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Author : Keng-Li Lan
Publisher :
ISBN 13 :
Total Pages : 442 pages
Book Rating : 4.3/5 (91 download)
Download or read book Mechanism and Specificity of G Protein Regulation by RGS Proteins written by Keng-Li Lan and published by . This book was released on 1999 with total page 442 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Stanley Michinobu Kanai
Publisher :
ISBN 13 :
Total Pages : 114 pages
Book Rating : 4.:/5 (993 download)
Download or read book Mechanisms of G Protein Regulation by RGS Proteins and Small Molecule Inhibitors written by Stanley Michinobu Kanai and published by . This book was released on 2017 with total page 114 pages. Available in PDF, EPUB and Kindle. Book excerpt: G protein coupled receptors transduce diverse extracellular signals like hormones, neurotransmitters, and photons to specific cellular responses through heterotrimeric G proteins. G proteins activate numerous effectors and signal transduction pathways, and therefore the regulation of G proteins is crucial for faithful propagation of specific cellular and physiological responses. A better understanding of the mechanisms that regulate G proteins should provide new insight into signaling pathways that govern healthy and disease states, and also provide opportunities for discovery of novel therapeutic targets.Regulator of G protein signaling (RGS) proteins are crucial regulators of G proteins, for they control amplitude and duration of G protein signaling responses. RGS2 is particularly important because it is associated with many physiological and disease processes. A key concept that has emerged is that physiological and disease processes are extremely sensitive to even modest changes in RGS2 expression levels. The goals of this dissertation were to investigate the mechanism that controls RGS2 levels and to determine how dynamic RGS2 levels affect GPCR signaling. The particular focus was on the ubiquitin proteasome pathway (UPP), which is one of the key mechanisms that control RGS2 expression levels. Rather than looking for components of the UPP that recognize and degrade RGS2, a comprehensive analysis was performed on the RGS2 N-terminal domain to identify signals required for degradation. This analysis revealed a novel bipartite hydrophobic motif that is required for degradation. Intriguingly, deletion of these hydrophobic motifs did not abrogate binding with E3 ligases associated with RGS2 degradation, suggesting additional mechanisms are involved. The effect of UPP mediated degradation of RGS2 on regulation of GPCR signaling was also explored. Using a cell based, kinetically resolved, GPCR reporter assay, it was demonstrated that proteasome degradation of RGS2 dynamically regulates GPCR signaling, influencing both agonist efficacy and the rate of receptor resensitization.G protein signaling pathways also can be modulated by small molecule inhibitors. YM-254890 and FR900359 are a class of small molecule inhibitors for G proteins that are selective and cell permeable. They are promising research tools and leads for therapeutic agents, but the exact molecular mechanism of action of these inhibitors is not known. The second part of the dissertation describes early stages of a study that aims to elucidate the mechanism of action of YM and FR. Preliminary results that support an allosteric model of inhibition are reported, followed by a discussion of future work that will further test this model.
Author : Stephen Sprang
Publisher : Academic Press
ISBN 13 : 0080552692
Total Pages : 262 pages
Book Rating : 4.0/5 (85 download)
Download or read book Mechanisms and Pathways of Heterotrimeric G Protein Signaling written by Stephen Sprang and published by Academic Press. This book was released on 2007-10-01 with total page 262 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume in the Advances in Protein Chemistry series features cutting-edge articles on topics in protein chemistry. This volume includes chapters on the structural basis of effector regulation and signal termination in heterotrimeric Gƒуnƒnproteins; How do receptors activate G proteins; Some mechanistic insights into GPCR activation from detergent solubilized ternary complexes on beads; Activation of G protein coupled receptors; Kinetic analysis of g-protein-coupled receptor signaling using fluorescence resonance energy transfer in living cells; Regulation of Rho Guanine Nucleotide Exchange Factors (RhoGEFs) by G proteins.
Author : Richard R. Neubig
Publisher : Academic Press
ISBN 13 : 0123859522
Total Pages : 408 pages
Book Rating : 4.1/5 (238 download)
Download or read book Pharmacology of G Protein Coupled Receptors written by Richard R. Neubig and published by Academic Press. This book was released on 2011-09-19 with total page 408 pages. Available in PDF, EPUB and Kindle. Book excerpt: G protein coupled receptors remain the most important class of therapeutic targets in medicine. In the last 5 years, tremendous advances have been made in our understanding of the structure and mechanism of this critical family of drug targets. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors. It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones. In addition, emerging drug targets such as receptor families for fatty acids, carboxylic acids, lipid mediators, etc. are included. Final chapters cover novel mechanisms of signal regulation through PDZ domains and RGS proteins. This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists. The present volume explores the modern experimental and conceptual framework for drug discovery for G protein coupled receptors It explores advances in structure determination and structure-based drug design as well as new concepts of allosteric modulation, functional selectivity/biased agonism, and pharmacological chaperones This volume will bring an up-to-date perspective on the G protein coupled receptor field to both academic and industry scientists
Author :
Publisher : Elsevier
ISBN 13 : 0080497268
Total Pages : 475 pages
Book Rating : 4.0/5 (84 download)
Download or read book Regulators of G Protein Signaling, Part A written by and published by Elsevier. This book was released on 2004-11-25 with total page 475 pages. Available in PDF, EPUB and Kindle. Book excerpt: Regulators of G Protein Signaling, Part A is an in-depth treatment of G-Protein Signaling, and will cover general methods of analysis of RGS protein analysis, including Expression and post-translational modification, Assays of GAP activity and allosteric control, Electrophysiological methods and RGS-insensitive Ga subunits, Mouse models of RGS protein action, Methods of RGS protein inhibition, and G-protein regulators of model organisms. - Table of Contents - Expression and post-translational modification - Assays of GAP activity and allosteric control - Electrophysiological methods and RGS-insenstitive Ga subunits - Mouse Models of RGS protein action - Methods of RGS protein inhibition - G-protein regulators of model organisms
Author : Alan V. Smrcka
Publisher : Springer Science & Business Media
ISBN 13 : 1592594301
Total Pages : 246 pages
Book Rating : 4.5/5 (925 download)
Download or read book G Protein Signaling written by Alan V. Smrcka and published by Springer Science & Business Media. This book was released on 2008-02-02 with total page 246 pages. Available in PDF, EPUB and Kindle. Book excerpt: Alan V. Smrcka presents a collection of cutting-edge methods for investigating G protein signaling from a variety of perspectives ranging from in vitro biochemistry to whole animal studies. Among the readily reproducible techniques presented are those for the purification of G proteins and effectors enzymes, assays of these purified G proteins and effector enzymes, and for the study of G proteins interactions with effectors in intact cells. Additional methods are provided for assaying G protein coupled receptor structure, function, and localization, and for studying the physiological roles for endogenous G proteins.
Author :
Publisher : Academic Press
ISBN 13 : 0080911978
Total Pages : 389 pages
Book Rating : 4.0/5 (89 download)
Download or read book Molecular Biology of RGS Proteins written by and published by Academic Press. This book was released on 2009-07-21 with total page 389 pages. Available in PDF, EPUB and Kindle. Book excerpt: Molecular Biology of RGS Proteins, a volume of Progress in Molecular Biology and Translational Science, will include historical discussion of RGS proteins, the role of RGS proteins in addiction, depression and Parkinson's disease and the biology and functional regulation of RGS9 isoforms. This publication further discusses RGS proteins in cellular signaling, protein control in lymphocyte function, and alternative splicing of RGS transcripts and nuclear RGS proteins, offering the latest in research of RGS proteins.
Author :
Publisher : Academic Press
ISBN 13 : 0128029544
Total Pages : 243 pages
Book Rating : 4.1/5 (28 download)
Download or read book RGS Protein Physiology and Pathophysiology written by and published by Academic Press. This book was released on 2015-06-23 with total page 243 pages. Available in PDF, EPUB and Kindle. Book excerpt: RGS Protein Physiology and Pathophysiology describes the current, state-of-the-art research occurring in the laboratories of leaders in the RGS protein field that utilize genetic mouse models to interrogate the function of RGS proteins in vivo. Each chapter describes the elucidated role of a specific RGS protein or family of RGS proteins in normal physiology and/or disease with particular emphasis on how these discoveries inform healthcare and drug discovery. The work is a timely reference as drugs targeting G protein coupled receptors represent 40% of currently marketed therapeutics. - Brings together information on the current state of the RGS protein field - Contains comprehensive descriptions of the known pathophysiological and physiological functions of RGS proteins, the first such undertaking - Gives particular emphasis to the ways these discoveries inform healthcare and drug discovery
Author : Steven Gu
Publisher :
ISBN 13 : 9780494609712
Total Pages : 452 pages
Book Rating : 4.6/5 (97 download)
Download or read book The Functional Characterization of Two Regulators of G-protein Signaling Proteins Abundantly Expressed in Vascular Smooth Muscle Cells written by Steven Gu and published by . This book was released on 2009 with total page 452 pages. Available in PDF, EPUB and Kindle. Book excerpt: Precise regulation of heterotrimeric G-protein signaling is important for maintaining proper cardiovascular system function. Indeed, G-protein signaling is frequently upregulated during cardiovascular disease suggesting that identifying mechanisms for inhibiting G-protein signaling may be an effective therapeutic strategy for the treatment and prevention of disease. The work presented in this thesis is directed at two RGS proteins, RGS2 and RGS5, the two highest expressing RGS proteins in VSMCs. Despite the large number of studies published on them, there is still much to be learned about the specific G-protein pathways that each RGS protein controls. Using genetic and molecular models, we set out to identify novel regulatory pathways controlling RGS2 and RGS5 function. We hypothesize that characterizing the determinants and regulation of RGS protein function will provide a better understanding of the signaling that occurs within VSMCs under both physiologic and pathophysiologic conditions.Finally, our last study focuses on the function and regulation of RGS5, the single highest expressing RGS protein in VSMCs. We show that the regulation of RGS5 is dependent, similar to other VSMC-specific genes, on the activity of SRF and myocardin. However, interestingly, RGS5 expression is further controlled by the extent of DNA methylation that occurs in its proximal promoter. We show that this is an important regulator of RGS5 expression both in development as well as during disease, specifically in-stent restenosis.Our work presented in the first three studies of this thesis, describes novel regulatory pathways that are involved in regulating RGS2 protein function. We describe the production of RGS2 protein isoforms that are the result of alternative translational start site usage. Interestingly, the expression pattern of these proteins is controlled by the signaling status of the cell. In the second two studies, we identify a functional consequence of RGS2-interaction with the plasma membrane. We show that this is dependent on the interaction between the amphipathic alpha-helix and anionic phospholipids present in the plasma membrane. We further show that disruptions in this interaction, as occurs in the human population, can lead to reduced RGS2 function and thus potentially hypertension.
Author : Lakshmi A. Devi
Publisher : Springer Science & Business Media
ISBN 13 : 1592599192
Total Pages : 414 pages
Book Rating : 4.5/5 (925 download)
Download or read book The G Protein-Coupled Receptors Handbook written by Lakshmi A. Devi and published by Springer Science & Business Media. This book was released on 2008-03-01 with total page 414 pages. Available in PDF, EPUB and Kindle. Book excerpt: A comprehensive survey of the many recent advances in the field of G protein-coupled receptors (GPCR). The authors describe the current knowledge of GPCR receptor structure and function, the different mechanisms involved in the regulation of GPCR function, and the role of pharmacological chaperones in GPCR folding and maturation. They also present new findings about how GPCR dimerization/oligomerization modifies the properties of individual receptors and show how recent developments are leading to significant advances in drug discovery, such as the detection of ligands for orphan GPCRs. Also discussed are the most recent developments that could lead to new drug discoveries: the role of GPCRs in mediating pain, the development of receptor-type selective drugs based on the structural plasticity of receptor activation, and the identification of natural ligands of orphan GPCRs (deorphanization) as possible drug targets.
Author :
Publisher : Elsevier
ISBN 13 : 0323994318
Total Pages : 230 pages
Book Rating : 4.3/5 (239 download)
Download or read book G Protein-Coupled Receptors - Part A written by and published by Elsevier. This book was released on 2022-12 with total page 230 pages. Available in PDF, EPUB and Kindle. Book excerpt: G Protein-Coupled Receptors, Part A, Volume 193 in the Progress in Molecular Biology and Translational Science series, highlights new advances in the field. G protein-coupled receptors (GPCRs) represent the largest class of cell surface proteins with an intricate involvement of nearly every physiological process in our body. Approximately, one third of the clinically prescribed medicines target GPCRs and the quest to improve the exiting GPCR-targeting therapeutics continues. These two volumes are focused on activation, signaling and regulation of GPCRs with specific examples of receptor systems and cellular processes. Covers a broad range of topics related to GPCR activation and signaling Covers several receptor systems with an emphasis on emerging paradigms Covers different processes and model systems with a focus on GPCRs
Author :
Publisher : Academic Press
ISBN 13 : 0128124040
Total Pages : 400 pages
Book Rating : 4.1/5 (281 download)
Download or read book G Protein-Coupled Receptors in Immune Response and Regulation written by and published by Academic Press. This book was released on 2017-09-23 with total page 400 pages. Available in PDF, EPUB and Kindle. Book excerpt: G Protein-Coupled Receptors in Immune Response and Regulation, Volume 136 presents emerging concepts related to the role of GPCRs in immune response and regulation. Users will find updated chapters on a variety of topics, including Beta-adrenergic signaling in the onset and progression of asthma, the Emerging roles of Regulators of G protein signaling (RGS) proteins in the immune system, information on Kinin receptors in immune response and pathogenic infections, and sections on GPCR signaling in C. elegans and its implications in immune response, GPCR Kinases in Inflammatory response and signaling, and GRK2 in Inflammation: Regulation of T cell receptors and IgE signaling. Chapters in this book discuss not only the well-known aspects of GPCR signaling in immunology, but also presents many emerging paradigms that have not yet been reported in classical textbooks. Each chapter presents a forward-looking discussion, providing a glimpse of the tremendous potential associated with the specific receptor systems discussed. Brings together contributions from leading experts in the area of GPCR biology Discusses current paradigms and the future potential of understanding GPCR signaling in immune response and regulation Presents the first of its kind book to focus on specific GPCR systems in various aspects of immunology, all brought together in one volume
Author : Sangdun Choi
Publisher : Springer
ISBN 13 : 9781493968008
Total Pages : 6330 pages
Book Rating : 4.9/5 (68 download)
Download or read book Encyclopedia of Signaling Molecules written by Sangdun Choi and published by Springer. This book was released on 2017-12-15 with total page 6330 pages. Available in PDF, EPUB and Kindle. Book excerpt: The second edition of this encyclopedia presents over 400 biologically important signaling molecules and the content is built on the core concepts of their functions along with early findings written by some of the world’s foremost experts. The molecules are described by recognized leaders in each molecule. The interactions of these single molecules in signal transduction networks will also be explored. This encyclopedia marks a new era in overview of current cellular signaling molecules for the specialist and the interested non-specialist alike. Currently, there are more than 30,000 genes in human genome. However, not all the proteins encoded by these genes work equally in order to maintain homeostasis. Understanding the important signaling molecules as completely as possible will significantly improve our research-based teaching and scientific capabilities.
Author : Vincent Shaw
Publisher :
ISBN 13 : 9781088395738
Total Pages : 201 pages
Book Rating : 4.3/5 (957 download)
Download or read book Understanding Specificity of Small Molecule Inhibitors of Regulators of G-protein Signaling (rgs) Proteins written by Vincent Shaw and published by . This book was released on 2019 with total page 201 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Author : Jeffrey L. Benovic
Publisher :
ISBN 13 :
Total Pages : 330 pages
Book Rating : 4.3/5 (91 download)
Download or read book Regulation of G Protein-coupled Receptor Function and Expression written by Jeffrey L. Benovic and published by . This book was released on 2000 with total page 330 pages. Available in PDF, EPUB and Kindle. Book excerpt: This comprehensive text describes many techniques that are used to define the molecular mechanisms involved in receptor regulation. It covers a broad range of important concepts and methodologies in the study of G protein-coupled receptors.
Author :
Publisher : Elsevier
ISBN 13 : 0080497276
Total Pages : 555 pages
Book Rating : 4.0/5 (84 download)
Download or read book Regulators of G Protein Signaling, Part B written by and published by Elsevier. This book was released on 2004-11-16 with total page 555 pages. Available in PDF, EPUB and Kindle. Book excerpt: Regulators of G Protein Signaling, Part B continues the in-depth treatment of the topic and covers the RSG protein superfamily including RZ, R4, R7, R12, RhoGEF, and GRK, as well as other heterotrimeric G-protein signaling regulators. - Table of Contents - RZ Subfamily - R4 Subfamily - R7 Subfamily - R12 Subfamily - RhoGEF Subfamily - GRK Subfamily - Other RGS proteins - Activators - Inhibitors - Other Modulators
Author : Peishen Zhao
Publisher :
ISBN 13 :
Total Pages : 492 pages
Book Rating : 4.:/5 (16 download)
Download or read book Regulation of G Protein Signaling by GoLoco Motif Containing Proteins written by Peishen Zhao and published by . This book was released on 2011 with total page 492 pages. Available in PDF, EPUB and Kindle. Book excerpt: Signal transduction via heterotrimeric G proteins in response to transmembrane G protein-coupled receptors plays a central aspect in how cells integrate extracellular stimuli and produce biological responses. In addition to receptor-mediated activation of heterotrimeric G proteins, during the last few decades, accessory proteins have been found to regulate G protein activity via different mechanisms. Several proteins have been identified that contain multiple G protein regulatory domains. Using various molecular and biochemical approaches, we have characterized the effects of two such proteins, G18 and RGS14, on G protein activity. Both proteins contain a second G protein binding domain in addition to the GoLoco domain, which primarily acts as a guanine nucleotide dissociation inhibitor (GDI) on Gi/o proteins. Our results identified that the N-terminal region of G18 is a novel G protein-interacting domain, which may have distinct regulatory effects within the Gi/o subfamily and could potentially play a role in differentiating signals between these related G proteins. In addition, we characterized the tissue and cellular distribution of G18. We found that G18 is expressed in primary isolated rat aortic smooth muscle cells and endothelial cells. A protein-protein interaction assay indicated that G18 is able to directly interact with RGS5, an RGS protein that is also highly expressed in vascular tissue. This interaction results in an increase in RGS5 GTPase accelerating protein (GAP) activity with little or no effect on G18 activity. In Chapter 4 of the thesis, we identified a novel GAP enhancing domain located at the Rasbinding (RB) region of RGS14. This enhancement may be due to the intramolecular interaction between the RB domain and the RGS domain. Furthermore, this interaction may also result in an inhibitory effect on the GDI activity of the RGS14 GoLoco motif. Overall, my work suggests that GoLoco motif containing proteins G18 and RGS14 are organizers of G protein signaling that also modulate RGS protein function.
