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Pharmacology
The history of pharmacology travels together to history of scientific method and the latest frontiers of pharmacology open a new world in the search of drugs. New technologies and continuing progress in the field of pharmacology has also changed radically the way of designing a new drug. In fact, modern drug discovery is based on deep knowledge of the disease and of both cellular and molecular mechanisms involved in its development. The purpose of this book was to give a new idea from the beginning of the pharmacology, starting from pharmacodynamic and reaching the new field of pharmacogenetic and ethnopharmacology.
Structure and Function of GPCRs
This book introduces readers to the latest advances in G protein-coupled receptor (GPCR) biology. It reviews our current understanding of the structural basis of ligand binding and allosteric mechanisms, following a decade of technological breakthroughs. Several examples of structure-based drug discovery are presented, together with the future challenges involved in designing better drugs that target GPCRs. In turn, the book illustrates the important concept of GPCR biased signaling in physiological contexts, and presents fluorescent- and light-based methodologies frequently used to measure GPCR signaling or to trace their dynamics in cells upon ligand activation. Taken together, the chapters provide an essential overview and toolkit for new scientific investigators who plan to develop GPCR projects. All chapters were written by experts in their respective fields, and share valuable insights and powerful methodologies for the GPCR field.
Fluorescence-Based Biosensors
One of the major challenges of modern biology and medicine consists in finding means to visualize biomolecules in their natural environment with the greatest level of accuracy, so as to gain insight into their properties and behaviour in a physiological and pathological setting. This has been achieved thanks to the design of novel imaging agents, in particular to fluorescent biosensors. Fluorescence Biosensors comprise a large set of tools which are useful for fundamental purposes as well as for applications in biomedicine, drug discovery and biotechnology. These tools have been designed and engineered thanks to the combined efforts of chemists and biologists over the last decade, and develo...
Ligand Design for G Protein-coupled Receptors
G protein-coupled receptors (GPCRs) are one of the most important target classes in pharmacology and are the target of many blockbuster drugs. Yet only with the recent elucidation of the rhodopsin structure have these receptors become amenable to a rational drug design. Based on recent examples from academia and the pharmaceutical industry, this book demonstrates how to apply the whole range of bioinformatics, chemoinformatics and molecular modeling tools to the rational design of novel drugs targeting GPCRs. Essential reading for medicinal chemists and drug designers working with this largest class of drug targets in the human genome.
G Protein-coupled Receptors
G protein-coupled receptors (GPCRs) are the largest family of cell-surface receptors, with more than 800 members identified thus far in the human genome. The book lies between the fields of chemical biology, molecular pharmacology, and medicinal chemistry.
mGLU Receptors
Metabotropic glutamate receptors (mGluRs) are members of the group C family of G-protein-coupled receptors. Eight different mGlu subtypes have been identified and classified into three groups based on amino acid sequence similarity, agonist pharmacology, and the signal transduction pathways to which they couple. They perform a variety of functions in the central and peripheral nervous systems, being involved in learning, memory, anxiety, and the perception of pain. They are found in pre- and postsynaptic neurons in synapses of the hippocampus, cerebellum, and cerebral cortex, as well as other parts of the bain and peripheral tissues. This volume will focus on the latest research in the role of Group I mGluRs in health and disease.
G Protein-Coupled Receptors
Provides a comprehensive overview of recent discoveries and current understandings of G protein-coupled receptors (GPCRs). Recent advances include the first mammalian non-rhodopsin GPCR structures and reconstitution of purified GPCRs into membrane discs for defined studies, novel signaling features including oligomerization, and advances in understanding the complex ligand pharmacology and physiology of GPCRs, in new assay technologies and drug targeting. The authors take time to detail the importance of the pathophysiological function and drug targeting of GPCRs, specifically β-adrenoceptors in cardiovascular and respiratory diseases, metabotropic glutamate receptors in CNS disorders, S1P receptors in the immune system, and Wnt/Frizzled receptors in osteoporosis. This book will be invaluable to researchers and graduate students in academia and industry who are interested in the GPCR field.
GABAB Receptor
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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.
