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G protein coupled receptor

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https://www.readbyqxmd.com/read/28231302/bioinformatic-prediction-of-g-protein-coupled-receptor-encoding-sequences-from-the-transcriptome-of-the-foreleg-including-the-haller-s-organ-of-the-cattle-tick-rhipicephalus-australis
#1
Sergio Munoz, Felix D Guerrero, Anastasia Kellogg, Andrew M Heekin, Ming-Ying Leung
The cattle tick of Australia, Rhipicephalus australis, is a vector for microbial parasites that cause serious bovine diseases. The Haller's organ, located in the tick's forelegs, is crucial for host detection and mating. To facilitate the development of new technologies for better control of this agricultural pest, we aimed to sequence and annotate the transcriptome of the R. australis forelegs and associated tissues, including the Haller's organ. As G protein-coupled receptors (GPCRs) are an important family of eukaryotic proteins studied as pharmaceutical targets in humans, we prioritized the identification and classification of the GPCRs expressed in the foreleg tissues...
2017: PloS One
https://www.readbyqxmd.com/read/28230370/coarse-grained-prediction-of-peptide-binding-to-g-protein-coupled-receptors
#2
Bartholomé Delort, Pedro Renault, Landry Charlier, Florent Raussin, Jean Martinez, Nicolas Floquet
In this study, we used the Martini Coarse-Grained model with no applied restraints to predict the binding mode of some peptides to G-Protein Coupled Receptors (GPCRs). Both the Neurotensin-1 and the chemokine CXCR4 receptors were used as test cases. Their ligands, NTS8-13 and CVX15 peptides, respectively, were initially positioned in the surrounding water box. Using a protocol based on Replica Exchange Molecular Dynamics (REMD), both opening of the receptors and entry of the peptides into their dedicated pockets were observed on the μs time-scale...
February 23, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28229904/regulation-of-g-protein-coupled-receptor-signalling-underpinning-neurobiology-of-mood-disorders-and-depression
#3
Dimitris K Grammatopoulos
G-protein coupled receptors (GPCRs) have long been at the centre of investigations of the neurobiology of depression and mood disorders. Different facets of GPCR signalling pathways, including those controlling monoaminergic and neuropeptidergic hormonal systems are believed to be dysregulated in major depressive and bipolar disorders. Although these receptors are key molecular targets for a variety of therapeutic agents and continue to be the focus of intense pharmaceutical development, the molecular mechanisms activated by these GPCRs and underpin the pathological basis of mood disorders remain poorly understood...
February 13, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28228611/anti-diabetic-action-of-all-trans-retinoic-acid-and-the-orphan-g-protein-coupled-receptor-gprc5c-in-pancreatic-%C3%AE-cells
#4
Stefan Amisten, Israa Mohammad Al-Amily, Arvind Soni, Ross Hawkes, Patricio Atanes, Shanta Jean Persaud, Patrik Rorsman, Albert Salehi
Pancreatic islets express high levels of the orphan G-protein coupled receptor C5C (GPRC5C), the function of which remains to be established. Here we have examined the role of GPRC5C in the regulation of insulin secretion and β-cell survival and proliferation using human and mouse pancreatic islets. The expression of GPRC5C was analysed by RNA-sequencing, qPCR, western blotting and confocal microscopy. Insulin secretion and cell viability were determined by RIA and MTS assays, respectively. GPRC5C mRNA expression and protein level were reduced in the islets from type-2 diabetic donors...
February 22, 2017: Endocrine Journal
https://www.readbyqxmd.com/read/28228552/core-engagement-with-%C3%AE-arrestin-is-dispensable-for-agonist-induced-vasopressin-receptor-endocytosis-and-erk-activation
#5
Punita Kumari, Ashish Srivastava, Eshan Ghosh, Ravi Ranjan, Shalini Dogra, Prem N Yadav, Arun K Shukla
G Protein-Coupled Receptors (GPCRs) exhibit highly conserved activation and signaling mechanisms where agonist stimulation leads to coupling of heterotrimeric G proteins and generation of second messenger response. This is followed by receptor phosphorylation, primarily in the carboxyl-terminus but also in the cytoplasmic loops, and subsequent binding of arrestins. GPCRs typically recruit arrestins through two different set of interactions, one involving phosphorylated receptor tail and the other mediated by the receptor core...
February 22, 2017: Molecular Biology of the Cell
https://www.readbyqxmd.com/read/28228527/activation-mechanism-of-the-g-protein-coupled-sweet-receptor-heterodimer-with-sweeteners-and-allosteric-agonists
#6
Soo-Kyung Kim, Yalu Chen, Ravinder Abrol, William A Goddard, Brian Guthrie
The sweet taste in humans is mediated by the TAS1R2/TAS1R3 G protein-coupled receptor (GPCR), which belongs to the class C family that also includes the metabotropic glutamate and γ-aminobutyric acid receptors. We report here the predicted 3D structure of the full-length TAS1R2/TAS1R3 heterodimer, including the Venus Flytrap Domains (VFDs) [in the closed-open (co) active conformation], the cysteine-rich domains (CRDs), and the transmembrane domains (TMDs) at the TM56/TM56 interface. We observe that binding of agonists to VFD2 of TAS1R2 leads to major conformational changes to form a TM6/TM6 interface between TMDs of TAS1R2 and TAS1R3, which is consistent with the activation process observed biophysically on the metabotropic glutamate receptor 2 homodimer...
February 22, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28227365/integrated-quantification-based-on-confocal-imaging-cell-crowding-modulates-heterogeneity-in-gpcr-mediated-calcium-oscillation
#7
Jophin G Joseph, S Nanda, S Vennamalla, G Bhure, Ranjana Singh, Soumya Jana, Lopamudra Giri, Jophin G Joseph, S Nanda, S Vennamalla, G Bhure, Ranjana Singh, Soumya Jana, Lopamudra Giri, Soumya Jana, Lopamudra Giri, Jophin G Joseph, S Nanda, Ranjana Singh, G Bhure, S Vennamalla
Results from single cell imaging, facilitated by high resolution microscopy, have demonstrated cell-to-cell variability within the same cell population in contexts ranging from cell growth to cell migration. Recent studies suggest that such variability conveys important information about diseased states. However, manual analysis and interpretation of heterogeneous calcium oscillation based on time-lapsed images, as practiced today, is tedious, and essentially infeasible for large datasets. As a practical alternative, we present an integrated platform that includes calcium imaging using confocal microscope, algorithmic cell segmentation, and statistical analysis...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28223965/central-control-of-feeding-behavior-by-the-secretin-pacap-and-glucagon-family-of-peptides
#8
REVIEW
Revathi Sekar, Lei Wang, Billy Kwok Chong Chow
Constituting a group of structurally related brain-gut peptides, secretin (SCT), pituitary adenylate cyclase-activating peptide (PACAP), and glucagon (GCG) family of peptide hormones exert their functions via interactions with the class B1 G protein-coupled receptors. In recent years, the roles of these peptides in neuroendocrine control of feeding behavior have been a specific area of research focus for development of potential therapeutic drug targets to combat obesity and metabolic disorders. As a result, some members in the family and their analogs have already been utilized as therapeutic agents in clinical application...
2017: Frontiers in Endocrinology
https://www.readbyqxmd.com/read/28223834/bile-salt-receptor-tgr5-is-highly-expressed-in-esophageal-adenocarcinoma-and-precancerous-lesions-with-significantly-worse-overall-survival-and-gender-differences
#9
Chunhong Pang, Amy LaLonde, Tony E Godfrey, Jianwen Que, Jun Sun, Tong Tong Wu, Zhongren Zhou
Bile acid reflux in the esophagus plays an important role in the carcinogenesis of esophageal adenocarcinoma (EAC). The G-protein coupled bile acid receptor (TGR5) has been associated with the development of gastrointestinal cancer. However, little is known regarding the role of TGR5 in esophageal carcinoma and precancerous lesions. We analyzed genomic DNA from 116 EACs for copy number aberrations via Affymetrix SNP6.0 microarrays. The TGR5 gene locus was amplified in 12.7% (14/116) of the EACs. The TGR5 protein expression was also assessed using immunohistochemistry from tissue microarrays, including Barrett's esophagus (BE), low-(LGD) and high-grade dysplasia (HGD), columnar cell metaplasia (CM), squamous epithelium (SE), EAC and squamous cell carcinoma...
2017: Clinical and Experimental Gastroenterology
https://www.readbyqxmd.com/read/28223719/hepatitis-c-virus-associated-pruritus-etiopathogenesis-and-therapeutic-strategies
#10
EDITORIAL
Youssef Alhmada, Denis Selimovic, Fadi Murad, Sarah-Lilly Hassan, Youssef Haikel, Mossaad Megahed, Matthias Hannig, Mohamed Hassan
In addition to its contributing role in the development of chronic liver diseases, chronic hepatitis C virus (HCV) infection is associated with extrahepatic manifestations, particularly, cutaneous-based disorders including those with pruritus as a symptom. Pruritus is frequently associated with the development of chronic liver diseases such as cholestasis and chronic viral infection, and the accumulation of bile acids in patients' sera and tissues as a consequence of liver damage is considered the main cause of pruritus...
February 7, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/28223697/dynamic-regulation-of-gdp-binding-to-g-proteins-revealed-by-magnetic-field-dependent-nmr-relaxation-analyses
#11
Yuki Toyama, Hanaho Kano, Yoko Mase, Mariko Yokogawa, Masanori Osawa, Ichio Shimada
Heterotrimeric guanine-nucleotide-binding proteins (G proteins) serve as molecular switches in signalling pathways, by coupling the activation of cell surface receptors to intracellular responses. Mutations in the G protein α-subunit (Gα) that accelerate guanosine diphosphate (GDP) dissociation cause hyperactivation of the downstream effector proteins, leading to oncogenesis. However, the structural mechanism of the accelerated GDP dissociation has remained unclear. Here, we use magnetic field-dependent nuclear magnetic resonance relaxation analyses to investigate the structural and dynamic properties of GDP bound Gα on a microsecond timescale...
February 22, 2017: Nature Communications
https://www.readbyqxmd.com/read/28223679/synthesis-and-ability-of-new-ligands-for-g-protein-coupled-receptors-17-gpr17
#12
Tongyou Zhuo, Shengxue Zhou, Wei Zhang, Catia Lambertucci, Rosaria Volpini
GPR17 is believed to be a novel target for the development of new therapeutic approaches to human stroke and multiple sclerosis. Hence, the selection of GPR17 ligands may be a potent way to reduce the progression of ischemic damage. New potential ligands for GPR17, mono-, di-, and triphosphate adenosine nucleotides substituted at N6-position with a methyl and a cyclopentyl group were synthesized. The ability of new ligands to bind GPR17 was evaluated using frontal affinity chromatography-mass spectrometry (FAC-MS) method...
February 22, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28223524/distinct-conformations-of-gpcr-%C3%AE-arrestin-complexes-mediate-desensitization-signaling-and-endocytosis
#13
Thomas J Cahill, Alex R B Thomsen, Jeffrey T Tarrasch, Bianca Plouffe, Anthony H Nguyen, Fan Yang, Li-Yin Huang, Alem W Kahsai, Daniel L Bassoni, Bryant J Gavino, Jane E Lamerdin, Sarah Triest, Arun K Shukla, Benjamin Berger, John Little, Albert Antar, Adi Blanc, Chang-Xiu Qu, Xin Chen, Kouki Kawakami, Asuka Inoue, Junken Aoki, Jan Steyaert, Jin-Peng Sun, Michel Bouvier, Georgios Skiniotis, Robert J Lefkowitz
β-Arrestins (βarrs) interact with G protein-coupled receptors (GPCRs) to desensitize G protein signaling, to initiate signaling on their own, and to mediate receptor endocytosis. Prior structural studies have revealed two unique conformations of GPCR-βarr complexes: the "tail" conformation, with βarr primarily coupled to the phosphorylated GPCR C-terminal tail, and the "core" conformation, where, in addition to the phosphorylated C-terminal tail, βarr is further engaged with the receptor transmembrane core...
February 21, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28223516/targeting-human-mas-related-g-protein-coupled-receptor-x1-to-inhibit-persistent-pain
#14
Zhe Li, Pang-Yen Tseng, Vinod Tiwari, Qian Xu, Shao-Qiu He, Yan Wang, Qin Zheng, Liang Han, Zhiping Wu, Anna L Blobaum, Yiyuan Cui, Vineeta Tiwari, Shuohao Sun, Yingying Cheng, Julie H Y Huang-Lionnet, Yixun Geng, Bo Xiao, Junmin Peng, Corey Hopkins, Srinivasa N Raja, Yun Guan, Xinzhong Dong
Human Mas-related G protein-coupled receptor X1 (MRGPRX1) is a promising target for pain inhibition, mainly because of its restricted expression in nociceptors within the peripheral nervous system. However, constrained by species differences across Mrgprs, drug candidates that activate MRGPRX1 do not activate rodent receptors, leaving no responsive animal model to test the effect on pain in vivo. Here, we generated a transgenic mouse line in which we replaced mouse Mrgprs with human MrgprX1 This humanized mouse allowed us to characterize an agonist [bovine adrenal medulla 8-22 (BAM8-22)] and a positive allosteric modulator (PAM), ML382, of MRGPRX1...
February 21, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28223438/dysregulated-gpcr-signaling-and-therapeutic-options-in-uveal-melanoma
#15
Vivian Chua, Dominic Lapadula, Clinita Randolph, Jeffrey L Benovic, Philip Wedegaertner, Andrew E Aplin
: Uveal melanoma (UM) is the most common primary intraocular malignant tumor in adults and arises from the transformation of melanocytes in the uveal tract. Even after treatment of the primary tumor, up to 50% of patients succumb to metastatic disease. The liver is the predominant organ of metastasis. There is an important need to provide effective treatment options for advanced stage UM. In order to provide the preclinical basis for new treatments, it is important to understand the molecular underpinnings of the disease...
February 21, 2017: Molecular Cancer Research: MCR
https://www.readbyqxmd.com/read/28223150/roles-of-g-protein-coupled-estrogen-receptor-gper-in-metabolic-regulation
#16
Geetanjali Sharma, Franck Mauvais-Jarvis, Eric R Prossnitz
Metabolic homeostasis is differentially regulated in males and females. The lower incidence of obesity and associated diseases in pre-menopausal females points towards the beneficial role of the predominant estrogen, 17β-estradiol (E2). The actions of E2 are elicited by nuclear and extra-nuclear estrogen receptor (ER) α and ERβ, as well as the G protein-coupled estrogen receptor (GPER, previously termed GPR30). The roles of GPER in the regulation of metabolism are only beginning to emerge and much remains unclear...
February 18, 2017: Journal of Steroid Biochemistry and Molecular Biology
https://www.readbyqxmd.com/read/28223044/7x7-rmsd-matrix-a-new-method-for-quantitative-comparison-of-the-transmembrane-domain-structures-in-the-g-protein-coupled-receptors
#17
Ting Wang, Yang Wang, Leihan Tang, Yong Duan, Haiguang Liu
The G-protein coupled receptors (GPCRs) share a conserved heptahelical fold in the transmembrane (TM) region, but the exact arrangements of the seven TM helices vary with receptors and their activation states. The differences or the changes have been observed in the experimentally solved structures, but have not been systematically and quantitatively investigated due to lack of suitable methods. In this work, we describe a novel method, called 7x7 RMSD matrix that is proposed specifically for comparing the characteristic 7TM bundle structures of GPCRs...
February 18, 2017: Journal of Structural Biology
https://www.readbyqxmd.com/read/28220900/membrane-cholesterol-access-into-a-g-protein-coupled-receptor
#18
Ramon Guixà-González, José L Albasanz, Ismael Rodriguez-Espigares, Manuel Pastor, Ferran Sanz, Maria Martí-Solano, Moutusi Manna, Hector Martinez-Seara, Peter W Hildebrand, Mairena Martín, Jana Selent
Cholesterol is a key component of cell membranes with a proven modulatory role on the function and ligand-binding properties of G-protein-coupled receptors (GPCRs). Crystal structures of prototypical GPCRs such as the adenosine A2A receptor (A2AR) have confirmed that cholesterol finds stable binding sites at the receptor surface suggesting an allosteric role of this lipid. Here we combine experimental and computational approaches to show that cholesterol can spontaneously enter the A2AR-binding pocket from the membrane milieu using the same portal gate previously suggested for opsin ligands...
February 21, 2017: Nature Communications
https://www.readbyqxmd.com/read/28220785/c-edge-loops-of-arrestin-function-as-a-membrane-anchor
#19
Ciara C M Lally, Brian Bauer, Jana Selent, Martha E Sommer
G-protein-coupled receptors are membrane proteins that are regulated by a small family of arrestin proteins. During formation of the arrestin-receptor complex, arrestin first interacts with the phosphorylated receptor C terminus in a pre-complex, which activates arrestin for tight receptor binding. Currently, little is known about the structure of the pre-complex and its transition to a high-affinity complex. Here we present molecular dynamics simulations and site-directed fluorescence experiments on arrestin-1 interactions with rhodopsin, showing that loops within the C-edge of arrestin function as a membrane anchor...
February 21, 2017: Nature Communications
https://www.readbyqxmd.com/read/28220211/competitive-association-binding-kinetic-assays-a-new-tool-to-detect-two-different-binding-orientations-of-a-ligand-to-its-target-protein-under-distinct-conditions
#20
Hans-Joachim Wittmann, Andrea Strasser
Within the last years, for several ligands, binding to G protein-coupled receptors or other target proteins, a binding of the ligand in two different orientations is described. One appropriate experimental technique to detect two different binding orientations is the crystallization of the ligand-protein-complex, but crystallization and subsequent X-ray analysis do not belong to the routine methods. By traditional competitive radioligand equilibrium binding assays, it is not possible to detect or to distinguish between two different binding orientations, but there is a possibility to identify two different binding orientations by performing kinetic competitive radioligand-binding assays...
February 20, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
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