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Journal articles on the topic 'GPCR Signalling Pathways'

Author: Grafiati

Published: 6 September 2023

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1

Mohamed, Raafat, Reearna Janke, Wanru Guo, et al. "GPCR transactivation signalling in vascular smooth muscle cells: role of NADPH oxidases and reactive oxygen species." Vascular Biology 1, no. 1 (2019): R1—R11. http://dx.doi.org/10.1530/vb-18-0004.

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The discovery and extension of G-protein-coupled receptor (GPCR) transactivation-dependent signalling has enormously broadened the GPCR signalling paradigm. GPCRs can transactivate protein tyrosine kinase receptors (PTKRs) and serine/threonine kinase receptors (S/TKRs), notably the epidermal growth factor receptor (EGFR) and transforming growth factor-β type 1 receptor (TGFBR1), respectively. Initial comprehensive mechanistic studies suggest that these two transactivation pathways are distinct. Currently, there is a focus on GPCR inhibitors as drug targets, and they have proven to be efficacio

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Ellisdon, Andrew M., and Michelle L. Halls. "Compartmentalization of GPCR signalling controls unique cellular responses." Biochemical Society Transactions 44, no. 2 (2016): 562–67. http://dx.doi.org/10.1042/bst20150236.

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With >800 members, G protein-coupled receptors (GPCRs) are the largest class of cell-surface signalling proteins, and their activation mediates diverse physiological processes. GPCRs are ubiquitously distributed across all cell types, involved in many diseases and are major drug targets. However, GPCR drug discovery is still characterized by very high attrition rates. New avenues for GPCR drug discovery may be provided by a recent shift away from the traditional view of signal transduction as a simple chain of events initiated from the plasma membrane. It is now apparent that GPCR signallin

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Liu, Ying, Yang Yang, Richard Ward, et al. "Biased signalling: the instinctive skill of the cell in the selection of appropriate signalling pathways." Biochemical Journal 470, no. 2 (2015): 155–67. http://dx.doi.org/10.1042/bj20150358.

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GPCRs (G-protein-coupled receptors) are members of a family of proteins which are generally regarded as the largest group of therapeutic drug targets. Ligands of GPCRs do not usually activate all cellular signalling pathways linked to a particular seven-transmembrane receptor in a uniform manner. The fundamental idea behind this concept is that each ligand has its own ability, while interacting with the receptor, to activate different signalling pathways (or a particular set of signalling pathways) and it is this concept which is known as biased signalling. The importance of biased signalling

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Bhattacharya, M., A. V. Babwah, and S. S. G. Ferguson. "Small GTP-binding protein-coupled receptors." Biochemical Society Transactions 32, no. 6 (2004): 1040–44. http://dx.doi.org/10.1042/bst0321040.

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Heterotrimeric GPCRs (G-protein-coupled receptors) form the largest group of integral membrane receptor proteins and mediate diverse physiological processes. In addition to signalling via heterotrimeric G-proteins, GPCRs can also signal by interacting with various small G-proteins to regulate downstream effector pathways. The small G-protein superfamily is structurally classified into at least five families: the Ras, Rho/Rac/cdc42, Rab, Sar1/Arf and Ran families. They are monomeric G-proteins with molecular masses over the range 20–30 kDa, which function as molecular switches to control many e

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Mary, Sophie, Jean-Alain Fehrentz, Marjorie Damian, et al. "How ligands and signalling proteins affect G-protein-coupled receptors' conformational landscape." Biochemical Society Transactions 41, no. 1 (2013): 144–47. http://dx.doi.org/10.1042/bst20120267.

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The dynamic character of GPCRs (G-protein-coupled receptors) is essential to their function. However, the details of how ligands and signalling proteins stabilize a receptor conformation to trigger the activation of a given signalling pathway remain largely unexplored. Multiple data, including recent results obtained with the purified ghrelin receptor, suggest a model where ligand efficacy and functional selectivity are directly related to different receptor conformations. Importantly, distinct effector proteins (G-proteins and arrestins) as well as ligands are likely to affect the conformatio

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Kamato, Danielle, Mai Gabr, Hirushi Kumarapperuma та ін. "Gαq Is the Specific Mediator of PAR-1 Transactivation of Kinase Receptors in Vascular Smooth Muscle Cells". International Journal of Molecular Sciences 23, № 22 (2022): 14425. http://dx.doi.org/10.3390/ijms232214425.

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Aims: G protein-coupled receptor (GPCR) transactivation of kinase receptors greatly expands the actions attributable to GPCRs. Thrombin, via its cognate GPCR, protease-activated receptor (PAR)-1, transactivates tyrosine and serine/threonine kinase receptors, specifically the epidermal growth factor receptor and transforming growth factor-β receptor, respectively. PAR-1 transactivation-dependent signalling leads to the modification of lipid-binding proteoglycans involved in the retention of lipids and the development of atherosclerosis. The mechanisms of GPCR transactivation of kinase receptors

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Gorvin, Caroline M. "Insights into calcium-sensing receptor trafficking and biased signalling by studies of calcium homeostasis." Journal of Molecular Endocrinology 61, no. 1 (2018): R1—R12. http://dx.doi.org/10.1530/jme-18-0049.

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The calcium-sensing receptor (CASR) is a class C G-protein-coupled receptor (GPCR) that detects extracellular calcium concentrations, and modulates parathyroid hormone secretion and urinary calcium excretion to maintain calcium homeostasis. The CASR utilises multiple heterotrimeric G-proteins to mediate signalling effects including activation of intracellular calcium release; mitogen-activated protein kinase (MAPK) pathways; membrane ruffling; and inhibition of cAMP production. By studying germline mutations in the CASR and proteins within its signalling pathway that cause hyper- and hypocalca

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Hart, Stefan, Oliver M. Fischer, Norbert Prenzel, et al. "GPCR-induced migration of breast carcinoma cells depends on both EGFR signal transactivation and EGFR-independent pathways." Biological Chemistry 386, no. 9 (2005): 845–55. http://dx.doi.org/10.1515/bc.2005.099.

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Abstract The epidermal growth factor receptor (EGFR) plays a key role in the regulation of important cellular processes under normal and pathophysiological conditions such as cancer. In human mammary carcinomas the EGFR is involved in regulating cell growth, survival, migration and metastasis and its activation correlates with the lack of response in hormone therapy. Here, we demonstrate in oestrogen receptor-positive and -negative human breast cancer cells and primary mammary epithelial cells a cross-communication between G protein-coupled receptors (GPCRs) and the EGFR. We present evidence t

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Fischer, O. M., S. Hart, A. Gschwind, and A. Ullrich. "EGFR signal transactivation in cancer cells." Biochemical Society Transactions 31, no. 6 (2003): 1203–8. http://dx.doi.org/10.1042/bst0311203.

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The EGFR (epidermal growth factor receptor) plays a key role in the regulation of essential normal cellular processes and in the pathophysiology of hyperproliferative diseases such as cancer. Recent investigations have demonstrated that GPCRs (G-protein-coupled receptors) are able to utilize the EGFR as a downstream signalling partner in the generation of mitogenic signals. This cross-talk mechanism combines the broad diversity of GPCRs with the signalling capacities of the EGFR and has emerged as a general concept in a multitude of cell types. The molecular mechanisms of EGFR signal transacti

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WERRY, Tim D., Graeme F. WILKINSON, and Gary B. WILLARS. "Mechanisms of cross-talk between G-protein-coupled receptors resulting in enhanced release of intracellular Ca2+." Biochemical Journal 374, no. 2 (2003): 281–96. http://dx.doi.org/10.1042/bj20030312.

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Alteration in [Ca2+]i (the intracellular concentration of Ca2+) is a key regulator of many cellular processes. To allow precise regulation of [Ca2+]i and a diversity of signalling by this ion, cells possess many mechanisms by which they are able to control [Ca2+]i both globally and at the subcellular level. Among these are many members of the superfamily of GPCRs (G-protein-coupled receptors), which are characterized by the presence of seven transmembrane domains. Typically, those receptors able to activate PLC (phospholipase C) enzymes cause release of Ca2+ from intracellular stores and influ

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Chen, Siyun, Tamar Getter, David Salom, et al. "Capturing a rhodopsin receptor signalling cascade across a native membrane." Nature 604, no. 7905 (2022): 384–90. http://dx.doi.org/10.1038/s41586-022-04547-x.

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AbstractG protein-coupled receptors (GPCRs) are cell-surface receptors that respond to various stimuli to induce signalling pathways across cell membranes. Recent progress has yielded atomic structures of key intermediates1,2 and roles for lipids in signalling3,4. However, capturing signalling events of a wild-type receptor in real time, across a native membrane to its downstream effectors, has remained elusive. Here we probe the archetypal class A GPCR, rhodopsin, directly from fragments of native disc membranes using mass spectrometry. We monitor real-time photoconversion of dark-adapted rho

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von Zastrow, M. "Role of endocytosis in signalling and regulation of G-protein-coupled receptors." Biochemical Society Transactions 29, no. 4 (2001): 500–504. http://dx.doi.org/10.1042/bst0290500.

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Many G-protein-coupled receptors (GPCRs) undergo agonist-induced endocytosis. Endocytosis contributes to distinct processes that regulate the number and functional activity of receptors present in the plasma membrane, contributing to the well described processes of receptor sequestration and down-regulation. Emerging evidence suggests additional functions of endocytosis in mediating GPCR signalling via certain effector pathways, such as mitogen-activated protein kinase modules. The diverse functions of endocytosis raise fundamental questions about the nature of the vesicular carriers and membr

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Gao, Zhengyin, Weng I. Lei, and Leo Tsz On Lee. "The Role of Neuropeptide-Stimulated cAMP-EPACs Signalling in Cancer Cells." Molecules 27, no. 1 (2022): 311. http://dx.doi.org/10.3390/molecules27010311.

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Neuropeptides are autocrine and paracrine signalling factors and mainly bind to G protein-coupled receptors (GPCRs) to trigger intracellular secondary messenger release including adenosine 3′, 5′-cyclic monophosphate (cAMP), thus modulating cancer progress in different kind of tumours. As one of the downstream effectors of cAMP, exchange proteins directly activated by cAMP (EPACs) play dual roles in cancer proliferation and metastasis. More evidence about the relationship between neuropeptides and EPAC pathways have been proposed for their potential role in cancer development; hence, this revi

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Al-Janabi, Ismail Ibrahim. "G Protein-Coupled Receptors: Undervalued Targets for Cancer Therapy." Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512) 31, no. 1 (2022): 1–19. http://dx.doi.org/10.31351/vol31iss1pp1-19.

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Despite the G protein-coupled receptors (GPCRs) being the largest family of signalling proteins at the surface of cells, their potential to be targeted in cancer therapy is still under-utilised. This review highlights the contribution of these receptors to the process of oncogenesis and points to some likely challenges that might be encountered in targeting them. GPCR-signalling pathways are often complex and can be tissue-specific. Cancer cells hijack these communication networks to their proliferative advantage. The role of selected GPCRs in the different hallmarks of cancer is examined to h

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Ladds, Graham, Alan Goddard, and John Davey. "Functional analysis of heterologous GPCR signalling pathways in yeast." Trends in Biotechnology 23, no. 7 (2005): 367–73. http://dx.doi.org/10.1016/j.tibtech.2005.05.007.

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Barclay, Zoë, Louise Dickson, Derek N. Robertson, et al. "5-HT2A receptor signalling through phospholipase D1 associated with its C-terminal tail." Biochemical Journal 436, no. 3 (2011): 651–60. http://dx.doi.org/10.1042/bj20101844.

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The 5-HT2AR (5-hydroxytryptamine-2A receptor) is a GPCR (G-protein-coupled receptor) that is implicated in the actions of hallucinogens and represents a major target of atypical antipsychotic agents. In addition to its classical signalling though PLC (phospholipase C), the receptor can activate several other pathways, including ARF (ADP-ribosylation factor)-dependent activation of PLD (phospholipase D), which appears to be achieved through a mechanism independent of heterotrimeric G-proteins. In the present study we show that wild-type and inactive constructs of PLD1 (but not PLD2) respectivel

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Gross, Victoria Elisabeth, and Simone Prömel. "Duale Rezeptorsignale: Wie setzen Adhäsions-GPCR Signale in Funktion um?" BIOspektrum 27, no. 5 (2021): 488–90. http://dx.doi.org/10.1007/s12268-021-1625-1.

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AbstractAdhesion GPCR are exceptional receptors due to their functional and structural diversity. A key to their function/signalling, setting them apart from other GPCR, is their extraordinarily large, complex N terminus, via which they mediate different molecular mechanisms and integrate diverse biological functions. Here, we discuss dual modes of adhesion GPCR action and how they translate into physiological functions: activation of G protein pathways and signals solely elicited by the N terminus.

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Pfleger, K. D. G., M. B. Dalrymple, J. R. Dromey та K. A. Eidne. "Monitoring interactions between G-protein-coupled receptors and β-arrestins". Biochemical Society Transactions 35, № 4 (2007): 764–66. http://dx.doi.org/10.1042/bst0350764.

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β-Arrestins 1 and 2 are ubiquitously expressed intracellular adaptor and scaffolding proteins that play important roles in GPCR (G-protein-coupled receptor) desensitization, internalization, intracellular trafficking and G-protein-independent signalling. Recent developments in BRET (bioluminescence resonance energy transfer) technology enable novel insights to be gained from real-time monitoring of GPCR–β-arrestin complexes in live cells for prolonged periods. In concert with confocal microscopy, assays for studying internalization and recycling kinetics such as ELISAs, and techniques for meas

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Sposini, Silvia, and Aylin C. Hanyaloglu. "Driving gonadotrophin hormone receptor signalling: the role of membrane trafficking." Reproduction 156, no. 6 (2018): R195—R208. http://dx.doi.org/10.1530/rep-18-0423.

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Our understanding of G protein-coupled receptor (GPCR) signalling has significantly evolved over the past decade, whereby signalling not only occurs from the plasma membrane but continues, or is reactivated, following internalisation in to endosomal compartments. The spatial organisation of GPCRs is thus essential to decode dynamic and complex signals and to activate specific downstream pathways that elicit the appropriate cellular response. For the gonadotrophin hormone receptors, membrane trafficking has been demonstrated to play a significant role in regulating its signal activity that in t

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Capper, Michael J., and Daniel Wacker. "How the ubiquitous GPCR receptor family selectively activates signalling pathways." Nature 558, no. 7711 (2018): 529–30. http://dx.doi.org/10.1038/d41586-018-05503-4.

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Alaridah, Nader, Nataliya Lutay, Erik Tenland, et al. "Mycobacteria Manipulate G-Protein-Coupled Receptors to Increase Mucosal Rac1 Expression in the Lungs." Journal of Innate Immunity 9, no. 3 (2016): 318–29. http://dx.doi.org/10.1159/000453454.

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Mycobacterium bovis bacille Calmette-Guérin (BCG) is currently the only approved vaccine against tuberculosis (TB). BCG mimics M. tuberculosis (Mtb) in its persistence in the body and is used as a benchmark to compare new vaccine candidates. BCG was originally designed for mucosal vaccination, but comprehensive knowledge about its interaction with epithelium is currently lacking. We used primary airway epithelial cells (AECs) and a murine model to investigate the initial events of mucosal BCG interactions. Furthermore, we analysed the impact of the G-protein-coupled receptors (GPCRs), CXCR1 an

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Baker, Jillian G., and Stephen J. Hill. "Multiple GPCR conformations and signalling pathways: implications for antagonist affinity estimates." Trends in Pharmacological Sciences 28, no. 8 (2007): 374–81. http://dx.doi.org/10.1016/j.tips.2007.06.011.

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Deupi, Xavier, Jörg Standfuss, and Gebhard Schertler. "Conserved activation pathways in G-protein-coupled receptors." Biochemical Society Transactions 40, no. 2 (2012): 383–88. http://dx.doi.org/10.1042/bst20120001.

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GPCRs (G-protein-coupled receptors) are seven-transmembrane helix proteins that transduce exogenous and endogenous signals to modulate the activity of downstream effectors inside the cell. Despite the relevance of these proteins in human physiology and pharmaceutical research, we only recently started to understand the structural basis of their activation mechanism. In the period 2008–2011, nine active-like structures of GPCRs were solved. Among them, we have determined the structure of light-activated rhodopsin with all the features of the active metarhodopsin-II, which represents so far the

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Alloatti, G., G. Montrucchio, G. Lembo та E. Hirsch. "Phosphoinositide 3-kinase γ: kinase-dependent and -independent activities in cardiovascular function and disease". Biochemical Society Transactions 32, № 2 (2004): 383–86. http://dx.doi.org/10.1042/bst0320383.

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Cardiac function is controlled by GPCRs (G-protein-coupled receptors) which exert their function by triggering numerous signalling pathways, including the activation of PI3K (phosphoinositide 3-kinase). The GPCR-activated PI3Kγ is weakly expressed in the heart, but the deletion of its expression in mice causes remarkable phenotypes. Indeed, the lack of PI3Kγ does not modify heart rate and blood pressure, but does increase contractility, particularly in response to stimuli that enhance cardiac contractile force, such as catecholamines. Consistently, treatment of mutant cardiomyocytes with β-adr

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Wiseman, Daniel N., Nikita Samra, María Monserrat Román Lara, Samantha C. Penrice, and Alan D. Goddard. "The Novel Application of Geometric Morphometrics with Principal Component Analysis to Existing G Protein-Coupled Receptor (GPCR) Structures." Pharmaceuticals 14, no. 10 (2021): 953. http://dx.doi.org/10.3390/ph14100953.

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The G protein-coupled receptor (GPCR) superfamily is a large group of membrane proteins which, because of their vast involvement in cell signalling pathways, are implicated in a plethora of disease states and are therefore considered to be key drug targets. Despite advances in techniques to study these receptors, current prophylaxis is often limited due to the challenging nature of their dynamic, complex structures. Greater knowledge and understanding of their intricate structural rearrangements will therefore undoubtedly aid structure-based drug design against GPCRs. Disciplines such as anthr

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Roberts, Chrissy H., Sander Ouburg, Mark D. Preston, Henry J. C. de Vries, Martin J. Holland, and Servaas A. Morré. "Pathway-Wide Genetic Risks in Chlamydial Infections Overlap between Tissue Tropisms: A Genome-Wide Association Scan." Mediators of Inflammation 2018 (June 3, 2018): 1–9. http://dx.doi.org/10.1155/2018/3434101.

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Chlamydia trachomatis is the most commonly diagnosed bacterial sexually transmitted infection and can lead to tubal factor infertility, a disease characterised by fibrosis of the fallopian tubes. Genetic polymorphisms in molecular pathways involving G protein-coupled receptor signalling, the Akt/PI3K cascade, the mitotic cell cycle, and immune response have been identified in association with the development of trachomatous scarring, an ocular form of chlamydia-related fibrotic pathology. In this case-control study, we performed genome-wide association and pathways-based analysis in a sample o

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Daly, Carole A., Martine J. Smit, and Bianca Plouffe. "The constitutive activity of the viral-encoded G protein-coupled receptor US28 supports a complex signalling network contributing to cancer development." Biochemical Society Transactions 48, no. 4 (2020): 1493–504. http://dx.doi.org/10.1042/bst20190988.

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US28 is a viral G protein-coupled receptor (GPCR) encoded by the human cytomegalovirus (HCMV). This receptor, expressed both during lytic replication and viral latency, is required for latency. US28 is binding to a wide variety of chemokines but also exhibits a particularly high constitutive activity robustly modulating a wide network of cellular pathways altering the host cell environment to benefit HCMV infection. Several studies suggest that US28-mediated signalling may contribute to cancer progression. In this review, we discuss the unique structural characteristics that US28 acquired thro

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Langer, I., and P. Robberecht. "Molecular mechanisms involved in vasoactive intestinal peptide receptor activation and regulation: current knowledge, similarities to and differences from the A family of G-protein-coupled receptors." Biochemical Society Transactions 35, no. 4 (2007): 724–28. http://dx.doi.org/10.1042/bst0350724.

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An actual paradigm for activation and regulation of the GPCR (G-protein-coupled receptors)/seven-transmembrane helix family of receptors essentially emerges from extensive studies of the largest family of receptors, the GPCR-A/rhodopsin family. The mechanisms regulating the GPCR-B family signal transduction are less precisely understood due in part to the lack of the conserved signatures of the GPCR-A family (E/DRY, NPXXY) and in part to the absence of a reliable receptor modelling, although some studies suggest that both families share similar features. Here, we try to highlight the current k

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Cattaneo, Fabio, Martina Castaldo, Melania Parisi, Raffaella Faraonio, Gabriella Esposito, and Rosario Ammendola. "Formyl Peptide Receptor 1 Modulates Endothelial Cell Functions by NADPH Oxidase-Dependent VEGFR2 Transactivation." Oxidative Medicine and Cellular Longevity 2018 (2018): 1–12. http://dx.doi.org/10.1155/2018/2609847.

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In the vasculature, NADPH oxidase is the main contributor of reactive oxygen species (ROS) which play a key role in endothelial signalling and functions. We demonstrate that ECV304 cells express p47phox, p67phox, and p22phox subunits of NADPH oxidase, as well as formyl peptide receptors 1 and 3 (FPR1/3), which are members of the GPCR family. By RT-PCR, we also detected Flt-1 and Flk-1/KDR in these cells. Stimulation of FPR1 by N-fMLP induces p47phox phosphorylation, which is the crucial event for NADPH oxidase-dependent superoxide production. Transphosphorylation of RTKs by GPCRs is a biologic

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CHO, Hyeseon, Kathleen HARRISON, Owen SCHWARTZ, and John H. KEHRL. "The aorta and heart differentially express RGS (regulators of G-protein signalling) proteins that selectively regulate sphingosine 1-phosphate, angiotensin II and endothelin-1 signalling." Biochemical Journal 371, no. 3 (2003): 973–80. http://dx.doi.org/10.1042/bj20021769.

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Normal cardiovascular development and physiology depend in part upon signalling through G-protein-coupled receptors (GPCRs), such as the angiotensin II type 1 (AT1) receptor, sphingosine 1-phosphate (S1P) receptors and endothelin-1 (ET-1) receptor. Since regulator of G-protein signalling (RGS) proteins function as GTPase-activating proteins for the Gα subunit of heterotrimeric G-proteins, these proteins undoubtedly have functional roles in the cardiovascular system. In the present paper, we show that human aorta and heart differentially express RGS1, RGS2, RGS3S (short-form), RGS3L (long-form)

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Masood, Mehar, Madahiah Bint E. Masood, Noor Us Subah, Maria Shabbir, Rehan Zafar Paracha, and Mehak Rafiq. "Investigating isoform switching in RHBDF2 and its role in neoplastic growth in breast cancer." PeerJ 10 (November 25, 2022): e14124. http://dx.doi.org/10.7717/peerj.14124.

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Background Breast cancer is the second leading cause of cancer-related deaths globally, and its prevalence rates are increasing daily. In the past, studies predicting therapeutic drug targets for cancer therapy focused on the assumption that one gene is responsible for producing one protein. Therefore, there is always an immense need to find promising and novel anti-cancer drug targets. Furthermore, proteases have an integral role in cell proliferation and growth because the proteolysis mechanism is an irreversible process that aids in regulating cellular growth during tumorigenesis. Therefore

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Rodrigues, A. R., A. M. Gouveia, J. G. Ferreira, and H. Almeida. "ACTH Induces ERK 1/2 Activation in Rat Adrenal Primary Cultures." Microscopy and Microanalysis 14, S3 (2008): 101–2. http://dx.doi.org/10.1017/s1431927608089526.

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Adrenocorticotropic hormone (ACTH) is the most potent stimulator of adrenal cortex, acting through the Melanocortin-2 receptor (MC2R). ACTH induces secretion of steroid hormones, critical for the normal stress response and plays also an important role on cell proliferation and differentiation. MC2R is a classical G-Protein coupled receptor (GPCR), thus activating Protein Kinase A (PKA). However, many studies suggested a cross-talk between different signalling pathways and a more complex intracellular network. In fact, in adrenocortical Y1 tumour cell line, ACTH may activate Extracellular Regul

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Fok, Christine, Milan Bogosanovic, Madhavi Pandya, Ravindra Telang, Peter R. Thorne, and Srdjan M. Vlajkovic. "Regulator of G Protein Signalling 4 (RGS4) as a Novel Target for the Treatment of Sensorineural Hearing Loss." International Journal of Molecular Sciences 22, no. 1 (2020): 3. http://dx.doi.org/10.3390/ijms22010003.

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We and others have previously identified signalling pathways associated with the adenosine A1 receptor (A1R) as important regulators of cellular responses to injury in the cochlea. We have shown that the “post-exposure” treatment with adenosine A1R agonists confers partial protection against acoustic trauma and other forms of sensorineural hearing loss (SNHL). The aim of this study was to determine if increasing A1R responsiveness to endogenous adenosine would have the same otoprotective effect. This was achieved by pharmacological targeting of the Regulator of G protein Signalling 4 (RGS4). R

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Chao, Moses V., Rithwick Rajagopal, and Francis S. Lee. "Neurotrophin signalling in health and disease." Clinical Science 110, no. 2 (2006): 167–73. http://dx.doi.org/10.1042/cs20050163.

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Neurotrophins are a unique family of polypeptide growth factors that influence the proliferation, differentiation, survival and death of neuronal and non-neuronal cells. They are essential for the health and well-being of the nervous system. NGF (nerve growth factor), BDNF (brain-derived neurotrophic factor), NT-3 (neurotrophin-3) and NT-4 (neurotrophin-4) also mediate additional higher-order activities, such as learning, memory and behaviour, in addition to their established functions for cell survival. The effects of neurotrophins depend upon their levels of availability, their affinity of b

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Rovira, Xavier, Jean-Philippe Pin, and Jesús Giraldo. "The asymmetric/symmetric activation of GPCR dimers as a possible mechanistic rationale for multiple signalling pathways." Trends in Pharmacological Sciences 31, no. 1 (2010): 15–21. http://dx.doi.org/10.1016/j.tips.2009.10.008.

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Kelly, Eamonn. "Ligand bias at the μ-opioid receptor". Biochemical Society Transactions 41, № 1 (2013): 218–24. http://dx.doi.org/10.1042/bst20120331.

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Ligand bias refers to the ability of a drug at a receptor to activate selectively particular cell signalling pathways over others, in a way that cannot be explained by traditional models of receptor theory. For a physiologically and therapeutically important GPCR (G-protein-coupled receptor) such as the MOPr (μ-opioid receptor), the role of ligand bias is currently being explored, not only in order to understand the molecular function of this receptor, but also with a view to developing better analgesic drugs with fewer adverse effects. In this short review, the ways to detect and quantify ago

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Zandona, Antonio, Tamara Zorbaz, Katarina Miš, Sergej Pirkmajer, and Maja Katalinić. "Cytotoxicity-related effects of imidazolium and chlorinated bispyridinium oximes in SH-SY5Y cells." Archives of Industrial Hygiene and Toxicology 73, no. 4 (2022): 277–84. http://dx.doi.org/10.2478/aiht-2022-73-3688.

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Abstract Current research has shown that several imidazolium and chlorinated bispyridinium oximes are cytotoxic and activate different mechanisms or types of cell death. To investigate this further, we analysed interactions between these oximes and acetylcholine receptors (AChRs) and how they affect several signalling pathways to find a relation between the observed toxicities and their effects on these specific targets. Chlorinated bispyridinium oximes caused time-dependent cytotoxicity by inhibiting the phosphorylation of STAT3 and AMPK without decreasing ATP and activated ERK1/2 and p38 MAP

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BISOTTO, Sandra, and Elizabeth D. FIXMAN. "Src-family tyrosine kinases, phosphoinositide 3-kinase and Gab1 regulate extracellular signal-regulated kinase 1 activation induced by the type A endothelin-1 G-protein-coupled receptor." Biochemical Journal 360, no. 1 (2001): 77–85. http://dx.doi.org/10.1042/bj3600077.

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The multisubstrate docking protein, growth-factor-receptor-bound protein 2-associated binder 1 (Gab1), which is phosphorylated on tyrosine residues following activation of receptor tyrosine kinases and cytokine receptors, regulates cell proliferation, survival and epithelial morphogenesis. Gab1 is also tyrosine phosphorylated following activation of G-protein-coupled receptors (GPCRs) where its function is poorly understood. To elucidate the role of Gab1 in GPCR signalling, we investigated the mechanism by which the type A endothelin-1 (ET-1) GPCR induced tyrosine phosphorylation of Gab1. Tyro

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Sandgren, Johanna, Stefan Holm, Ana Maria Marino, et al. "Whole Exome- and mRNA-Sequencing of an AT/RT Case Reveals Few Somatic Mutations and Several Deregulated Signalling Pathways in the Context ofSMARCB1Deficiency." BioMed Research International 2015 (2015): 1–12. http://dx.doi.org/10.1155/2015/862039.

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Background. AT/RTs are rare aggressive brain tumours, mainly affecting young children. Most cases present with genetic inactivation ofSMARCB1, a core member of the SWI/SNF chromatin-remodeling complex. We have performed whole exome- and mRNA-sequencing on an early onset AT/RT case for detection of genetic events potentially contributing to the disease.Results. Ade novogermline variant inSMARCB1, c.601C>T p.Arg201∗, in combination with somatic deletion of the healthy allele is likely the major tumour causing event. Only seven somatic small scale mutations were discovered (hittingSEPT03, H2BF

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Nath, D., N. J. Williamson, R. Jarvis, and G. Murphy. "Shedding of c-Met is regulated by crosstalk between a G-protein coupled receptor and the EGF receptor and is mediated by a TIMP-3 sensitive metalloproteinase." Journal of Cell Science 114, no. 6 (2001): 1213–20. http://dx.doi.org/10.1242/jcs.114.6.1213.

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A wide repertoire of transmembrane proteins are proteolytically released from the cell surface by a process known as ‘ectodomain shedding’, under both normal and pathophysiological conditions. Little is known about the physiological mechanisms that regulate this process. As a model system, we have investigated the metalloproteinase-mediated cleavage of the hepatocyte growth factor receptor, Met. We show that epidermal growth factor (EGF) receptor activation, either directly by EGF or indirectly via the G-protein coupled receptor (GPCR) agonist lysophosphatidic acid (LPA), induces cleavage of M

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YOWE, David, Nadine WEICH, Mercy PRABHUDAS, et al. "RGS18 is a myeloerythroid lineage-specific regulator of G-protein-signalling molecule highly expressed in megakaryocytes." Biochemical Journal 359, no. 1 (2001): 109–18. http://dx.doi.org/10.1042/bj3590109.

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Myelopoiesis and lymphopoiesis are controlled by haematopoietic growth factors, including cytokines, and chemokines that bind to G-protein-coupled receptors (GPCRs). Regulators of G-protein signalling (RGSs) are a protein family that can act as GTPase-activating proteins for Gαi- and Gαq-class proteins. We have identified a new member of the R4 subfamily of RGS proteins, RGS18. RGS18 contains clusters of hydrophobic and basic residues, which are characteristic of an amphipathic helix within its first 33 amino acids. RGS18 mRNA was most highly abundant in megakaryocytes, and was also detected s

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Labani, Nedjma, Florence Gbahou, Marc Noblet, et al. "Pistacia vera Extract Potentiates the Effect of Melatonin on Human Melatonin MT1 and MT2 Receptors with Functional Selectivity." Pharmaceutics 15, no. 7 (2023): 1845. http://dx.doi.org/10.3390/pharmaceutics15071845.

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Melatonin is a tryptophan derivative synthesized in plants and animals. In humans, melatonin acts on melatonin MT1 and MT2 receptors belonging to the G protein-coupled receptor (GPCR) family. Synthetic melatonin receptor agonists are prescribed for insomnia and depressive and circadian-related disorders. Here, we tested 25 commercial plant extracts, reported to have beneficial properties in sleep disorders and anxiety, using cellular assays (2─[125I]iodomelatonin binding, cAMP inhibition, ERK1/2 activation and β-arrestin2 recruitment) in mock-transfected and HEK293 cells expressing MT1 or MT2.

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Kostenis, Evi. "G Proteins in Drug Screening: From Analysis of Receptor-G Protein Specificity to Manipulation of GPCR-Mediated Signalling Pathways." Current Pharmaceutical Design 12, no. 14 (2006): 1703–15. http://dx.doi.org/10.2174/138161206776873734.

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Kumar, Shree Senthil, Marie-Louise Ward, and Kathleen Grace Mountjoy. "Quantitative high-throughput assay to measure MC4R-induced intracellular calcium." Journal of Molecular Endocrinology 66, no. 4 (2021): 285–97. http://dx.doi.org/10.1530/jme-20-0285.

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The melanocortin-4 receptor (MC4R), a critical G-protein-coupled receptor (GPCR) regulating energy homeostasis, activates multiple signalling pathways, including mobilisation of intracellular calcium ([Ca2+]i). However, very little is known about the physiological significance of MC4R-induced [Ca2+]i since few studies measure MC4R-induced [Ca2+]i. High-throughput, read-out assays for [Ca2+]i have proven unreliable for overexpressed GPCRs like MC4R, which exhibit low sensitivity mobilising [Ca2+]i. Therefore, we developed, optimised, and validated a robust quantitative high-throughput assay usi

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Gorvin, Caroline M. "Molecular and clinical insights from studies of calcium-sensing receptor mutations." Journal of Molecular Endocrinology 63, no. 2 (2019): R1—R16. http://dx.doi.org/10.1530/jme-19-0104.

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Twenty-five years have elapsed since the calcium-sensing receptor (CaSR) was first identified in bovine parathyroid and the receptor is now recognized as a fundamental contributor to extracellular Ca2+ (Ca2+ e) homeostasis, regulating parathyroid hormone release and urinary calcium excretion. The CaSR is a class C G-protein-coupled receptor (GPCR) that is functionally active as a homodimer and couples to multiple G-protein subtypes to activate intracellular signalling pathways. The importance of the CaSR in the regulation of Ca2+ e has been highlighted by the identification of >400 differen

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González-Guede, I., M. López-Ramos, L. Rodriguez Rodriguez, L. Abasolo, and B. Fernandez. "POS0409 IMPLICATION OF GLYPICANS AND NOTUM IN BONE MARROW MESENCHYMAL STROMAL CELLS DURING OSTEOGENIC DIFFERENTIATION IN OSTEOARTHRITIC DISEASE." Annals of the Rheumatic Diseases 82, Suppl 1 (2023): 459.3–460. http://dx.doi.org/10.1136/annrheumdis-2023-eular.6294.

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BackgroundOsteoarthritis (OA) is accompanied by an excessive formation of underlying bone caused by homeostatic alterations. It has been described that in OA joints there is an up-regulation of the WNT/β-catenine pathway driving to the differentiation of Mesenchymal Stromal Cells (MSCs) into osteocytes [1]. Glypicans 1-6 act as co-receptors of WNT pathway, improving interactions between molecules [2]. On the other hand, NOTUM plays a role as a negative regulator of the pathway preventing WNT binding to its receptors and favouring the soluble form of Glypicans [3]. All these evidences lead us t

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Coquant, G., D. Aguanno, L. Brot, et al. "P043 3-oxo-C12:2, a Quorum Sensing molecule from the gut, exerts anti-inflammatory effects through a bitter taste receptor." Journal of Crohn's and Colitis 16, Supplement_1 (2022): i160. http://dx.doi.org/10.1093/ecco-jcc/jjab232.172.

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Abstract Background Acyl-Homoserine Lactones (AHLs) are Quorum Sensing molecules involved in the communication network of bacteria and can also have an impact on the host’s cells. We recently showed, in the human gut ecosystem, the presence of AHLs. Among them, we identified one that has never been described: 3-oxo-C12:2. This molecule was decreased in Inflammatory Bowel Disease (IBD) patients, and its presence was correlated to normobiosis. Interestingly, 3-oxo-C12:2 is structurally close to an AHL well described and synthesized by P. aeruginosa, 3-oxo-C12. We intent to describe 3-oxo-C12:2 e

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Little, Peter J. "GPCR responses in vascular smooth muscle can occur predominantly through dual transactivation of kinase receptors and not classical Gαq protein signalling pathways". Life Sciences 92, № 20-21 (2013): 951–56. http://dx.doi.org/10.1016/j.lfs.2013.03.017.

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Raimondi, Francesco, Joshua G. Burkhart, Matthew J. Betts, Robert B. Russell, and Guanming Wu. "Leveraging biochemical reactions to unravel functional impacts of cancer somatic variants affecting protein interaction interfaces." F1000Research 10 (November 3, 2021): 1111. http://dx.doi.org/10.12688/f1000research.74395.1.

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Background: Considering protein mutations in their biological context is essential for understanding their functional impact, interpretation of high-dimensional datasets and development of effective targeted therapies in personalized medicine. Methods: We combined the curated knowledge of biochemical reactions from Reactome with the analysis of interaction-mediating 3D interfaces from Mechismo. In addition, we provided a software tool for users to explore and browse the analysis results in a multi-scale perspective starting from pathways and reactions to protein-protein interactions and protei

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Raimondi, Francesco, Joshua G. Burkhart, Matthew J. Betts, Robert B. Russell, and Guanming Wu. "Leveraging biochemical reactions to unravel functional impacts of cancer somatic variants affecting protein interaction interfaces." F1000Research 10 (December 12, 2022): 1111. http://dx.doi.org/10.12688/f1000research.74395.3.

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Background: Considering protein mutations in their biological context is essential for understanding their functional impact, interpretation of high-dimensional datasets and development of effective targeted therapies in personalized medicine. Methods: We combined the curated knowledge of biochemical reactions from Reactome with the analysis of interaction-mediating 3D interfaces from Mechismo. In addition, we provided a software tool for users to explore and browse the analysis results in a multi-scale perspective starting from pathways and reactions to protein-protein interactions and protei

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