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Receptors, G-Protein-Coupled (45):
  • Receptors, Muscarinic
  • Receptors, Lysophospholipid
  • Receptors, FSH
  • Receptors, Formyl Peptide
  • Receptors, Corticotropin-Releasing Hormone
  • Receptors, Calcium-Sensing
  • Receptors, Angiotensin
  • Receptors, Pheromone
  • Receptors, Serotonin
  • Receptors, Purinergic
  • Receptors, Vasoactive Intestinal Peptide
  • Receptors, Somatostatin
  • Receptors, Oxytocin
  • Receptors, Opioid
  • Receptors, Neurotensin
  • Receptors, Galanin
  • Receptors, Endothelin
  • Receptors, Glucagon
  • Receptors, Cholecystokinin
  • Receptors, Bradykinin
  • Receptors, Parathyroid Hormone
  • Receptors, Metabotropic Glutamate
  • Rhodopsin
  • Receptors, Pituitary Adenylate Cyclase-Activating Polypeptide
  • Receptors, Melatonin
  • Receptors, Cannabinoid
  • Receptors, Calcitonin Gene-Related Peptide
  • Receptors, Bombesin
  • Receptors, Vasopressin
  • Receptors, Thrombin
  • Receptors, Odorant
  • Receptors, Ghrelin
  • Receptors, Chemokine
  • Receptors, Calcitonin
  • Receptors, Neuropeptide Y
  • Receptors, GABA-B
  • Receptors, Melanocortin
  • Receptors, LHRH
  • Receptors, Eicosanoid
  • Receptors, Catecholamine
  • Receptors, LH
  • Receptors, Histamine H2
  • Receptors, Histamine H1
  • Receptor, PAR-2
  • Receptor, Anaphylatoxin C5a
Home > Amino Acids, Peptides, and Proteins > Proteins > Membrane Proteins > Receptors, Cell Surface > Receptors, G-Protein-Coupled

Recent article

Receptors, G-Protein-Coupled

Molecular Systems Biology (7) 2011
Arabidopsis G-protein interactome reveals connections to cell wall carbohydrates and morphogenesis
Karsten Klopffleisch, Nguyen Phan, Kelsey Augustin, Robert S Bayne, Katherine S Booker, Jose R Botella, Nicholas C Carpita, Tyrell Carr, Jin-Gui Chen, Thomas Ryan Cooke, Arwen Frick-Cheng, Erin J Friedman, Brandon Fulk, Michael G Hahn, Kun Jiang, Lucia Jorda, Lydia Kruppe, Chenggang Liu, Justine Lorek, Maureen C McCann, Antonio Molina, Etsuko N Moriyama, M Shahid Mukhtar, Yashwanti Mudgil, Sivakumar Pattathil, John Schwarz, Steven Seta, Matthew Tan, Ulrike Temp, Yuri Trusov, Daisuke Urano, Bastian Welter, Jing Yang, Ralph Panstruga, Joachim F Uhrig and Alan M Jones
Abstract
We screened a set of proteins from the G-protein complex using two-hybrid complementation in yeast. After deep and exhaustive interrogation, we detected 544 interactions between 434 proteins, of which 68 highly interconnected proteins form the core G-protein interactome. Within this core, over half... | PMID: 21952135

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Journal of Chemical Information and Modeling (51)8 2011
G-protein coupled receptors virtual screening using genetic algorithm focused chemical space.
Carleton Sage, Runtong Wang and Gareth Jones
Abstract
We sought to develop an appropriate method to examine large sets of GPCR ligand information for both screening collection enhancement and hit expansion. To this end, we have implemented a modified version of BDACCS that removes highly correlated descriptors (rBDACCS). To test the hypothesis that a s... | PMID: 21761904

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Journal of Laboratory Automation (16)4 2011
G protein-coupled receptor heteromer identification technology: identification and profiling of GPCR heteromers.
Sanam Mustafa and Kevin D G Pfleger
Abstract
Traditionally, G protein-coupled receptors (GPCRs) were thought to function as monomeric units activating linear signaling pathways to reach a single functional response. However, it is now recognized that GPCRs can exist as higher order structures, such as homomers or heteromers. Th... | PMID: 21764024

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Nature Chemical Biology (7)8 2011
Receptors: clicking class B GPCR ligands.
Thomas P Sakmar
Abstract
PMID: 21769095

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Cancer Biology & Therapy (12)1 2011
Role of GPER/GPR30 in tumoral testicular germ cells proliferation.
Nicolas Chevalier, Adil Bouskine and Patrick Fenichel
Abstract
We agree with this hypothesis and would like to highlight here some published results supporting this hypothesis and give some details concerning the role of estrogens and xeno-estrogens in testicular carcinogenesis and the effects of GPER antagonist in human seminoma cells. We are sure that this in... | PMID: 21508670

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Cancer Cell (19)6 2011
PI3Kγ mediates kaposi's sarcoma-associated herpesvirus vGPCR-induced sarcomagenesis.
Daniel Martin, Rebeca Galisteo, Alfredo A Molinolo, Reinhard Wetzker, Emilio Hirsch and J Silvio Gutkind
Abstract
We explored whether KSHV oncogenes deploy cell type-specific signaling pathways activating mTOR, which could be exploited to halt KS development while minimizing immune suppressive effects. We found that PI3Kγ, a PI3K isoform exhibiting restricted tissue distribution, is strictly required for signa... | PMID: 21665152

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Chemmedchem (6)6 2011
Design strategies for bivalent ligands targeting GPCRs.
Jeremy Shonberg, Peter J Scammells and Ben Capuano
Abstract
Specifically designed bivalent ligands targeting G protein-coupled receptor (GPCR) dimeric structures have become increasingly popular in recent literature. The advantages of the bivalent approach are numerous, including enhanced potency and receptor subtype specificity. However, t... | PMID: 21520422

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Chemmedchem (6)6 2011
Discovery of a competitive apelin receptor (APJ) antagonist.
N J Maximilian Macaluso, Sarah L Pitkin, Janet J Maguire, Anthony P Davenport and Robert C Glen
Abstract
We report the design and discovery of a novel APJ antagonist. By using a bivalent ligand approach, we have designed compounds with two 'affinity' motifs and a short series of linker groups with different conformational and non-bonded interaction properties. One of these, cyclo(1-6)CRPRLC-KH-cyclo(9-... | PMID: 21560248

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Nature Reviews Endocrinology (7)6 2011
G protein-coupled receptors: mutations and endocrine diseases.
Gilbert Vassart and Sabine Costagliola
Abstract
Over the past 20 years, naturally occurring mutations that affect G protein-coupled receptors (GPCRs) have been identified, mainly in patients with endocrine diseases. The study of loss-of-function or gain-of-function mutations has contributed to our understanding of the pathophysiol... | PMID: 21301490

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Clinical and Translational Science (4)3 2011
Bile acids regulate cardiovascular function.
Sandeep Khurana, Jean-Pierre Raufman and Thomas L Pallone
Abstract
We provide a comprehensive review of the actions of BAs on cardiovascular function. In the heart and the systemic circulation, BAs interact with plasma membrane G-protein-coupled receptors, for example, TGR5 and muscarinic receptors, and nuclear receptors, for example, the farnesoid (FXR) and pregna... | PMID: 21707953

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Journal of Proteome Research (10)5 2011
Identification and relative quantitation of an orphan G-protein coupled receptor SREB2 (GPR85) protein in tissue using a linear ion trap mass spectrometer.
Masatoshi Yuri, Masashi Hiramoto, Masanori Naito, Mitsuyuki Matsumoto, Shun-ichiro Matsumoto, Shuji Morita, Keitaro Mori, Hiroyuki Yokota and Toshio Teramura
Abstract
We previously prepared a SREB2-overexpressing transgenic mouse for functional analysis but were unable to confirm SREB2 protein expression level by immunochemical or biochemical methods. In this article, we report mass spectrometric identification and relative quantitative analysis of SREB2 in the f... | PMID: 21395347

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Nature Chemical Biology (7)5 2011
Signaling: retromer arrests receptor on the run.
Jan R T van Weering and Peter J Cullen
Abstract
PMID: 21502946

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Chemical Biology & Drug Design (77)5 2011
CoMSIA study on substituted aryl alkanoic acid analogs as GPR40 agonists.
Aaditya Bhatt, Pallav D Patel, Maulik R Patel, Satyakam Singh, Cesar A Lau-Cam and Tanaji T Talele
Abstract
GPR40, a G-protein-coupled receptor has been well established to play a crucial role in regulating blood glucose levels. Hence, GPR40 is a potential target for future antidiabetic agents. The present 3D QSAR study is aimed at delineating structural parameters governing GPR40 agonisti... | PMID: 21352503

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Cancer Biology & Therapy (11)8 2011
Role of GPR30 in testicular germ cell tumors: a potential new anticancer target.
Giovanni Vitale, Alessandra Dicitore, Giovanna Sciortino, Alberto Abbruzzese, Luca Persani and Daniele Santini
Abstract
PMID: 21372633

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Nature (472)7341 2011
Reproductive biology: bone returns the favour.
Sonya M Schuh-Huerta and Renee A Reijo Pera
Abstract
PMID: 21475191

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Biochimica et Biophysica Acta (1812)4 2011
Tumor necrosis factor-alpha regulates the Hypocretin system via mRNA degradation and ubiquitination.
Shuqin S Zhan, Guo-Qiang GQ Cai, Anni A Zheng, Yuping Y Wang, Jianping J Jia, Haotian H Fang, Youfeng Y Yang, Meng M Hu and Qiang Q Ding
Abstract
We test our hypothesis that the Hypocretin system is regulated by TNF-α. Prepro-Hypocretin and Hypocretin receptor 2 (HcrtR2) can be detected at a very low level in rat B35 neuroblastoma cells. In response to TNF-α, Prepro-Hypocretin mRNA and protein levels are down-regulated, and also HcrtR2 prot... | PMID: 21094253

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International journal of clinical and experimental pathology (4)4 2011
Expression of the adult intestinal stem cell marker Lgr5 in the metastatic cascade of colorectal cancer.
Britta Kleist, Li Xu, Guojun Li and Christian Kersten
Abstract
We evaluated immunohistochemical Lgr5 expression in 31 distant metastases and in primary tumor compartments with relevance for metastasizing, comprising 89 colorectal carcinomas. Lgr5 expression was seen in 51.6% of distant metastases. 12.9%, 14.8% and 26.7% of primary tumors with histologically con... | PMID: 21577318

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Developmental Cell (20)3 2011
Rspo3 binds syndecan 4 and induces Wnt/PCP signaling via clathrin-mediated endocytosis to promote morphogenesis.
Bisei Ohkawara, Andrei Glinka and Christof Niehrs
Abstract
The R-Spondin (Rspo) family of secreted Wnt modulators is involved in development and disease and holds therapeutic promise as stem cell growth factors. Despite growing biological importance, their mechanism of action is poorly understood. Here, we show that Rspo3 binds syndecan 4 (... | PMID: 21397842

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Developmental Cell (20)3 2011
Rspo3 binds syndecan 4 and induces Wnt/PCP signaling via clathrin-mediated endocytosis to promote morphogenesis.
Bisei Ohkawara, Andrei Glinka and Christof Niehrs
Abstract
The R-Spondin (Rspo) family of secreted Wnt modulators is involved in development and disease and holds therapeutic promise as stem cell growth factors. Despite growing biological importance, their mechanism of action is poorly understood. Here, we show that Rspo3 binds syndecan 4 (... | PMID: 21397842

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Organic Letters (13)5 2011
Enantioselective synthesis of a GPR40 agonist AMG 837 via catalytic asymmetric conjugate addition of terminal alkyne to α,β-unsaturated thioamide.
Ryo Yazaki, Naoya Kumagai and Masakatsu Shibasaki
Abstract
A concise enantioselective synthetic route to a potent GPR40 agonist AMG 837 is described. The crucial catalytic asymmetric conjugate addition of terminal alkyne was promoted by a soft Lewis acid/hard Brønsted base cooperative catalyst, allowing efficient construction of the requisi... | PMID: 21291204

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Genes, Brain and Behavior (10)2 2011
Contribution of LPHN3 to the genetic susceptibility to ADHD in adulthood: a replication study.
M Ribasés, J A Ramos-Quiroga, C Sánchez-Mora, R Bosch, V Richarte, G Palomar, X Gastaminza, A Bielsa, M Arcos-Burgos, M Muenke, F X Castellanos, B Cormand, M Bayés and M Casas
Abstract
We undertook a case-control association study in 334 adult patients with ADHD and 334 controls with 43 single nucleotide polymorphisms (SNPs) covering the LPNH3 gene. Single- and multiple-marker analyses showed additional evidence of association between LPHN3 and combined type ADHD in adulthood [P =... | PMID: 21040458

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Molecular Systems Biology (7) 2011
Analysis of multiple compound–protein interactions reveals novel bioactive molecules
Hiroaki Yabuuchi, Satoshi Niijima, Hiromu Takematsu, Tomomi Ida, Takatsugu Hirokawa, Takafumi Hara, Teppei Ogawa, Yohsuke Minowa, Gozoh Tsujimoto and Yasushi Okuno
Abstract
We demonstrate that machine learning of multiple CPIs can not only assess drug polypharmacology but can also efficiently identify novel bioactive scaffold-hopping compounds. Through a machine-learning technique that uses multiple CPIs, we have successfully identified novel lead compounds for two pha... | PMID: 21364574

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Respiratory Physiology & Neurobiology (175)2 2011
Functional characterization of heterotrimeric G-proteins in rat diaphragm muscle.
Ana Luiza Andrade-Lopes, Marcelo Pires-Oliveira, Francisco Sandro Menezes-Rodrigues and Rosely Oliveira Godinho
Abstract
We evaluate the expression and activation of rat diaphragm or cultured skeletal muscle G-proteins using [(35)S]GTPγS. Total membrane Gα subunit content was 4-7 times higher in rat primary cultured myotubes and L6 cell line than in diaphragm (32.6±1.2fmol/mg protein) and 7-27% of them were in the... | PMID: 21084061

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YAKUGAKU ZASSHI (131)2 2011
[Roles of histamine in the exacerbated allergic dermatitis].
Noriyasu N Hirasawa and Kazuo K Ohuchi
Abstract
We established a novel dermatitis model in mice earlobes and analyzed the roles of histamine using specific antagonists for histamine receptors. After sensitization with picryl chloride (PiCl) by painting it on the earlobes of cyclophosphamide-treated mice, 12-O-tetradecanoylphorbol 13-acetate (TPA)... | PMID: 21297358

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Pigment Cell & Melanoma Research (24)1 2011
Quantitative expression profiling of G-protein-coupled receptors (GPCRs) in metastatic melanoma: the constitutively active orphan GPCR GPR18 as novel drug target.
Y Qin, E M E Verdegaal, M Siderius, J P Bebelman, M J Smit, R Leurs, R Willemze, C P Tensen and S Osanto
Abstract
We quantified expression of 94 human GPCRs, including 75 orphan GPCRs and 19 chemokine receptors, and 36 chemokine ligands, in 40 melanoma metastases from different individuals and benign nevi. Inter-metastatic site comparison revealed that orphan GPR174 and CCL28 are statistically significantly ove... | PMID: 20880198

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Assay and Drug Development Technologies (9)1 2011
Application of G protein-coupled receptor-heteromer identification technology to monitor β-arrestin recruitment to G protein-coupled receptor heteromers.
Heng B See, Ruth M Seeber, Martina Kocan, Karin A Eidne and Kevin D G Pfleger
Abstract
Understanding the role of G protein-coupled receptor (GPCR; also known as a 7 transmembrane receptor) heteromerization in the physiology and pathophysiology of cellular function has now become a major research focus. However, there is currently a lack of cell-based assays capable of... | PMID: 21133678

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Current Allergy & Asthma Reports (11)1 2011
The role of the histamine H4 receptor in atopic dermatitis.
Susanne Mommert, Maria Gschwandtner, Ralf Gutzmer and Thomas Werfel
Abstract
We describe a possible genetic impact on the expression level of the histamine H4 receptor and summarize the current data regarding the activity of the histamine H4 receptor on the key effector cells in atopic dermatitis. We do so in the context of whether the histamine H4 receptor offers a novel ta... | PMID: 21104170

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Audio, Transactions of the IRE Professional Group on (6)3 2011
Global array-based transcriptomics from minimal input RNA utilising an optimal RNA isolation process combined with SPIA cDNA probes.
Laura L Kennedy, Mahesh M Pauriah, Valerie V Godfrey, Jacqueline J Howie, Helen H Dennis, Daniel D Crowther, Allan A Struthers, Catharine C Goddard, Giora G Feuerstein, Chim C Lang and Gino G Miele
Abstract
We have established an optimised RNA isolation workflow specifically designed to yield maximal RNA from minimal cell numbers. This procedure obtained RNA yield sufficient for carrying out global transcriptional profiling from vascular endothelial cell biopsies, clinical material not previously amena... | PMID: 21445340

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Audio, Transactions of the IRE Professional Group on (6)3 2011
The zinc transporter SLC39A14/ZIP14 controls G-protein coupled receptor-mediated signaling required for systemic growth.
Shintaro S Hojyo, Toshiyuki T Fukada, Shinji S Shimoda, Wakana W Ohashi, Bum-Ho BH Bin, Haruhiko H Koseki and Toshio T Hirano
Abstract
We report that the cell membrane-localized Zn transporter SLC39A14 controls G-protein coupled receptor (GPCR)-mediated signaling. Mice lacking Slc39a14 (Slc39a14-KO mice) exhibit growth retardation and impaired gluconeogenesis, which are attributable to disrupted GPCR signaling in the growth plate,... | PMID: 21445361

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Science Signaling (4)181 2011
The distinct roles of two GPCRs, MrgprC11 and PAR2, in itch and hyperalgesia.
Qin Liu, Hao-Jui Weng, Kush N Patel, Zongxiang Tang, Haihua Bai, Martin Steinhoff and Xinzhong Dong
Abstract
We show that Mrgprs (Mas-related G protein-coupled receptors), particularly MrgprC11, rather than PAR2 (protease-activated receptor 2) as previously thought, mediate this type of itch. A shorter peptide, SLIGR, which specifically activates PAR2 but not MrgprC11, induced thermal pain hypersensitivity... | PMID: 21775281

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Science Signaling (4)159 2011
The crystal structure of a self-activating G protein alpha subunit reveals its distinct mechanism of signal initiation.
Janice C Jones, Jeffrey W Duffy, Mischa Machius, Brenda R S Temple, Henrik G Dohlman and Alan M Jones
Abstract
We determined its crystal structure. AtGPA1 is structurally similar to animal G protein α subunits, but our crystallographic and biophysical studies revealed that it had distinct properties. Notably, the helical domain of AtGPA1 displayed pronounced intrinsic disorder and a tendency to disengage fr... | PMID: 21304159

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Science Signaling (4)155 2011
Activation state of the M3 muscarinic acetylcholine receptor modulates mammalian odorant receptor signaling.
Yun Rose Li and Hiroaki Matsunami
Abstract
We show that the interaction of ORs with the type 3 muscarinic acetylcholine receptor (M3-R), which is found in olfactory sensory neurons (OSNs), modulated OR responses to cognate odorants. In human embryonic kidney-293T cells, ORs and the M3-R physically interacted, and the M3-R increased the poten... | PMID: 21224444

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Acta Physiologica (201)1 2011
Apelin stimulation of duodenal bicarbonate secretion: feeding-dependent and mediated via apelin-induced release of enteric cholecystokinin.
G Flemström, K Mäkelä, A K Purhonen, M Sjöblom, G Jedstedt, J Walkowiak and K H Herzig
Abstract
We have investigated the effects of apelin peptides on duodenal bicarbonate secretion in vivo and the release of cholecystokinin (CCK) from acutely isolated mucosal cells and the neuroendocrine cell line STC-1. Lewis × Dark Agouti rats had free access to water and, unless fasted ove... | PMID: 20726845

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Acta Physiologica (201)1 2011
Acid sensing by visceral afferent neurones.
P Holzer
Abstract
Acidosis in the gastrointestinal tract can be both a physiological and pathological condition. While gastric acid serves digestion and protection from pathogens, pathological acidosis is associated with defective acid containment, inflammation and ischaemia. The pH in the oesophagus,... | PMID: 20456281

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Acta Physiologica (201)1 2011
Acid sensing by visceral afferent neurones.
P Holzer
Abstract
Acidosis in the gastrointestinal tract can be both a physiological and pathological condition. While gastric acid serves digestion and protection from pathogens, pathological acidosis is associated with defective acid containment, inflammation and ischaemia. The pH in the oesophagus,... | PMID: 20456281

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PLoS ONE (6)8 2011
Sarco/Endoplasmic reticulum Ca2+-ATPases (SERCA) contribute to GPCR-mediated taste perception.
Naoko Iguchi, Tadahiro Ohkuri, Jay P Slack, Ping Zhong and Liquan Huang
Abstract
We sought the molecules involved in [Ca(2+)](c) regulation using a single-taste-cell transcriptome approach. We found that Serca3, a member of the sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA) family that sequesters cytosolic Ca(2+) into endoplasmic reticulum, is exclusively expressed in sweet/u... | PMID: 21829714

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Fetal and Pediatric Pathology (Print Edition) (30)4 2011
Immunohistochemical characterization of sonic hedgehog and its downstream signaling molecules during human penile development.
Bahig M Shehata, James M Elmore, Yasmin Bootwala, Charlotte K Steelman, Jessica B Bare, Carla J Shoffeitt, Ruoxiang Wang, Haiyen E Zhau, Dalin He, Guodong Zhu and Leland W Chung
Abstract
Hypospadias is a common congenital anomalies, yet its molecular basis remains unknown. Recent studies have linked perturbations in the Hedgehog signaling pathway to hypospadias. However, the expression of Sonic hedgehog (Shh) has not been reported during genital development. Immunohi... | PMID: 21434830

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Journal of Biological Chemistry (285)52 2010
ANKRD13C acts as a molecular chaperone for G protein-coupled receptors.
Audrey Parent, Sébastien J Roy, Christian Iorio-Morin, Marie-Claude Lépine, Pascale Labrecque, Maxime A Gallant, Deborah Slipetz and Jean-Luc Parent
Abstract
We have isolated ANKRD13C, a protein of unknown function, as an interacting partner for the DP receptor for prostaglandin D(2). In the present study we report the characterization of this novel protein as a regulator of DP biogenesis and trafficking in the biosynthetic pathway. Co-localization by co... | PMID: 20959461

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Journal of Chemical Information and Modeling (50)12 2010
Ligand-steered modeling and docking: A benchmarking study in class A G-protein-coupled receptors.
Sharangdhar S Phatak, Edgar A Gatica and Claudio N Cavasotto
Abstract
We have enhanced and validated the ligand-steered homology method through cross-modeling and investigated the performance of the thus generated models in docking-based screening. The ligand-steered modeling method uses information about existing ligands to optimize the binding site by accounting for... | PMID: 21080692

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Biochemical and Biophysical Research Communications (403)1 2010
The relationship between GPR40 and lipotoxicity of the pancreatic β-cells as well as the effect of pioglitazone.
Peiwen Wu, Liyong Yang and Ximei Shen
Abstract
These results indicate that GPR40 mediates the short-term effects of FFAs on GSIS, but does not mediate the chronic lipotoxicity on β-cells. The reverse role of pioglitazone on lipotoxicity of β-cells may be related to GPR40. Copyright © 2010 Elsevier Inc. All rights reserved.... | PMID: 21036144

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Chemmedchem (5)12 2010
Redefining the TGR5 triterpenoid binding pocket at the C-3 position.
Cédric Genet, Céline Schmidt, Axelle Strehle, Kristina Schoonjans, Johan Auwerx, Régis Saladin and Alain Wagner
Abstract
PMID: 20979081

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Journal of Endocrinology (207)3 2010
Regulation of pancreatic islet gene expression in mouse islets by pregnancy.
B T Layden, V Durai, M V Newman, A M Marinelarena, C W Ahn, G Feng, S Lin, X Zhang, D B Kaufman, N Jafari, G L Sørensen and W L Lowe
Abstract
Pancreatic β cells adapt to pregnancy-induced insulin resistance by unclear mechanisms. This study sought to identify genes involved in β cell adaptation during pregnancy. To examine changes in global RNA expression during pregnancy, murine islets were isolated at a time point of increased β cell... | PMID: 20847227

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Biochemical and Biophysical Research Communications (402)4 2010
Association of the subunits of the calcium-independent receptor of α-latrotoxin.
Oxana V Serova, Nadezhda V Popova, Alexander G Petrenko and Igor E Deyev
Abstract
We evaluated the amount of p120-p85 complex still presented on the cellular membrane and confirmed that on cell surface major amount of mature CIRL-1 presented as a p120-p85 subunit complex. Copyright © 2010 Elsevier Inc. All rights reserved.... | PMID: 20971062

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Biochemical and Biophysical Research Communications (402)4 2010
The human bitter taste receptor, hTAS2R16, discriminates slight differences in the configuration of disaccharides.
Takanobu Sakurai, Takumi Misaka, Yohei Ueno, Masaji Ishiguro, Shinji Matsuo, Yoshiro Ishimaru, Tomiko Asakura and Keiko Abe
Abstract
We used calcium imaging analysis of human embryonic kidney 293T cells that heterologously expressed human taste receptors to demonstrate that gentiobiose activated hTAS2R16, a bitter taste receptor, but not hT1R2/hT1R3, a sweet taste receptor. In contrast, isomaltose activated hT1R2/hT1R3. As a resu... | PMID: 20965151

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Nature Medicine (16)12 2010
Crippling SWI-SNF makes tumors GLI-ful.
Jeremy F Reiter
Abstract
PMID: 21135845

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Biochemical and Biophysical Research Communications (402)3 2010
Generation and characterization of T1R2-LacZ knock-in mouse.
Ken Iwatsuki, Masatoshi Nomura, Atsushi Shibata, Reiko Ichikawa, Patricio L M Enciso, Lixiang Wang, Ryoichi Takayanagi, Kunio Torii and Hisayuki Uneyama
Abstract
We have generated a T1R2-LacZ reporter knock-in mouse to investigate tissue distribution of T1R2 at a single-cell level. We found that the LacZ gene expression in these mice was faithful to the expression of T1R2 in the taste tissue and in the gastrointestinal tract where T1R3 expression has been re... | PMID: 20965149

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Biochemical and Biophysical Research Communications (402)2 2010
Novel GPR119 agonist AS1535907 contributes to first-phase insulin secretion in rat perfused pancreas and diabetic db/db mice.
Shigeru Yoshida, Takahide Ohishi, Tetsuo Matsui, Hirotsugu Tanaka, Hiroyuki Oshima, Yasuhiro Yonetoku and Masayuki Shibasaki
Abstract
We evaluated the therapeutic potential of a novel small molecule GPR119 agonist, AS1535907, which was modified from the previously identified 2,4,6-tri-substituted pyrimidine core agonist AS1269574. AS1535907 displayed an EC50 value of 4.8 μM in HEK293 cells stably expressing human GPR119 and stimu... | PMID: 20937249

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Science Translational Medicine (2)58 2010
News from the brain: the GPR124 orphan receptor directs brain-specific angiogenesis.
Elisabetta Dejana and Daniel Nyqvist
Abstract
During development, microvessels acquire specialized functions to meet the requirements of different tissues and organs. The vasculature of the brain constitutes one of the best examples of an organ-specific and highly specialized microvasculature, in which the endothelial cells that... | PMID: 21084718

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Bulletin du cancer (97)11 2010
[Cell signalling and cancer].
J Robert
Abstract
We will present here a general classification of the main pathways of cell signalling and some of the recurrent mechanisms used for the transmission of information between cells and inside cells.... | PMID: 21047720

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Journal of Endocrinology (207)2 2010
Evidence for expression of relaxin hormone-receptor system in the boar testis.
Shinichi Kato, Siqin, Itaru Minagawa, Takuya Aoshima, Dai Sagata, Hirokazu Konishi, Keiichiro Yogo, Tatsuo Kawarasaki, Hiroshi Sasada, Hiroshi Tomogane and Tetsuya Kohsaka
Abstract
We characterised the expression pattern and cellular localisation of both RLN and its own receptor LGR7 (RXFP1) in boar testes during postnatal development by molecular and immunological approaches. Testes were collected from Duroc boars, and partial cDNA sequences of the boar homologue of human RXF... | PMID: 20807724

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CNS and Neurological Disorders (9)5 2010
Prime time for G-protein-coupled receptor heteromers as therapeutic targets for CNS disorders: the dopamine D₁-D₃ receptor heteromer.
Sergi Ferré, Carmen Lluis, José Luis Lanciego and Rafael Franco
Abstract
A number of G-protein-coupled receptors (GPCRs) are currently under consideration as potential therapeutic targets for drugs acting in the central nervous system (CNS). Attempts to discover new medications have operated under the assumption that GPCRs are monomers and that a specific... | PMID: 20632968

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CNS and Neurological Disorders (9)5 2010
Trafficking and signaling of G protein-coupled receptors in the nervous system: implications for disease and therapy.
Nigel W Bunnett and Graeme S Cottrell
Abstract
G protein-coupled receptors (GPCRs) are expressed throughout the nervous system where they regulate multiple physiological processes, participate in neurological diseases, and are major targets for therapy. Given that many GPCRs respond to neurotransmitters and hormones that are pres... | PMID: 20632972

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CNS and Neurological Disorders (9)5 2010
Regulation of corticostriatal synaptic plasticity by G protein-coupled receptors.
R López de Maturana and R Sánchez-Pernaute
Abstract
Dopamine modulation of excitatory neurotransmission is critical in the control of movement, emotion and reward. In the striatum, medium size spiny neurons (MSNs) are responsible for the integration of cortical and thalamic information that flows through parallel, partly overlapping,... | PMID: 20632967

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CNS and Neurological Disorders (9)5 2010
Heteromerization of G protein-coupled receptors: relevance to neurological disorders and neurotherapeutics.
Laura Albizu, José L Moreno, Javier González-Maeso and Stuart C Sealfon
Abstract
Because G protein-coupled receptors (GPCRs) are numerous, widely expressed and involved in major physiological responses, they represent a relevant therapeutic target for drug discovery, particularly regarding pharmacological treatments of neurological disorders. Among the biological... | PMID: 20632964

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CNS and Neurological Disorders (9)5 2010
New frontiers in G protein-coupled receptor regulation of neurological disorders.
Stuart Maudsley
Abstract
PMID: 20632974

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Biochemical Journal (432)1 2010
Lysophosphatidylcholines activate G2A inducing G(αi)₋₁-/G(αq/)₁₁- Ca²(+) flux, G(βγ)-Hck activation and clathrin/β-arrestin-1/GRK6 recruitment in PMNs.
Samina Y Khan, Nathan J D McLaughlin, Marguerite R Kelher, Phillip Eckels, Fabia Gamboni-Robertson, Anirban Banerjee and Christopher C Silliman
Abstract
We hypothesize that lyso-PC activation of G2A causes the increases in cytosolic Ca²(+) via release of G(α) and G(βγ) subunits, kinase activation, and the recruitment of clathrin, β-arrestin-1 and GRK6 (G-protein receptor kinase 6) to G2A for signal transduction. PMNs were isolated by standard t... | PMID: 20799926

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PNAS (107)43 2010
Kinetics of G-protein-coupled receptor endosomal trafficking pathways revealed by single quantum dots.
Katye M Fichter, Marc Flajolet, Paul Greengard and Tania Q Vu
Abstract
We show accurate measurement of the internalization and endosomal trafficking of single groups of serotonin (5-hydroxytryptamine, 5-HT) receptors using single quantum dot (QD) probes and quantitative colocalization. We demonstrate that the presence of a QD tag does not interfere with 5-HT receptor i... | PMID: 20940319

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EMBO Journal (29)20 2010
Dishevelled, a Wnt signalling component, is involved in mitotic progression in cooperation with Plk1.
Koji Kikuchi, Yohei Niikura, Katsumi Kitagawa and Akira Kikuchi
Abstract
These results suggested that Dvl2 is involved in mitotic progression by regulating the dynamics of MT plus-ends and the SAC in Plk1-dependent and -independent manners.... | PMID: 20823832

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Plasmid (64)3 2010
The p1D4-hrGFP II expression vector: a tool for expressing and purifying visual pigments and other G protein-coupled receptors.
James M Morrow and Belinda S W Chang
Abstract
We have engineered an expression vector, p1D4-hrGFP II, in order to efficiently express visual pigments in mammalian cell culture. This expression vector is based on pIRES-hrGFP II (Stratagene), with the addition of a C-terminal 1D4 epitope tag for immunoblotting and immunoaffinity purification. Thi... | PMID: 20627111

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British Journal of Cancer (103)8 2010
¹H nuclear magnetic resonance spectroscopy characterisation of metabolic phenotypes in the medulloblastoma of the SMO transgenic mice.
S K Hekmatyar, M Wilson, N Jerome, R M Salek, J L Griffin, A Peet and R A Kauppinen
Abstract
Human medulloblastomas exhibit diverse molecular pathology. Aberrant hedgehog signalling is found in 20-30% of human medulloblastomas with largely unknown metabolic consequences. Transgenic mice over-expressing smoothened (SMO) receptor in granule cell precursors with high incidence of exophytic med... | PMID: 20842126

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