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Combinatorial Strategies in Biology and Chemistry
Combinatorial chemistry has taken the pharmaceutical industry by storm over the past ten to fifteen years. There has been a massive investment in automation by pharmaceutical companies and a demand for graduates/PhDs with experience and knowledge of combinatorial chemistry. These days the academic education of chemists and biologists is gradually converging, so those entering the pharmaceutical industry need to be not only chemistry graduates but also biologists applying their biological knowledge to chemistry. Many chemists, however, still require experience in biological methods and similarly biologists have not yet realized the power of chemical methods. This book will therefore help ease...
Contemporary Accounts in Drug Discovery and Development
CONTEMPORARY ACCOUNTS IN DRUG DISCOVERY AND DEVELOPMENT A useful guide for medicinal chemists and pharmaceutical scientists Drug discovery is a lengthy and complex process that typically involves identifying an unmet medical need, determining a biological target, chemical library screening to identify a lead, chemical optimization, preclinical studies and clinical trials. This process often takes many years to complete, and relies on practitioners’ knowledge of chemistry and biology, but also—and perhaps more importantly—on experience. Improving the success rate in discovery and development through a thorough knowledge of drug discovery principles and advances in technology is critical...
Adiponectin
First published in 1943, Vitamins and Hormones is the longest-running serial published by Academic Press. Under the capable and qualified editorial leadership of Dr. Gerald Litwack, Vitamins and Hormones continues to publish cutting-edge reviews of interest to endocrinologists, biochemists, nutritionists, pharmacologists, cell biologists and molecular biologists. Others interested in the structure and function of biologically active molecules like hormones and vitamins will, as always, turn to this series for comprehensive reviews by leading contributors to this and related disciplines. - Contributions from leading authorities - Informs and updates on all the latest developments in the field
Neuropeptide Y and Drug Development
Neuropeptide Y (NPY) is a ubiquitous and important messenger in the nervous system, with a wide range of physiological roles. It is involved in the body energy balance and is one of the most potent stimuli of food intake known. NPY also acts to regulate central and peripheral autonomic functions. This book, written by academic and industrial experts in the field, links the most recent basic experimental knowledge about NPY and its receptors with areas of clinical importance. This book will be of interest to those working in all areas of research affected by NPY, such as food intake and energy homeostasis, cardiovascular regulation and G-protein-coupled receptors, as well as those interested in the development of drugs as NPY targets. - The hypothalamic role of NPY and its relationship with eating disorders and diabetes - The sympathetic nervous system role of NPY and its involvement in cardiovascular disorders - Characterization of NPY receptor types and their brain distribution, molecular biology and pharmacology - Development of peptide and non-peptide receptor antagonists
Combinatorial Peptide and Nonpeptide Libraries
With combinatorial chemistry millions of organic compounds can be produced simultaneously, quickly, and in most cases by automated procedures. These compound libraries are a cost-effective resource for the pharmaceutical industry in their search for biologically active lead structures. Furthermore simultaneous parallel synthesis of single peptides and peptide libraries solve the problem of the worldwide increasing demand for peptides. The synthetic methods described here in detail contribute to a forward-looking technology that has a high impact for industrial and academic research. Fast and efficient analytical techniques are essential for using the complicated product mixtures and detecting by-products. Various synthetic approaches and technologies, mass spectrometry, and screening assays are discussed extensively. This book is a must and an indispensible source of information for every researcher in this rapidly developing field, which spans organic synthesis, biochemistry, biotechnology, pharmaceutical, medicinal, and clinical chemistry.
Constitutive Activity in Receptors and Other Proteins, Part B
This volume of Methods in Enzymology covers the current methodology for the detection and assessment of constitutively active proteins. The chapters written by expert authors who are leaders in the field, provide hints and tricks not available in primary research publications.It is extensively referenced, with useful figures and tables throughout the volume. - Expert authors who are leaders in the field - Extensively referenced and useful figures and tables - Provides hints and tricks to facilitate reproduction of methods
NPY Family of Peptides in Neurobiology, Cardiovascular and Metabolic Disorders: from Genes to Therapeutics
The NPY-family of peptides encompasses several groups of neurotransmitters and hormones, which exert diverse biological and pathological actions that bear on all major vital systems. The recognition of the role of NPY in stimulation of food intake has already resulted in discovery of potent and selective NPY receptor Y-5 antagonists which are in clinical development for obesity while NPY Y1 receptors are targeted for cardiovascular indications. Research into the multiple functions of NPY and its receptors in neurological and affective disorders are also actively pursued. This book is a unique compilation of the most recent breakthroughs in NPY/PYY neurobiology, cardiovascular and metabolic disorders, written by internationally renowned experts with the objective to synthesize leading concepts and data in support for translational medicine.
Neuropeptide GPCRs in neuroendocrinology
The human genome encompasses ˜ 860 G protein-coupled receptors (GPCRs) including 374 non-chemosensory GPCRs. Half of these latter GPCRs recognize (neuro)peptides as natural ligands. GPCRs thus play a pivotal role in neuroendocrine communication. In particular, GPCRs are involved in the neuroendocrine control of feeding behavior, reproduction, growth, hydromineral homeostasis and stress response. GPCRs are also major drug targets and hence possess a strong potential for the development of innovative pharmaceuticals. The aim of this Research Topic was to assemble a series of review articles and original research papers on neuropeptide GPCRs and their ligands that would illustrate the different facets of the studies currently conducted in this domain.
Synthesis and Analytics of Rigidified Peptide Architectures. Neuropeptide Y Dipeptide Scan Ring-Chain-Equilibria of Iminopeptides Thiazole Amino Acids for Thiopeptide Antibiotics
The architectures (three-dimensional shapes) of peptides determine their respective biological functions. Therefore, the correct alignment of functionalities in a structure by constraining the flexibility is a key process in evolution as well as in medicinal chemistry in order to increase binding affinity and selectivity. The rigidification of a peptide chain can have local effects (incorporation of the amino acid proline) or it can globally restrain flexibility (macrocyclization). Furthermore, the combination of both strategies has given rise to complex antibiotics with highly optimized modes of action. This work approaches these principles in three topics and for different purposes. The fi...
