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Fragment-based Drug Discovery
From its origins as a niche technique more than 15 years ago, fragment-based approaches have become a major tool for drug and ligand discovery, often yielding results where other methods have failed. Written by the pioneers in the field, this book provides a comprehensive overview of current methods and applications of fragment-based discovery, as well as an outlook on where the field is headed. The first part discusses basic considerations of when to use fragment-based methods, how to select targets, and how to build libraries in the chemical fragment space. The second part describes established, novel and emerging methods for fragment screening, including empirical as well as computational approaches. Special cases of fragment-based screening, e. g. for complex target systems and for covalent inhibitors are also discussed. The third part presents several case studies from recent and on-going drug discovery projects for a variety of target classes, from kinases and phosphatases to targeting protein-protein interaction and epigenetic targets.
Fragment-based Approaches in Drug Discovery
This first systematic summary of the impact of fragment-based approaches on the drug development process provides essential information that was previously unavailable. Adopting a practice-oriented approach, this represents a book by professionals for professionals, tailor-made for drug developers in the pharma and biotech sector who need to keep up-to-date on the latest technologies and strategies in pharmaceutical ligand design. The book is clearly divided into three sections on ligand design, spectroscopic techniques, and screening and drug discovery, backed by numerous case studies.
Can Japan Globalize?
Japan's deepest recession since the Second World War has come to an end in 2000. Yet, the task of reforming Japan is far from completed. The current political drift has brought deregulation to a premature end putting the still vulnerable recovery at risk. What structural changes have already taken place? What important reforms have to be undertaken in the future? The contributions of the book shed light on the transitional path of the Japanese system amid rapid globalization. Can Japan Globalize? covers a broad range of areas from macro- and micro-economic structures to political and social relations.
BioNMR in Drug Research
The vast progress made in the investigation of biomolecules using NMR has only recently been rewarded with the Nobel Prize for Kurt Wüthrich. Edited by a former coworker of Wüthrich, this book presents the theoretical background on NMR of biomolecules, plus the use of NMR techniques in determining the structures of proteins and nucleic acids. BioNMR spectroscopy offers a universal tool for examining the binding of an active substance to its target protein. Its use thereby benefits the rational development of drugs. This interaction can now be investigated in a hitherto unparalleled precision and displayed in 3D - an important prerequisite for the targeted development of new active substances. The latest methods for characterizing substance-receptor complexes are demonstrated backed by many case studies from pharmaceutical research. Thus it comes as no surprise that a large number of the authors are working for leading pharmaceutical companies. With its successful mixture of basic information and application strategies, coupled with many real-life examples, this is an invaluable guide for both NMR spectroscopists and pharmaceutical researchers.
The Geometry of Biological Time
Dealing with dynamics of processes that repeat themselves regularly, this revised and updated edition extends the thread from 1980 to the present day, concentrating on areas of interest where there will be much activity in the future. This involves going through spatial biochemical, electrophysiological, and organismic dynamical systems and patterns that were discovered by pursuing the theme of phase singularities introduced in the original book. In particular the work on excitability in cell membranes will be thoroughly updated as will the references throughout the book.
Isotope labeling in Biomolecular NMR
NMR spectroscopy has undergone a revolution in recent years with the advent of several new methods overcoming the problems of sensitivity and resolution. Recent developments in biotechnology have made it easier and economical to introduce 13C, 15N and 2H into proteins and nucleic acids. At the same time, there has been an explosion in the number of NMR experiments that utilize such isotope labeled samples. Thus, a combination of isotopic labeling and multidimensional, multinuclear NMR has opened up new avenues for structural studies of proteins, nucleic acids and their complexes. This book will focus on recent developments in isotope labeling methods for structural studies of small molecules, peptides, proteins and nucleic acids. The aim of the book is to serve as a compendium of isotope labeling for the biomolecular NMR community providing comprehensive coverage of the existing methods and latest developments along with protocols and practical hints on the various experimental aspects. The book will cover a wide range of topics in isotope labeling under one title including emerging areas of metabolonomics and solid state NMR.
Protein Tyrosine Kinases
Leading researchers, from the Novartis group that pioneered Gleevec/GlivecTM and around the world, comprehensively survey the state of the art in the drug discovery processes (bio- and chemoinformatics, structural biology, profiling, generation of resistance, etc.) aimed at generating PTK inhibitors for the treatment of various diseases, including cancer. Highlights include a discussion of the rationale and the progress made towards generating "selective" low molecular-weight kinase inhibitors; an analysis of the normal function, role in disease, and application of platelet-derived growth factor antagonists; and a summary of the factors involved in successful structure-based drug design. Additional chapters address the advantages and disadvantages of in vivo preclinical models for testing protein kinase inhibitors with antitumor activity and the utility of different methods in the drug discovery and development process for determining "on-target" vs "off-target" effects of kinase inhibitors.
Biocomputing 2001 - Proceedings Of The Pacific Symposium
The Pacific Symposium on Biocomputing brings together key researchers from the international biocomputing community. It is designed to be maximally responsive to the need for critical mass in subdisciplines within biocomputing. This book contains peer-reviewed articles in computational biology.
CADD and Informatics in Drug Discovery
This book updates knowledge on recent advances in computational, biophysical and bioinformatics tools/techniques and their practical applications in modern drug design and discovery paradigm. It also encompasses fundamental principles, advanced methodologies and applications of various CADD approaches including several cutting-edge areas; presenting recent developments covering ongoing trends in the field of computer-aided drug discovery. Having contributions by a global team of experts, the book is expected to be an ideal resource for drug discovery scientists, medicinal chemists, pharmacologists, toxicologists, phytochemists, biochemists, biologists, R&D personnel, researchers, students, t...
Bioactive Conformation II
This series presents critical reviews of the present position and future trends in modern chemical research. It contains short and concise reports on chemistry, each written by the world renowned experts. The volume is still valid and useful after five or ten years. More information, as well as the electronic version of the whole content, is available at: springerlink.com.
