keyword
MENU ▼
Read by QxMD icon Read
search

GPCR signaling

keyword
https://www.readbyqxmd.com/read/28096465/sequences-within-the-c-terminus-of-the-metabotropic-glutamate-receptor-mglur5-are-responsible-for-inner-nuclear-membrane-localization
#1
Ismail Sergin, Yuh-Jiin I Jong, Steven K Harmon, Vikas Kumar, Karen L O'Malley
Traditionally G-protein coupled receptors (GPCR) are thought to be located on the cell surface where they transmit extracellular signals to the cytoplasm. However recent studies indicate that some GPCRs are also localized to various subcellular compartments such as the nucleus where they appear required for various biological functions. For example, the metabotropic glutamate receptor 5, mGluR5, is concentrated at the inner nuclear membrane (INM) where it mediates Ca2+ changes in the nucleoplasm by coupling with Gq/11...
January 17, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28094771/orphan-gpr182-suppresses-erk-mediated-intestinal-proliferation-during-regeneration-and-adenoma-formation
#2
Daniel O Kechele, R Eric Blue, Bailey Zwarycz, Scott T Espenschied, Amanda T Mah, Marni B Siegel, Charles M Perou, Shengli Ding, Scott T Magness, P Kay Lund, Kathleen M Caron
Orphan GPCRs provide an opportunity to identify potential pharmacological targets, yet their expression patterns and physiological functions remain challenging to elucidate. Here, we have used a genetically engineered knockin reporter mouse to map the expression pattern of the Gpr182 during development and adulthood. We observed that Gpr182 is expressed at the crypt base throughout the small intestine, where it is enriched in crypt base columnar stem cells, one of the most active stem cell populations in the body...
January 17, 2017: Journal of Clinical Investigation
https://www.readbyqxmd.com/read/28093215/melanocortin-4-receptor-constitutive-activity-inhibits-l-type-voltage-gated-calcium-channels-in-neurons
#3
F Agosti, S Cordisco Gonzalez, V Martinez Damonte, M J Tolosa, N Di Siervi, H B Schioth, C Davio, M Perello, J Raingo
The melanocortin 4 receptor (MC4R) is a G protein-coupled receptor (GPCR) that is expressed in several brain nuclei playing a crucial role in the regulation of energy balance controlling the homeostasis of the organism. It displays both agonist-evoked and constitutive activity, and moreover, it can couple to different G proteins. Most of the research on MC4R has been focused on agonist-induced activity, while the molecular and cellular basis of MC4R constitutive activity remains scarcely studied. We have previously shown that neuronal N-type voltage-gated calcium channels (CaV2...
January 13, 2017: Neuroscience
https://www.readbyqxmd.com/read/28087443/an-update-on-the-physiological-and-therapeutic-relevance-of-gpcr-oligomers
#4
REVIEW
Batoul Farran
The traditional view on GPCRs held that they function as single monomeric units composed of identical subunits. This notion was overturned by the discovery that GPCRs can form homo- and hetero-oligomers, some of which are obligatory, and can further assemble into receptor mosaics consisting of three or more protomers. Oligomerisation exerts significant impacts on receptor function and physiology, offering a platform for the diversification of receptor signalling, pharmacology, regulation, crosstalk, internalization and trafficking...
January 10, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28074005/synergistic-regulation-of-serotonin-and-opioid-signaling-contributes-to-pain-insensitivity-in-nav1-7-knockout-mice
#5
Jörg Isensee, Leonhardt Krahé, Katharina Moeller, Vanessa Pereira, Jane E Sexton, Xiaohui Sun, Edward Emery, John N Wood, Tim Hucho
Genetic loss of the voltage-gated sodium channel Nav1.7 (Nav1.7(-/-)) results in lifelong insensitivity to pain in mice and humans. One underlying cause is an increase in the production of endogenous opioids in sensory neurons. We analyzed whether Nav1.7 deficiency altered nociceptive heterotrimeric guanine nucleotide-binding protein-coupled receptor (GPCR) signaling, such as initiated by GPCRs that respond to serotonin (pronociceptive) or opioids (antinociceptive), in sensory neurons. We found that the nociceptive neurons of Nav1...
January 10, 2017: Science Signaling
https://www.readbyqxmd.com/read/28073700/the-yeast-ste2p-g-protein-coupled-receptor-dimerizes-on-the-cell-plasma-membrane
#6
Orkun Cevheroğlu, Gözde Kumaş, Melinda Hauser, Jeffrey M Becker, Çağdaş D Son
Dimerization of G protein-coupled receptors (GPCR) may play an important role in maturation, internalization, signaling and/or pharmacology of these receptors. However, the location where dimerization occurs is still under debate. In our study, variants of Ste2p, a yeast mating pheromone GPCR, were tagged with split EGFP (enhanced green fluorescent protein) fragments inserted between transmembrane domain seven and the C-terminus or appended to the C-terminus. Bimolecular Fluorescence Complementation (BiFC) assay was used to determine where receptor dimerization occurred during protein trafficking by monitoring generation of EGFP fluorescence, which occurred upon GPCR dimerization...
January 7, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28073248/interplay-of-g-protein-coupled-receptors-with-the-membrane-insights-from-supra-atomic-coarse-grain-molecular-dynamics-simulations
#7
Xavier Periole
G protein-coupled receptors (GPCRs) are central to many fundamental cellular signaling pathways. They transduce signals from the outside to the inside of cells in physiological processes ranging from vision to immune response. It is extremely challenging to look at them individually using conventional experimental techniques. Recently, a pseudo atomistic molecular model has emerged as a valuable tool to access information on GPCRs, more specifically on their interactions with their environment in their native cell membrane and the consequences on their supramolecular organization...
January 11, 2017: Chemical Reviews
https://www.readbyqxmd.com/read/28059859/pro-inflammatory-cytokines-mediate-gpcr-dysfunction
#8
Maradumane L Mohan, Neelakantan T Vasudevan, Sathyamangla V Naga Prasad
Pro-inflammatory reaction by the body occurs acutely in response to injury that is considered primarily beneficial. However, sustained pro-inflammatory cytokines observed with chronic pathologies such as metabolic syndrome, cancer, and arthritis are detrimental and in many cases is a major cardio-vascular risk factor. Pro-inflammatory cytokines such as interleulin-1 (IL-1), IL-6, and tumor necrosis factor α (TNFα) have long been implicated in cardiovascular risk and considered to be a major underlying cause for heart failure...
December 24, 2016: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28059858/cardiac-gpcr-mediated-egfr-transactivation-impact-and-therapeutic-implications
#9
Laurel A Grisanti, Shuchi Guo, Douglas G Tilley
G protein-coupled receptors (GPCR) remain primary therapeutic targets for numerous cardiovascular disorders, including heart failure (HF), due to their influence on cardiac remodeling in response to elevated neurohormone signaling. GPCR blockers have proven to be beneficial in the treatment of HF by reducing chronic G protein activation and cardiac remodeling, thereby extending the lifespan of HF patients. Unfortunately this effect does not persist indefinitely, thus next generation therapeutics aim to selectively block harmful GPCR-mediated pathways while simultaneously promoting beneficial signaling...
January 3, 2017: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/28059140/identification-and-functional-characterisation-of-5-ht4-receptor-in-sea-cucumber-apostichopus-japonicus-selenka
#10
Tianming Wang, Zhen Yang, Naiming Zhou, Lina Sun, Zhenming Lv, Changwen Wu
Serotonin (5-HT) is an important neurotransmitter and neuromodulator that controls a variety of sensory and motor functions through 5-HT receptors (5-HTRs). The 5-HT4R subfamily is linked to Gs proteins, which activate adenylyl cyclases (ACs), and is involved in many responses in peripheral organs. In this study, the 5-HT4R from Apostichopus japonicus (Aj5-HT4R) was identified and characterised. The cloned full-length Aj5-HT4R cDNA is 1,544 bp long and contains an open reading frame 1,011 bp in length encoding 336 amino acid proteins...
January 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28049717/a-novel-hect-ubiquitin-ligase-regulating-chemotaxis-and-development-in-dictyostelium-discoideum
#11
Barbara Pergolizzi, Enrico Bracco, Salvatore Bozzaro
Cyclic AMP binding to G protein-coupled receptors orchestrates chemotaxis and development in Dictyostelium. By activating the RasC-TORC2-AKT/PKB module, cAMP regulates cell polarization during chemotaxis. TORC2 also mediates GPCR-dependent stimulation of adenylyl cyclase A (ACA), enhancing cAMP relay and developmental gene expression. Thus, mutants defective in the TORC2 Pia/Rictor subunit are impaired in chemotaxis and development. Near-saturation mutagenesis of a Pia/Rictor mutant by random gene disruption led to selection of two suppressor mutants, in which spontaneous chemotaxis and development were restored...
January 3, 2017: Journal of Cell Science
https://www.readbyqxmd.com/read/28045251/a-g-protein-coupled-receptor-dimerization-interface-in-human-cone-opsins
#12
Beata Jastrzebska, William D Comar, Megan J Kaliszewski, Kevin C Skinner, Morgan H Torcasio, Anthony S Esway, Hui Jin, Krzysztof Palczewski, Adam W Smith
G protein-coupled receptors (GPCRs) detect a wide variety of physical and chemical signals and transmit that information across the cellular plasma membrane. Dimerization is a proposed modulator of GPCR signaling, but the structure and stability of class A GPCR dimerization have been difficult to establish. Here we investigated the dimerization affinity and binding interface of human cone opsins, which initiate and sustain daytime color vision. Using a time-resolved fluorescence approach, we found that human red cone opsin exhibits a strong propensity for dimerization, whereas the green and blue cone opsins do not...
November 29, 2016: Biochemistry
https://www.readbyqxmd.com/read/28035083/us28-a-virally-encoded-gpcr-as-an-antiviral-target-for-human-cytomegalovirus-infection
#13
REVIEW
Sungjin Lee, Yoon Hee Chung, Choongho Lee
Viruses continue to evolve a new strategy to take advantage of every aspect of host cells in order to maximize their survival. Due to their central roles in transducing a variety of transmembrane signals, GPCRs seem to be a prime target for viruses to pirate for their own use. Incorporation of GPCR functionality into the genome of herpesviruses has been demonstrated to be essential for pathogenesis of many herpesviruses-induced diseases. Here, we introduce US28 of human cytomegalovirus (HCMV) as the beststudied example of virally-encoded GPCRs to manipulate host GPCR signaling...
January 1, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28035079/biased-g-protein-coupled-receptor-signaling-new-player-in-modulating-physiology-and-pathology
#14
REVIEW
Zuzana Bologna, Jian-Peng Teoh, Ahmed S Bayoumi, Yaoliang Tang, Il-Man Kim
G protein-coupled receptors (GPCRs) are a family of cell-surface proteins that play critical roles in regulating a variety of pathophysiological processes and thus are targeted by almost a third of currently available therapeutics. It was originally thought that GPCRs convert extracellular stimuli into intracellular signals through activating G proteins, whereas β-arrestins have important roles in internalization and desensitization of the receptor. Over the past decade, several novel functional aspects of β-arrestins in regulating GPCR signaling have been discovered...
January 1, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/28034910/yeast-gpcr-signaling-reflects-the-fraction-of-occupied-receptors-not-the-number
#15
Alan Bush, Gustavo Vasen, Andreas Constantinou, Paula Dunayevich, Inés Lucía Patop, Matías Blaustein, Alejandro Colman-Lerner
According to receptor theory, the effect of a ligand depends on the amount of agonist-receptor complex. Therefore, changes in receptor abundance should have quantitative effects. However, the response to pheromone in Saccharomyces cerevisiae is robust (unaltered) to increases or reductions in the abundance of the G-protein-coupled receptor (GPCR), Ste2, responding instead to the fraction of occupied receptor. We found experimentally that this robustness originates during G-protein activation. We developed a complete mathematical model of this step, which suggested the ability to compute fractional occupancy depends on the physical interaction between the inhibitory regulator of G-protein signaling (RGS), Sst2, and the receptor...
December 29, 2016: Molecular Systems Biology
https://www.readbyqxmd.com/read/28028617/calcium-gated-k-channels-of-the-kca1-1-and-kca3-1-type-couple-intracellular-ca-2-signals-to-membrane-hyperpolarization-in-mesenchymal-stromal-cells-from-the-human-adipose-tissue
#16
Michail V Tarasov, Marina F Bystrova, Polina D Kotova, Olga A Rogachevskaja, Veronika Y Sysoeva, Stanislav S Kolesnikov
Electrogenesis in mesenchymal stromal cells (MSCs) remains poorly understood. Little is known about ion channels active in resting MSCs and activated upon MSC stimulation, particularly, by agonists mobilizing Ca(2+) in the MSC cytoplasm. A variety of Ca(2+)-gated ion channels may couple Ca(2+) signals to polarization of the plasma membrane. Here, we studied MSCs from the human adipose tissue and found that in cells responsive to ATP and adenosine with Ca(2+) transients or exhibiting spontaneous Ca(2+) oscillations, Ca(2+) bursts were associated with hyperpolarization mediated by Ca(2+)-gated K(+) channels...
December 27, 2016: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/28027487/functional-selectivity-and-dualsteric-bitopic-gpcr-targeting
#17
REVIEW
Ramona Schrage, Evi Kostenis
Functional selectivity provides a new avenue to selectively engage particular pathways of the pleiotropic signaling repertoire of a G protein-coupled receptor. First examples for signaling biased compounds at the angiotensin II receptor and the μ opioid receptor have progressed to clinical trials and are promising in regard to selective activation of signaling pathways that can be linked to beneficial clinical outcomes. Dualsteric/bitopic hybrid compounds which consist of at least two pharmacophores combined in one single ligand are more recent examples for functionally selective ligands...
December 24, 2016: Current Opinion in Pharmacology
https://www.readbyqxmd.com/read/28026967/identification-of-molecular-targets-for-4-5-dichloro-2-n-octyl-4-isothiazolin-3-one-dcoit-in-teleosts-new-insight-into-mechanism-of-toxicity
#18
Lianguo Chen, Doris W T Au, Chenyan Hu, Drew R Peterson, Bingsheng Zhou, Pei-Yuan Qian
Environmental pollutants are capable of concomitantly inducing diverse toxic effects. However, it is largely unknown which effects are directly induced and which effects are secondary, thus calling for definitive identification of the initiating molecular event for a pollutant to elucidate the mechanism of toxicity. In present study, affinity pull-down assays were used to identify target proteins for 4,5-dichloro-2-n-octyl-4-isothiazolin-3-one (DCOIT), a costal pollutant of emerging concern, in various tissues (e...
December 27, 2016: Environmental Science & Technology
https://www.readbyqxmd.com/read/28025563/novel-structural-approaches-to-study-gpcr-regulation
#19
REVIEW
Marco A Alfonzo-Méndez, Rocío Alcántara-Hernández, J Adolfo García-Sáinz
BACKGROUND: Upon natural agonist or pharmacological stimulation, G protein-coupled receptors (GPCRs) are subjected to posttranslational modifications, such as phosphorylation and ubiquitination. These posttranslational modifications allow protein-protein interactions that turn off and/or switch receptor signaling as well as trigger receptor internalization, recycling or degradation, among other responses. Characterization of these processes is essential to unravel the function and regulation of GPCR...
December 23, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28018974/hypoxia-sensing-through-%C3%AE-adrenergic-receptors
#20
Hoi I Cheong, Kewal Asosingh, Olivia R Stephens, Kimberly A Queisser, Weiling Xu, Belinda Willard, Bo Hu, Josephine Kam Tai Dermawan, George R Stark, Sathyamangla V Naga Prasad, Serpil C Erzurum
Life-sustaining responses to low oxygen, or hypoxia, depend on signal transduction by HIFs, but the underlying mechanisms by which cells sense hypoxia are not completely understood. Based on prior studies suggesting a link between the β-adrenergic receptor (β-AR) and hypoxia responses, we hypothesized that the β-AR mediates hypoxia sensing and is necessary for HIF-1α accumulation. Beta blocker treatment of mice suppressed hypoxia induction of renal HIF-1α accumulation, erythropoietin production, and erythropoiesis in vivo...
December 22, 2016: JCI Insight
keyword
keyword
63996
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"