Methods in Molecular Biology, Volume 716: Drug Design and Discovery: Methods and Protocols

Abstract

Over the past few years, small molecule screening has undergone a dramatic shift from simple ‘cheap and fast’ high-throughput assay systems to more complex screening setups where one aims to use more physiologically relevant systems. The new edition of ‘Methods in Molecular Biology: Drug Design and Discovery’ aims to cover aspects of this new approach with a comprehensive volume about various strategies in drug discovery. This volume is an easily accessible collection of protocols covering a broad range of different screening methodologies. The book is divided into 16 chapters that cover topics such as the design of large therapeutic molecules (DNA or peptides), revised protocols for the use of conventional assays in primary screening, computational methods and animal models for pre-clinical evaluation of drug candidates. One particular emphasis is the use of computational methods in drug discovery, which is covered in the first four chapters of the book. Chapter 4 (‘Methods for evaluation of structural and biological properties of anti-invasive natural products’) deserves particular mention in this regard, and the authors provide protocols for isolation and purification of compounds, the use of 3D model systems in cell culture and 3D QSAR modelling applications. Another major emphasis of this book is the use of animal models in primary screening (such as chapter 12, ‘Chemical screening with zebrafish embryos’ and chapter 10, ‘Imaging NFkB signaling in mice for screening anticancer drugs’) or in pre-clinical testing (chapter 15, ‘Evaluation of antibacterial activity of proteins and peptides using a specific animal model for wound healing’). Other noteworthy areas covered are the use of mass spectroscopy, in vivo imaging in drug discovery, and the use of in vitro phage display for selection of peptide ligands in human placental transcytosis systems (chapter 8; clearly a gem in this book). The strong academic background of the authors makes this book highly recommendable to everyone involved in drug screening and has a particular appeal to an academic audience. Written in the highly successful format of the Methods in Molecular Biology series, each chapter includes a background on the topic, a list of materials required, a detailed step-by-step description of the methods and a notes section that draws attention to potential pitfalls and highlights some of the key steps in the procedure. All protocols provide very detailed instructions, a characteristic of the Methods in Molecular Biology series. The only minor drawback of this volume is the slightly misleading title. This collection of protocols touches very briefly on drug design. The book rather focuses on novel approaches to drug screening and physiological validation. It is highly recommended for all those who are performing drug screening or who aim to be doing so in the near future.