Download or read book Evolutionary Analysis of G protein Coupled Receptor Structure and Function written by Srinivasan Madabushi and published by . This book was released on 2005 with total page 422 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book G Protein Coupled Receptors written by Jesus Giraldo and published by Royal Society of Chemistry. This book was released on 2011-08-16 with total page 549 pages. Available in PDF, EPUB and Kindle. Book excerpt: 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. They regulate the function of most cells in the body, and represent approximately 3% of the genes in the human genome. These receptors respond to a wide variety of structurally diverse ligands, ranging from small molecules, such as biogenic amines, nucleotides and ions, to lipids, peptides, proteins, and even light. Ligands (agonists and antagonists) acting on GPCRs are important in the treatment of numerous diseases, including cardiovascular and mental disorders, retinal degeneration, cancer, and AIDS. It is estimated that these receptors represent about one third of the actual identified targets of clinically used drugs. The determination of rhodopsin crystal structure and, more recently, of opsin, 1 and 2 adrenergic and A2A adenosine receptors provides both academia and industry with extremely valuable data for a better understanding of the molecular determinants of receptor function and a more reliable rationale for drug design. GPCR structure and function constitutes a hot topic. The book, which lies between the fields of chemical biology, molecular pharmacology and medicinal chemistry, is divided into three parts. The first part considers what receptor structures tell us about the mechanism of receptor activation. Part II focuses on receptor function. It discusses what the data from biophysical and mutational studies, and the analysis of the interactions of the receptor with ligands and regulator proteins, tell us about the process of signal transduction. The final part, on modelling and simulation, details new insights on the link between structure and mechanism and their implications in drug design.
Download or read book Molecular Evolution of Pyroglutamylated RFamide Peptide and Orphan G Protein Coupled Receptor written by Rigers Bakiu and published by GRIN Verlag. This book was released on 2016-12-13 with total page 114 pages. Available in PDF, EPUB and Kindle. Book excerpt: Document from the year 2016 in the subject Biology - Evolution, grade: -, Agricultural University of Tirana, language: English, abstract: G protein-coupled receptors (GPCRs) are members of a large protein family that share common structural motifs, including seven transmembrane helices, and play pivotal roles in cell-to-cell communications and in the regulation of cell functions. GPR103 is an orphan GPCR that shows similarities with orexin, neuropeptide FF, and cholecystokinin receptors. In humans, 26RFa/QRFP has been found to be an endogenous ligand for the orphan receptor, GPR103 and it is one of the RFamide peptides, which have been shown to exert important neuroendocrine, behavioural, sensory and autonomic functions. All the information we have till know couldn’ be available if we didn’t know the evolution of this important proteins and the relative interactions, which were discovered recently to be important for the regulation of locomotor activity, sleep and these neuropeptides and receptors exert neuroprotective effect in Alzheimer’s Disease. Anyway, there is a long way to be walked on, because there is a need of additional information, while studing the molecular evolution of these proteins and peptides. What is the Molecular Evolution? In the First chapter the readers can find all about this branch of science and the problems this branch had overcomed in order to bring to the scientific community the molecularisation of the evolution concepts. In the following chapter to the readers is presented a descriptive overview of G-proteins and G-protein coupled receptor. In the other chapters it is also presented 26RFA/QRFP and pyroglutamylated RFamide peptide receptor (QRFPR) molecular evolution, where it is described the molecular phylogeny and the functional implication. It is even shown the unique study regarding the presence on natural selection (positive or negative selection) during the evolution of QRFPRs in mammals and fish species. In the end of the book are shown the recent important finding regarding the function and the role of QRFP and its receptor, together with the experimental approach applied to zebrafish and rodents. Anyway, it is imperative to mention that all the available knowledge from experiments to these animals can be useful for the curation of disorders and other deseases like Alzheimer’s Disease, only if we could understand well their molecular evolution.
Download or read book Structure Function Analysis of G Protein Coupled Receptors written by Jürgen Wess and published by Wiley-Liss. This book was released on 1999-06-15 with total page 448 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume provides a concise, up-to-date presentation of methods (including molecular, genetic, biochemical, and biophysical) which have been used successfully in studying the structure and function of GPCRs. With contributions from international leaders in the field, the editor provides overviews of various techniques, followed by in-depth descriptions of basic procedures and discussions of critical experimental parameters. Structure-Function Analysis of G Protein-Coupled Receptors is an invaluable reference for receptor biochemists and biological chemists, pharmacologists, and neuroscientists as well as molecular biologists, cell biologists, and structural biologists worldwide.
Download or read book The Structure of G Protein coupled Receptors in the Light of Evolution written by Holger Römpler and published by . This book was released on 2006 with total page 276 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book G Protein Coupled Receptors written by Gabriel Berstein and published by CRC Press. This book was released on 2019-04-24 with total page 424 pages. Available in PDF, EPUB and Kindle. Book excerpt: Covering recently developed methods in membrane-bound receptors, this book emphasizes receptor structure and function, knowledge of which is essential to the study of signal transduction. G Protein-Coupled Receptors has culled contributors from domestic and international sources, providing a broad base of knowledge. Some topics covered are the r
Download or read book G Protein Coupled Receptors written by Tatsuya Haga and published by CRC Press. This book was released on 2005-08-04 with total page 336 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book provides a broad base of knowledge of G-protein-coupled receptors. Useful at both the university and industrial levels, this book is of particular interest to those who are developing therapeutic approaches to diseases using drugs that influence receptor activation.
Download or read book G Protein Coupled Receptor Genetics written by Craig W. Stevens and published by Humana. This book was released on 2016-09-17 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: G Protein‐Coupled Receptor Genetics: Research and Methods in the Post‐Genomic Era features practical techniques inspired by the fast moving GPCR field. From powerful bioinformatic tools tracing the evolution of GPCRs, to methods for the cellular transfection of engineered viruses containing GPCRs, to optogenetic techniques that produce light-activated GPCRs in live mice, what was once science fiction is now science fact. This detailed volume includes sections covering genetic mechanisms, a genetic toolbox for GPCR discovery, as well as genetic aspects of G protein-coupled receptors in health and medicine. Written for the Methods in Pharmacology and Toxicology series, this book contains the kind of key implementation advice that encourages successful results in the lab. Authoritative and easy to use, G Protein‐Coupled Receptor Genetics: Research and Methods in the Post‐Genomic Era serves as an ideal guide for researchers aiming to continue our progress in this dynamic and exciting area of study.
Download or read book Molecular Dissection of G protein Coupled Receptor Signaling and Oligomerization written by Michael J. Rizzo and published by . This book was released on 2019 with total page 132 pages. Available in PDF, EPUB and Kindle. Book excerpt: G protein coupled receptors (GPCRs) are a superfamily of transmembrane proteins responsible for transducing extracellular stimuli into intracellular responses. GPCRs are indispensable to a vast variety of distinct physiologies and behaviors and represent approximately 50% of all human drug targets. However, considerable debate exists as to the structural basis for GPCR activation, with a classical monomeric (two state model) conflicting with a growing number of reports indicating that these receptors form higher order functional oligomers. These receptor-receptor interactions can impact receptor trafficking, ligand sensitivity, desensitization, and strength of effector response. As such, an understanding of GPCR oligomerization is indispensable to our overall understanding of receptor dynamics. Additionally, the specific molecular events underlying receptor activation and signaling remain incompletely understood. Since the initial discovery of the GPCR receptor family, a number of conserved amino acid motifs have been identified that have been shown to play specific and critical roles in GPCR activation, intracellular G-protein coupling, and receptor desensitization. Still, many of these motifs remain incompletely described, with some motifs having only been evaluated in a small subset of receptors, and experimental evidence suggests that in some cases, these conserved motifs may have divergent roles in specific receptor subfamilies. As such, the conservation of these motifs throughout GPCR evolution represents and interesting and unresolved aspect of GPCR function. The goal of this research was two-fold. In one study, I utilized a combination of bioinformatics, site-directed mutagenesis, signaling assays, and fluorescent microscopy techniques to evaluate the functional role and evolutionary conservation of a specific amino acid motif, the WxFG motif, which is present in approximately 90% of all Class A receptors. Our investigation showed that, in contrast to previous studies of this motif, disruption of the WxFG motif results in trafficking defects across a range of GPCRs representing multiple Class A GPCR subfamilies, regardless of taxa. A second study evaluated whether Drosophila GPCRs, specifically a subset of neuropeptide receptors, assembled as higher order structures at the plasma membrane. While there have been many receptors shown to assemble as dimers or oligomers at the plasma membrane since the phenomenon was first recognized over two decades ago, the majority of these studies focused on vertebrate GPCRs, and the question of whether invertebrate GPCRs show similar phenotypes has been poorly evaluated, and to date, no Drosophila GPCR has been empirically demonstrated to assemble as a dimer. To gain a deeper understanding of GPCR molecular assembly, I evaluated multiple Drosophila receptors utilizing FRET microscopy to determine both the prevalence of GPCR dimerization among Drosophila neuropeptide receptors, and determine whether dimerization is conserved across taxa in specific receptor subfamilies. This investigation showed that all Drosophila GPCRs tested were able to assemble as homodimers when expressed in a heterologous expression system, suggesting that not only do Drosophila GPCRs likely assemble as higher order structures at the plasma membrane, but also that the phenomenon of receptor dimerization is an ancient property of the receptor superfamily that has been conserved throughout GPCR evolution. Taken together, these investigations further our understanding of the molecular events underlying GPCR signaling, and suggest that many aspects of receptor function are not taxa specific, and are likely fundamental features of GPCR function that have been conserved throughout the evolution of this receptor superfamily.
Download or read book Thermodynamics and Kinetics of Drug Binding written by György Keserü and published by John Wiley & Sons. This book was released on 2015-08-17 with total page 360 pages. Available in PDF, EPUB and Kindle. Book excerpt: This practical reference for medicinal and pharmaceutical chemists combines the theoretical background with modern methods as well as applications from recent lead finding and optimization projects. Divided into two parts on the thermodynamics and kinetics of drug-receptor interaction, the text provides the conceptual and methodological basis for characterizing binding mechanisms for drugs and other bioactive molecules. It covers all currently used methods, from experimental approaches, such as ITC or SPR, right up to the latest computational methods. Case studies of real-life lead or drug development projects are also included so readers can apply the methods learned to their own projects. Finally, the benefits of a thorough binding mode analysis for any drug development project are summarized in an outlook chapter written by the editors.
Download or read book Adhesion GPCRs written by Simon Yona and published by Springer. This book was released on 2011-07-12 with total page 199 pages. Available in PDF, EPUB and Kindle. Book excerpt: Upon completion of the human genome project over 800 G protein-coupled receptor 1 (GPCR) genes, subdivided into five categories, were identified. These receptors sense a diverse array of stimuli, including peptides, ions, lipid analogues, light and odour, in a discriminating fashion. Subsequently, they transduce a signal from the ligand–receptor complex into numerous cellular responses. The importance of GPCRs is further reflected in the fact that they constitute the most common target for therapeutic drugs across a 2 wide range of human disorders. Phylogenetic analysis of GPCRs produced the GRAFS classification system, which subdivides GPCRs into five discrete families: glutamate, rhodopsin, adhesion, frizzled/taste2 and secretin receptors. The adhesion-GPCR family 2 can be further subdivided into eight groups. The field of adhesion-GPCR biology has indeed become large enough to require a volume dedicated solely to this field. The contributors to this book have made a courageous effort to address the key concepts of adhesion-GPCR biology, including the evolution and biochemistry of adhesion-GPCRs; there are extensive discussions on the functional nature of these receptors during development, the immune response and tumourgenesis. Finally, there are chapters dedicated to adhesion-GPCR signalling, an area of intense investigation.
Download or read book Structural Biology in Drug Discovery written by Jean-Paul Renaud and published by John Wiley & Sons. This book was released on 2020-01-09 with total page 1367 pages. Available in PDF, EPUB and Kindle. Book excerpt: With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins
Download or read book Amine G protein Coupled Receptors in Model Vertebrate Organisms written by Kanwal Naeem and published by . This book was released on 2012 with total page 202 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book G Protein Coupled Receptors in Drug Discovery written by Marta Filizola and published by Humana. This book was released on 2015-08-11 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This detailed volume provides an overview of recent techniques employed in the field of G protein-coupled receptors (GPCRs) to screen for new drugs and to derive information about their receptor structure, dynamics, and function for the purpose of developing improved therapeutics. Owing to remarkable recent advances in the structural, biophysical and biochemical analyses of these receptors, as well as a growing body of evidence hinting at the possible relevance of allosteric modulators, biased agonists and oligomer-selective ligands as improved therapeutic agents, drug discovery for GPCRs has recently taken a completely new direction. For this book, expert contributors have shared their protocols and views on the impact of these methodologies on modern drug discovery. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols and tips on troubleshooting and avoiding known pitfalls. Practical and fully updated, G Protein-Coupled Receptors in Drug Discovery: Methods and Protocols, Second Edition serves as an ideal guide for a diverse audience from structural and molecular biologists to pharmacologists and drug designers who wish to explore this extensive class of key drug targets.
Download or read book G Protein Coupled Receptor Signaling written by Mario Tiberi and published by Humana Press. This book was released on 2019-03-01 with total page 406 pages. Available in PDF, EPUB and Kindle. Book excerpt: This detailed volume assembles comprehensive protocols to assist with the study of structural, molecular, cell biological, and in vivo facets of GPCRs, and to enable the development of experimental tools for screening novel GPCR drugs. Sections explore the tweaking of ligands, bioluminescence and FRET approaches, specific GPCR signaling properties, as well as visualization of subcellular compartmentalization. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials and reagents, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and practical, G Protein-Coupled Receptor Signaling: Methods and Protocols serves as an ideal reference for life scientists working in a variety of research fields including molecular pharmacology, cell and developmental biology, brain behavior and physiology, drug development and screening. Chapter 4 is available open access under a CC BY 4.0 license via link.springer.com.
Download or read book Neuromorphic Olfaction written by Krishna C. Persaud and published by CRC Press. This book was released on 2016-04-19 with total page 237 pages. Available in PDF, EPUB and Kindle. Book excerpt: Many advances have been made in the last decade in the understanding of the computational principles underlying olfactory system functioning. Neuromorphic Olfaction is a collaboration among European researchers who, through NEUROCHEM (Fp7-Grant Agreement Number 216916)-a challenging and innovative European-funded project-introduce novel computing p
Download or read book Crystallization of Membrane Proteins written by Hartmut Michel and published by CRC Press. This book was released on 2018-01-18 with total page 343 pages. Available in PDF, EPUB and Kindle. Book excerpt: The precise knowledge of the structure of biological macromolecules forms the basis of understanding their function and their mechanism of action. It also lays the foundation for rational protein and drug design. The only method to obtain this knowledge is still crystallography. At present, the structures of about 400 proteins are known at or nearly at atomic proteins. However, only two of them are membrane proteins or complexes of the membrane proteins. The reasons for the difference is not the crystals of membrane proteins resists forming special problems when being analysed. The reason is that the membrane proteins resist into forming into well-ordered crystals. The intention of this book is to help to produce well-ordered crystals proteins and to provide guidelines, it is aimed at both biochemists and protein crystallographer‘s.
