A Practical Guide to Assay Development and High-Throughput Screening in Drug Discovery

by Taosheng Chen

Overview

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.

Product Details

ISBN-13:	9780367384708
Publisher:	Taylor & Francis
Publication date:	10/15/2019
Pages:	292
Product dimensions:	7.00(w) x 10.00(h) x (d)

About the Author

Taosheng Chen earned a BS in biophysics and an MS in molecular cell biology from Fudan University in Shanghai, China. He received his PhD in cell and molecular biology from the University of Vermont at Burlington. Dr. Chen joined the faculty of the Department of Chemical Biology and Therapeutics and became director of the HTS Center at the St. Jude Children’s Research Hospital in Memphis in 2006. His laboratory focuses on studying the regulation of transcription factors and their implications in drug metabolism and drug resistance as well as in pediatric cancers. Dr. Chen has authored more than 20 peer-reviewed articles in the areas of cancer biology, drug metabolism, signal transduction, and drug discovery technology.

Table of Contents

Preface vii

Acknowledgments ix

About the Editor xi

Contributors xiii

Chapter 1 Assay Development for Protein Kinases and Phosphatases J. Fraser Glickman 1

Chapter 2 Fluorescence-Based Biochemical Protease Assay Formats Julian Woelcke Ulrich Hassiepen 25

Chapter 3 Assay Development for Nuclear Hormone Receptors Chang Bai Eric N. Johnson 49

Chapter 4 Assay Development for G Protein-Coupled Receptors and Ion Channels Joseph G. McGivern Yi-xin Qian Paul H. Lee 59

Chapter 5 Assay Development for Heat Shock Proteins Zhenhai Gao Susan Fong 83

Chapter 6 Assay Development for Cell Viability and Apoptosis for High-Throughput Screening Terry L. Riss Richard A. Moravec Andrew L. Niles 99

Chapter 7 Assay Development for Antimicrobial Drug Discovery H. Howard Xu 123

Chapter 8 Image-Based High-Content Screening Yan Feng Christopher J. Wilson 143

Chapter 9 Application of RNA Interference in Drug Discovery Natalie M. Wolters Jeffrey P. MacKeigan 157

Chapter 10 Assay Development Using Primary and Primary-Like Cells Sabrina Corazza Erik J. Wade 169

Chapter 11 Screening Automation Wei Zheng Catherine Z. Chen 183

Chapter 12 Compound Library Management Dalin Nie 193

Chapter 13 Unique Discovery Aspects of Utilizing Botanical Sources Susan P. Manly Troy Smillie John P. Hester Ikhlas Khan Louis Coudurier 213

Chapter 14 Screening Informatics Stephan C. Schürer Nicholas F. Tsinoremas 233

Index 265