Download or read book Modulation of Signal Transduction of Heptahelical Receptors by Other Receptors and G Proteins written by Ain Uustare and published by . This book was released on 2006 with total page 126 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Oligomerization and Allosteric Modulation in G Protein Coupled Receptors written by and published by Academic Press. This book was released on 2012-12-02 with total page 495 pages. Available in PDF, EPUB and Kindle. Book excerpt: In this thematic volume of Progress in Molecular Biology and Translational Science, researchers reflect on recent developments and research surrounding G protein-coupled receptors. The chapters cover a large breadth of research, including GPCR role in stem cell function and pharmacology. Authors explore in-depth research techniques and applications of GPCR usage, covering theory, laboratory approaches, and unique qualities that make GPCRs a crucial tool in microbiological and cancer research. Contributions from leading authorities Informs and updates on all the latest developments in the field
Download or read book Allosteric Modulation of G Protein Coupled Receptors written by Robert Laprairie and published by Academic Press. This book was released on 2022-02-05 with total page 214 pages. Available in PDF, EPUB and Kindle. Book excerpt: Allosteric Modulation of G Protein-Coupled Receptors reviews fundamental information on G protein-coupled receptors (GPCRs) and allosteric modulation, presenting original research in the area and collectively providing a comprehensive description of key issues in GPCR allosteric modulation. The book provides background on core concepts of molecular pharmacology while also introducing the most important advances and studies in the area. It also discusses key methodologies. This is an essential book for researchers and advanced students engaged in pharmacology, toxicology and pharmaceutical sciences training and research. Many of the GPCR-targeted drugs released in the past decade have specifically worked via allosteric mechanisms. Unlike direct orthosteric-acting compounds that occupy a similar receptor site to that of endogenous ligands, allosteric modulators alter GPCR-dependent signaling at a site apart from the endogenous ligand. Recent methodological and analytical advances have greatly improved our ability to understand the signaling mechanisms of GPCRs. We now know that allostery is a common regulatory mechanism for all GPCRs and not – as we once believed – unique to a few receptor subfamilies. Introduces background on core concepts of molecular pharmacology, including statistical analyses, non-linear regression, complex models and GPCR-dependent signal transduction as they relate to allosteric modulation Discusses critical advances and landmark studies, including discoveries in the area of GPCR allosteric modulation, which are reviewed for their importance in positive and negative regulation, protein-protein interactions, and small molecule drug discovery Includes key methodologies used to study allosteric modulation at the in silico, in vitro, and in vivo levels of drug discovery and characterization
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 Signal Transduction by G Protein Coupled Receptors written by Paul H. J. Nederkoorn and published by . This book was released on 2014-01-15 with total page 168 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Molecular Aspects of G Protein coupled Receptors written by Francisco Ciruela and published by Nova Publishers. This book was released on 2008 with total page 328 pages. Available in PDF, EPUB and Kindle. Book excerpt: In the recent years, studies based on two-hybrid screens, proteomic, biochemical and cell biology approaches, have shown that intracellular domains of G protein-coupled receptors (GPCR) or heptaspanning membrane receptors (HSMRs) interact with intracellular proteins. These interactions are the basis of a protein network associated to these receptors which includes scaffolding proteins containing one or several PDZ (post-synaptic density-95, discs large, zona occludens-1) domains, signalling proteins and proteins of the cytoskeleton. The present book is focused on the emerging evidence for interactions of G protein-coupled receptors with scaffolding, cytoskeletal and signalling proteins that will play a role in the targeting, anchoring and functioning of these receptors in the plasma membrane, thus contributing to cell development and plasticity.
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 Mechanisms of Signal Transduction written by Johannes Lukas Bos and published by IOS Press. This book was released on 2000 with total page 298 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book contains overviews of topics that have been discussed. It includes contributions from leading experts in the field on small GTPases, protein kinesis, receptors and transcription factors. A particular focus was the influence of oxygen radicals on signalling processes. It also contains the contributions of scientists early in their career, who have made an excellent contribution to the institute.
Download or read book Receptor Signal Transduction Protocols written by Gary B. Willars and published by Springer Science & Business Media. This book was released on 2008-02-03 with total page 420 pages. Available in PDF, EPUB and Kindle. Book excerpt: This second edition of Receptor Signal Transduction Protocols not only has a new editor, but also a greater focus on G-protein-coupled receptors, their properties per se, and their coupling to immediate downstream binding partners—principally, although not exclusively, the heterotrimeric G-proteins. The new edition combines updates of key chapters from the first edition, as well as a large number of new contributions covering key methodologies that have emerged, or been extended to receptor/G-protein research, in the past 5–6 years. In common with many fields, the range of methods used to assess the first steps in signal transduction are continually expanding and methods that might have been considered too specialized five years ago are now sufficiently routine to be included here. Unlike many research areas, where off-the-shelf kits have made research basically foolproof, signal transduction research still requires considerable expertise, and the methods included here are provided by internationally recognized experts in their fields who have many years of experience using the methods they describe. This not only allows each chapter to impart a clear description of the method, but also to furnish invaluable troubleshooting advice for when things do not go entirely according to plan. Once again we would like to thank the Series Editor, John Walker, for the invitation to compile this second edition, and to express our gratitude to all of the authors who have enthusiastically agreed to provide the uniformly excellent contributions.
Download or read book Functional Selectivity of G Protein Coupled Receptor Ligands written by Kim Neve and published by Springer Science & Business Media. This book was released on 2009-02-27 with total page 290 pages. Available in PDF, EPUB and Kindle. Book excerpt: Functional selectivity refers to the ability of different ligands acting at one receptor subtype to activate multiple signaling pathways in unique combinations; that is, one drug can be an agonist at pathway A and an antagonist or partial agonist at pathway B, and another drug can have the reverse profile. Functional selectivity has profound implications for drug development, for chemical biology, and for the design of experiments to characterize receptor function. In Functional Selectivity of G Protein-Coupled Receptors expert neuroscientists and pharmacologists review the work that demonstrated the existence of functional selectivity, placed it within a theoretical framework, and provided a mechanistic basis for the phenomenon. This exciting, comprehensive, and future-oriented volume includes chapters that focus on theoretical and mechanistic aspects of functional selectivity and that cut across subfamilies of GPCRs. Additional chapters focus on subfamilies of therapeutically relevant receptors where there is considerable evidence of ligand functional selectivity. Accessible and authoritative, Functional Selectivity of G Protein-Coupled Receptors is a valuable educational tool and reference source for students and scientists interested in drug development, chemical biology, and GPCR function.
Download or read book Principles of Endocrinology and Hormone Action written by Antonino Belfiore and published by Springer. This book was released on 2018-02-08 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume provides comprehensive coverage of the current knowledge of the physiology of the endocrine system and hormone synthesis and release, transport, and action at the molecular and cellular levels. It presents essential as well as in-depth information of value to both medical students and specialists in Endocrinology, Gynecology, Pediatrics, and Internal Medicine. Although it is well established that the endocrine system regulates essential functions involved in growth, reproduction, and homeostasis, it is increasingly being recognized that this complex regulatory system comprises not only hormones secreted by the classic endocrine glands but also hormones and regulatory factors produced by many organs, and involves extensive crosstalk with the neural and immune system. At the same time, our knowledge of the molecular basis of hormone action has greatly improved. Understanding this complexity of endocrine physiology is crucial to prevent endocrine disorders, to improve the sensitivity of our diagnostic tools, and to provide the rationale for pharmacological, immunological, or genetic interventions. It is such understanding that this book is designed to foster.
Download or read book G Protein Coupled Receptors written by and published by Academic Press. This book was released on 2016-02-26 with total page 522 pages. Available in PDF, EPUB and Kindle. Book excerpt: G-Protein-Coupled Receptors: Signaling, Trafficking, and Regulation, a new volume in the Methods in Cell Biology series continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers research methods in G-Protein-Coupled Receptors, and includes sections on such topics signaling, trafficking and regulation. Covers the increasingly appreciated cell biology field of G-protein-coupled receptors Includes both established and new technologies Contributed by experts in the field Covers topics such as signaling, trafficking, and regulation
Download or read book G Protein Coupled Receptors Emerging Paradigms in Activation Signaling and Regulation Part B written by and published by Academic Press. This book was released on 2018-05-15 with total page 202 pages. Available in PDF, EPUB and Kindle. Book excerpt: International Review of Cell and Molecular Biology reviews and details current advances in cell and molecular biology. The IRCMB series has a worldwide readership, maintaining a high standard by publishing invited articles on important and timely topics that are authored by prominent cell and molecular biologists. The articles published in IRCMB have a high impact and an average cited half-life of 9 years. This great resource ranks high amongst scientific journals dealing with cell biology. Publishes only invited review articles on selected topics Authored by established and active cell and molecular biologists, and drawn from international sources Offers a wide range of perspectives on specific subjects
Download or read book G Protein Coupled Receptors written by and published by Academic Press. This book was released on 2019-01-05 with total page 332 pages. Available in PDF, EPUB and Kindle. Book excerpt: G-Protein-Coupled Receptors, Part B, 2nd Edition, Volume 149, the latest release in the Methods in Cell Biology series, continues the legacy of this premier serial with quality chapters authored by leaders in the field. This volume covers Optical Approaches for Visualization of Arrestin Binding to Muscarinic Receptors, Luciferase Reporter Assay for Unlocking Ligand-mediated Signaling of GPCRs, Assays to Measure GPCR Dependent Cellular Migration, Characterization of the Frizzled GPCRs, Binding Assays for Bradykinin and Angiotensin Receptors, Detection of Misfolded Rhodopsin Aggregates in Cells, Measuring GPCR Ubiquitination and Trafficking, Culture of Primary Neurons and its Use in Studying GPCR Trafficking, and much more. Covers the increasingly appreciated cell biology field of G-protein-coupled receptors Includes both established and new technologies Contributed by experts in the field
Download or read book Modulation of G Protein coupled Receptor Intracellular Trafficking and Signal Transduction written by Jessica L. Esseltine and published by . This book was released on 2012 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt: The seven transmembrane-spanning G Protein-coupled Receptor (GPCR) super family is the largest family of cell-surface receptors, comprising greater than 650 members. GPCRs represent the primary targets of most therapeutic drugs. Desensitization, endocytosis and recycling are major mechanisms of receptor regulation and intracellular trafficking of GPCRs is linked to the Rab family of small G proteins. In the present study, we examined whether multiple Rab GTPase regulate receptor trafficking through endosomal cellular compartments as a consequence of their direct association with GPCRs. We find that Rab4, Rab7 and Rab11 all bind to the last 10 amino acid residues of the angiotensin II Type 1 (AT1R) carboxyl-terminal tail. We show that the Rab GTPases compete with one another for receptor binding and that Rab4 effectively displaces Rab11 from the receptor. In contrast, Rab11 overexpression does not prevent Rab4 binding to the AT1R. Overexpression of wild-type Rab4, but not Rab11, facilitates AT1R dephosphorylation, and a constitutively active Rab4-Q67L mutant reduces AT1R desensitization and promotes AT1R resensitization. We also find that Rab8, a RabGTPase involved in the regulation of secretory/recycling vesicles, modulation of the actin cytoskeleton and cell polarity, interacts with the carboxyl-terminal tail of metabotropic glutamate receptor 1 (mGluR1a) and attenuates mGluR1a signalling and endocytosis in a protein kinase C-dependent manner. Finally, we have examined several previously uncharacterised but naturally occurring single nucleotide polymorphisms (SNPs) in mGluR1a that have been associated with cancer that may alter mGluR1a signalling. We find that SNPs found within the ligand binding domain of mGluR1a result in both decreased cell surface expression and basal inositol 1,4,5, trisphosphate formation and bias mGluR1a signalling via the ERK1/2 pathway. Additional mGluR1a SNPs localized to the mGluR1a glutamate binding site, intracellular regulatory domains and Homer binding site also result in changes in mGluR1a subcellular localization, signalling and cell morphology. Taken together, these results indicate that GPCR signalling is significantly modulated by the association of intracellular regulatory proteins that can be influenced by receptor structure.
Download or read book Trends in Signal Transduction Research written by Jennifer N. Meyers and published by Nova Publishers. This book was released on 2007 with total page 270 pages. Available in PDF, EPUB and Kindle. Book excerpt: Signal transduction is any process by which a cell converts one kind of signal or stimulus into another. Processes referred to as signal transduction often involve a sequence of biochemical reactions inside the cell, which are carried out by enzymes and linked through second messengers. In many transduction processes, an increasing number of enzymes and other molecules become engaged in the events that proceed from the initial stimulus. Responses of cells to environmental signals, toxins and stressors have profound implications for diverse aspects of human health and disease including development, cystic fibrosis, diabetes, asthma, heart, autoimmune diseases and cancer. The delineation of the signal transduction pathways affected in these and other complex human diseases are likely to present new avenues for therapeutic intervention and understanding of human disease mechanisms.
Download or read book Peptidergic G Protein coupled Receptors written by Pierangelo Geppetti and published by IOS Press. This book was released on 1999 with total page 238 pages. Available in PDF, EPUB and Kindle. Book excerpt: Peptides are a rapidly growing class of mediators whose activity regulates homeostasis as well as pathological processes. Most of the peptide-activated receptors belong to the superfamily of 7 transmembrane domain receptors coupled to G proteins. Peptides of different sizes (from a few to more than 100 aminoacids) activate peptidergic receptors by interacting at specific sites, that often differ from those where antagonists bind. Other receptors are activated by proteases that, by cleaving the receptor extracellular region, unmask a tethered ligand. G protein-coupled receptors for chemokines represent the way of entry of the HIV virus in target cells. The great impact of non peptide agonist/antagonists in current and future medicine reflects these large variety of functions and modes of activation of peptidergic G protein-coupled receptors.
