participants discussed challenges in neuroscience research for enabling faster entry of potential treatments into first-in-human trials, explored how new and emerging tools and technologies may improve the efficiency of research, and considered mechanisms to facilitate a more effective and efficient development pipeline. There are several challenges to the current drug development pipeline for nervous system disorders. The fundamental etiology and pathophysiology of many nervous system disorders are unknown and the brain is inaccessible to study, making it difficult to develop accurate models. Patient heterogeneity is high, disease pathology can occur years to decades before becoming clinically apparent, and diagnostic and treatment biomarkers are lacking. In addition, the lack of validated targets, limitations related to the predictive validity of animal models - the extent to which the model predicts clinical efficacy - and regulatory barriers can also impede translation and drug development for nervous system disorders. Improving and Accelerating Therapeutic Development for Nervous System Disorders identifies avenues for moving directly from cellular models to human trials, minimizing the need for animal models to test efficacy, and discusses the potential benefits and risks of such an approach. This report is a timely discussion of opportunities to improve early drug development with a focus toward preclinical trials.
This detailed book explores protocols for a wide array of preclinical pharmacology and toxicology evaluations to be applied to chemical drugs and their development through in vitro, involving tissues and cell lines, and in vivo models, using animals as experimental systems, utilized to conduct pharmacological research. Written for the Springer Protocols Handbooks series, the methodologies included in this collection have been standardized by the authors through extensive use in the lab so that they are ready to be applied in the labs of readers around the world. Authoritative and practical, Bioassays in Experimental and Preclinical Pharmacology aims to assist undergraduate and postgraduate students, research scholars, scientists, and other academicians performing research in the vital field of drug discovery.
Essential principles and practice of assay development The first comprehensive, integrated treatment of the subject, Assay Development: Fundamentals and Practices covers the essentials and techniques involved in carrying out an assay project in either a biotechnology/drug discovery setting or a platform setting. Rather than attempting comprehensive coverage of all assay development technologies, the book introduces the most widely used assay development technologies and illustrates the art of assay development through a few commonly encountered biological targets in assay development (e.g., proteases, kinases, ion channels, and G protein-coupled receptors). Just enough biological background for these biological targets is provided so that the reader can follow the logics of assay development. Chapters discuss: The basics of assay development, including foundational concepts and applications Commonly used instrumental methods for both biochemical assays and cell-based assays Assay strategies for protein binding and enzymatic activity Cell-based assays High-throughput screening An in-depth study of the now popular Caliper's off-chip kinase assay provides an instructive, real-world example of the assay development process.
Exploring innovative routes of drug discovery in the postgenomic era, Microbial Genomics and Drug Discovery examines bioinformatic and genomic approaches for the identification, detection, selection, and validation of new antibacterial targets and vaccine candidates. The book discusses potential pathways for effective infection control, inhibition of antibacterial resistance, and acceleration of the drug discovery process. This comprehensive reference describes procedures to recognize common targets in various bacterial species for the design of broad-spectrum antibiotics and clearly illustrates the use of pathway tools in a genomics-based drug discovery project.
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.
