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"With increasing use of ligand-binding assays (LBAs) in the pharmaceutical industry, the need to critically evaluate technical and regulatory issues related to the use of these technologies has increased greatly. This book fills that void and provides a reference text covering critical aspects of the development, validation, and implementation of LBAs in the drug development field. It includes: immunochemistry and protein chemistry, method development, validation, statistics, software, regulatory issues, and applications to immunogenicity and biomarkers. "

"The lock-and-key principle formulated by Emil Fischer as early as the end of the 19th century has still not lost any of its significance for the life sciences. The basic aspects of ligand-protein interaction may be summarized under the term 'molecular recognition' and concern the specificity as well as stability of ligand binding. Molecular recognition is thus a central topic in the development of active substances, since stability and specificity determine whether a substance can be used as a drug. Nowadays, computer-aided prediction and intelligent molecular design make a large contribution to the constant search for, e. g., improved enzyme inhibitors, and new concepts such as that of pharmacophores are being developed."

"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."

"The book closes with chapters on recent progress in technologies: protein engineering to promote crystallization, micro-crystallization, and high-throughput crystallography. Withitsbroadperspective,thebookprovidesastate-of-the-artoverviewonimportant results and techniques that are relevant for protein 3D structure-based drug design."

"This book about protein-protein Interactions as drug targets, targeting the MDM2-p53 protein-protein interaction for new cancer therapeutics, the development of small-molecule IAP antagonists for the treatment of cancer, protein-protein interaction targets to inhibit HIV-1 infection, inhibitors of protein-protein interactions paramyxovirus fusion ? a focus on respiratory syncytial virus, rational design strategies for developing synthetic inhibitors of helical protein interfaces, and the discovery of navitoclax, a Bcl-2 family inhibitor."

"This book the only comprehensive guide of its kind, this groundbreaking two-volume resource provides an overview of the entire sequence of operations involved in drug discovery and development from initial conceptualization to commercialization to clinicians and medical practitioners.Volume 2 : drug development delves into the nitty-gritty details of optimizing the synthetic route, drug manufacturing, outsourcing, and marketing-including drug coloring and delivery methods.Featuring contributions from a world-class team of experts, Drug discovery and development :- Features fascinating case studies, including the discovery and development of erythromycin analogs, Tagamet, and Ultiva (remifentanil)- Discusses the discovery of medications for bacterial infections, Parkinson's disease, psoriasis, peptic ulcers, atopic dermatitis, asthma, and cancer- Includes chapters on combinatorial chemistry, molecular biology-based drug discovery, genomics, and chemogenomics"

"This book contains case studies of the discovery of erythromycin analogs (antibiotics), Tagamet, and Ultiva (remifentanil). Discusses the discovery of agents for the treatment and management of bacterial infections, Parkinson's disease, psoriasis, ulcers and stomach pain, atopic dermatitis, asthma, and cancer. Contains chapters on combinatorial chemistry, molecular biology-based drug discovery, genomics, and chemogenomics.The first volume of this set thoroughly describes conceptualizing a drug, creating a library of candidates for testing, screening those candidates for in vitro and in vivo activity, conducting and analyzing the results of clinical trials, and revising the drug as necessary."

"This timely guide to kinase inhibitor drug development is the first to cover the entire drug pipeline, from target identification to compound development and clinical application. Edited by the pioneers in the field, on the drug development side this ready reference discusses classical medicinal chemistry approaches as well as current chemical genomics strategies. On the clinical side, both current and future therapeutic application areas for kinase inhibitor drugs are addressed, with a strong focus on oncology drugs.Backed by recent clinical experience with first-generation drugs in the battle against various forms of cancer, this is crucial reading for medicinal, pharmaceutical and biochemists, molecular biologists, and oncologists, as well as those working in the pharmaceutical industry."

"Over the past two decades the benefits of label-free biosensor analysis have begun to make an impact in the market, and systems are beginning to be used as mainstream research tools in many drug discovery laboratories. Label-free technologies for drug discovery summarises the latest and emerging developments in label-free detection systems, their underlying technology principles and end-user case studies that reveal the power and limitations of label-free in all areas of drug discovery.Label-free technologies discussed include SPR, NMR, high-throughput mass spectrometry, resonant waveguide plate-based screening, transmitted-light imaging, isothermal titration calorimetry, optical and impedance cell-based assays and other biophysical methods. The technologies are discussed in relation to their use as screening technologies, high-content technologies, hit finding and hit validation strategies, mode of action and ADME/T, access to difficult target classes, cell-based receptor/ligand interactions particularly orphan receptors, and antibody and small molecule affinity and kinetic analysis. Label-Free Technologies For Drug Discovery is an essential guide to this emerging class of tools for researchers in drug discovery and development, particularly high-throughput screening and compound profiling teams, medicinal chemists, structural biologists, assay developers, ADME/T specialists, and others interested in biomolecular interaction analysis."

"This book is about structural, physical, and chemical properties of fluorous compounds, selective fluoroalkylation of organic compounds by tackling the “negative fluorine effect”, synthetic and biological applications of fluorous reagents as phase tags, chemical applications of fluorous reagents and scavengers, methods for the synthesis of peptides and oligonucleotides, fluorous organic hybrid solvents for non-fluorous organic synthesis, fluorous catalysis : from the origin to recent advances, fluorous organocatalysis, thiourea based fluorous organocatalyst, fluoroponytailed crown ethers and quaternary ammonium salts as solid–liquid phase transfer catalysts in organic synthesis, fluorous hydrogenation, fluorous hydrosilylation, fluorous hydroformylation, incorporation of fluorous glycosides to cell membrane and saccharide chain elongation teflon AF materials, ecotoxicology of organofluorous compounds, and biology of fluoro-organic compounds."