Advances in chemistry, biology and genomics coupled with laboratory automation and computational technologies have led to the rapid emergence of the multidisciplinary field of chemical genomics. This edited text, with contributions from experts in the field, discusses the new techniques and applications that help further the study of chemical genomics. The beginning chapters provide an overview of the basic principles of chemical biology and chemical genomics. This is followed by a technical section that describes the sources of small-molecule chemicals; the basics of high-throughput screening technologies; and various bioassays for biochemical-, cellular- and organism-based screens. The final chapters connect the chemical genomics field with personalized medicine and the druggable genome for future discovery of new therapeutics. This book will be valuable to researchers, professionals and graduate students in many fields, including biology, biomedicine and chemistry.

Chemical genomics is a highly interdisciplinary and very exciting field of research both in academics and in the life sciences industry. The Ernst Schering Research Foundation Workshop 58 was organized to bring together scientific leaders in the field to discuss the implications of chemical genomics for drug discovery. Various aspects of the interface between chemistry and biology are covered in this volume, such as chemogenomics efforts in the pharmaceutical industry, diversity-oriented synthesis, chemogenomic approaches to the study of cell function, screening technologies, and natural products as tools in chemical biology.

Chemical genomics is an exciting new field that aims to transform biolo- cal chemistry into a high-throughput industrialized process, much in the same way that molecular biology has been transformed by genomics. The inter- tion of small organic molecules with biological systems (mostly proteins) underpins drug discovery in the pharmaceutical and biotechnology industries, and therefore a volume of laboratory protocols that covers the key aspects of chemical genomics would be of use to biologists and chemists in these orga- zations. Academic scientists have been exploring the functions of proteins using small molecules as probes for many years and therefore would also b- efit from sharing ideas and laboratory procedures. Whatever the organizational backgrounds of the scientists involved, the challenges of extracting the ma- mum human benefit from genome sequencing projects remains considerable, and one where it is increasingly recognized that chemical genomics will play an important part. Chemical Genomics: Reviews and Protocols is divided into two sections, the first being a series of reviews to describe what chemical genomics is about and to set the scene for the protocol chapters. The subject is introduced by Paul Caron, who explains the various flavors of chemical genomics. This is f- lowed by Lutz Weber and Philip Dean who cover the interaction between organic molecules and protein targets from the different perspectives of la- ratory experimentation and in silico design. The protocols begin with the me- ods developed in Christopher Lowes’ laboratory (Roque et al.

Since the publication of the pioneering first edition of Chemical Genomics and Proteomics more than seven years ago, the area of chemical genomics has rapidly expanded and diversified to numerous novel methods and subdisciplines, such as chemical glycomics and lipidomics. This second edition has been updated to uniquely reflect this interdisciplinary feature as well as the remarkable developments that have occurred. The new edition also covers innovative applications from cell biology to drug discovery to, more recently, clinical diagnostics and medical practice, which utilize the concepts of chemical genomics. The text provides an overview of the strategies and methodologies of chemical genomics, focusing on emerging technologies and recent applications in the areas of combination chemical genetics, toxicogenomics, drug chemical genomics and proteomics, and orthogonal chemical genetics. It describes the development and application of novel analytical methods used in lipodomics, such as steroidomics. The book also discusses biomarker discovery applications of microarray technologies using DNA, RNA, and protein and glycan arrays. Chapters cover further applications of biomolecular biomarkers for disease diagnosis, in small molecule drug R&D, and during therapeutic use of medicines. These include prognostic, disease specific, response (surrogate), and toxicity biomarkers. In addition, the text explores the principles of contemporary systems biology and genomics in experimental medicine—a new paradigm that demonstrates a network-oriented view and advanced statistical and informatics data management, opening the way toward personalized medicine. Finally, various in silico chemogenomics approaches are addressed for predicting binding of drug candidates to undesirable targets, which would help in designing better clinical candidates with fewer side effects. This new edition benefits a broad range of readers from industrial and academic researchers in drug discovery, medicinal chemistry, and molecular and cell biology to physicians in clinical diagnostics and students in related fields of study.

Chemical genomics is a highly interdisciplinary and very exciting field of research both in academics and in the life sciences industry. The Ernst Schering Research Foundation Workshop 58 was organized to bring together scientific leaders in the field to discuss the implications of chemical genomics for drug discovery. Various aspects of the interface between chemistry and biology are covered in this volume, such as chemogenomics efforts in the pharmaceutical industry, diversity-oriented synthesis, chemogenomic approaches to the study of cell function, screening technologies, and natural products as tools in chemical biology.

Chemical Biology of the Genome provides a comprehensive overview of essential concepts and principles of genomic and epigenomics dynamics as explored through the lens of chemical biology. Key examples and case studies illustrate chemical biology methods for study and analysis of the genome and epigenome, with an emphasis on relevance to physiological and pathophysiological processes and drug discovery. Authors and international leaders in biochemical studies of the genome, Drs. Siddhartha Roy and Tapas Kundu, adopt an integrated, interdisciplinary approach throughout, demonstrating how fast evolving chemical and mass-scale sequencing tools are increasingly used to interpret biochemical processes of the genome. Later sections discuss chemical modifications of the genome, DNA sequence recognition by proteins and gene regulation, GWAS and EpiGWAS studies, 3D architecture of the genome, and functional genome architecture. In-depth, discovery focused chapters examine intervention in gene networks using SiRNA/ShRNA, miRNA, and anti-miR, small molecule modulation of iPS, drug resistance pathways altered DNA methylation as drug targets, anti-miR as therapeutics, and nanodelivery of drugs. Offers an interdisciplinary discussion of the chemical biology of the genome and epigenome, employing illustrative case studies in both physiological and pathophysiological contexts Supports researchers in employing chemical and mass-scale sequencing approaches to interpret genomic and epigenomic dynamics Highlights innovative pathways and molecular targets for new disease study and drug discovery

This text covers new techniques and applications in chemical genomics for researchers, professionals and graduates in biology, biomedicine and chemistry.