GPBAR1

Summary

Gene Symbol: GPBAR1
Description: G protein-coupled bile acid receptor 1
Alias: BG37, GPCR19, GPR131, M-BAR, TGR5, G-protein coupled bile acid receptor 1, G-protein coupled bile acid receptor BG37, G-protein coupled receptor GPCR19, membrane bile acid receptor, membrane-type receptor for bile acids
Species: human
Products:     GPBAR1

Top Publications

  1. Maruyama T, Miyamoto Y, Nakamura T, Tamai Y, Okada H, Sugiyama E, et al. Identification of membrane-type receptor for bile acids (M-BAR). Biochem Biophys Res Commun. 2002;298:714-9 pubmed
    ..Here we report a novel category of bile acid receptor, a membrane-type G protein-coupled receptor (GPCR), BG37. Bile acids induced rapid and dose-dependent elevation of intracellular cAMP levels in BG37-expressing cells, but ..
  2. Kawamata Y, Fujii R, Hosoya M, Harada M, Yoshida H, Miwa M, et al. A G protein-coupled receptor responsive to bile acids. J Biol Chem. 2003;278:9435-40 pubmed publisher
    ..We found that a novel G protein-coupled receptor, TGR5, is responsive to bile acids as a cell-surface receptor...
  3. Keitel V, Reinehr R, Gatsios P, Rupprecht C, Gorg B, Selbach O, et al. The G-protein coupled bile salt receptor TGR5 is expressed in liver sinusoidal endothelial cells. Hepatology. 2007;45:695-704 pubmed
    ..Whether SEC are responsive to bile salts is unknown. TGR5, a G-protein-coupled bile acid receptor, which triggers cAMP formation, has been discovered recently in macrophages...
  4. Keitel V, Cupisti K, Ullmer C, Knoefel W, Kubitz R, Haussinger D. The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders. Hepatology. 2009;50:861-70 pubmed publisher
    b>TGR5 (Gpbar-1) is a plasma membrane-bound, G protein-coupled receptor for bile acids. TGR5 messenger RNA (mRNA) has been detected in many tissues, including rat cholangiocytes and mouse gallbladder...
  5. Müssig K, Staiger H, Machicao F, Machann J, Schick F, Schäfer S, et al. Preliminary report: genetic variation within the GPBAR1 gene is not associated with metabolic traits in white subjects at an increased risk for type 2 diabetes mellitus. Metabolism. 2009;58:1809-11 pubmed publisher
    ..GLP-1) production in enteroendocrine L-cells, are mediated by the G-protein-coupled bile acid receptor 1 (GPBAR1)...
  6. Thomas C, Gioiello A, Noriega L, Strehle A, Oury J, Rizzo G, et al. TGR5-mediated bile acid sensing controls glucose homeostasis. Cell Metab. 2009;10:167-77 pubmed publisher
    b>TGR5 is a G protein-coupled receptor expressed in brown adipose tissue and muscle, where its activation by bile acids triggers an increase in energy expenditure and attenuates diet-induced obesity...
  7. Karlsen T, Franke A, Melum E, Kaser A, Hov J, Balschun T, et al. Genome-wide association analysis in primary sclerosing cholangitis. Gastroenterology. 2010;138:1102-11 pubmed publisher
    ..We aimed to characterize the genetic susceptibility to primary sclerosing cholangitis (PSC) by means of a genome-wide association analysis of single nucleotide polymorphism (SNP) markers...
  8. Watanabe M, Houten S, Mataki C, Christoffolete M, Kim B, Sato H, et al. Bile acids induce energy expenditure by promoting intracellular thyroid hormone activation. Nature. 2006;439:484-9 pubmed
    ..BAs activate mitogen-activated protein kinase pathways, are ligands for the G-protein-coupled receptor (GPCR) TGR5 and activate nuclear hormone receptors such as farnesoid X receptor alpha (FXR-alpha; NR1H4)...
  9. Ichikawa R, Takayama T, Yoneno K, Kamada N, Kitazume M, Higuchi H, et al. Bile acids induce monocyte differentiation toward interleukin-12 hypo-producing dendritic cells via a TGR5-dependent pathway. Immunology. 2012;136:153-62 pubmed publisher
    ..However, DCs differentiated with the specific agonist for TGR5, a transmembrane BA receptor, showed an IL-12 hypo-producing phenotype...

More Information

Publications134 found, 100 shown here

  1. Song X, Zhu S, Xie Y, Liu J, Sun L, Zeng D, et al. JTC801 Induces pH-dependent Death Specifically in Cancer Cells and Slows Growth of Tumors in Mice. Gastroenterology. 2018;154:1480-1493 pubmed publisher
    ..Levels of CA9 are increased in human cancer tissues. JTC801 might be developed for treatment of pancreatic cancer. ..
  2. Rohde U. EndoBarrier gastrointestinal liner. Delineation of underlying mechanisms and clinical effects. Dan Med J. 2016;63: pubmed
    ..Thus, bile acids appear to increase GLP-1 secretion via activation of the TGR5 receptor on the intestinal L cell. Recently FXR receptors were postulated to contribute to GLP-1 secretion too...
  3. Ginos B, Navarro S, Schwarz Y, Gu H, Wang D, Randolph T, et al. Circulating bile acids in healthy adults respond differently to a dietary pattern characterized by whole grains, legumes and fruits and vegetables compared to a diet high in refined grains and added sugars: A randomized, controlled, crossover feeding. Metabolism. 2018;83:197-204 pubmed publisher
    ..and inflammation through activation of farnesoid X receptor (FXR) and G protein-coupled bile acid receptor 1 (TGR5), have not been studied...
  4. Chow E, Quach H, Zhang Y, Wang J, Evans D, Li A, et al. Disrupted Murine Gut-to-Human Liver Signaling Alters Bile Acid Homeostasis in Humanized Mouse Liver Models. J Pharmacol Exp Ther. 2017;360:174-191 pubmed
    ..nonparenchymal cells (Tgf-?1) and cholangiocytes [plasma membrane-bound, G protein-coupled receptor for bile acids (Tgr5)], suggestive of irregular regeneration processes in hFRGN livers...
  5. Cattaneo F, Guerra G, Parisi M, De Marinis M, Tafuri D, Cinelli M, et al. Cell-surface receptors transactivation mediated by g protein-coupled receptors. Int J Mol Sci. 2014;15:19700-28 pubmed publisher
    ..These studies may suggest the design of novel strategies for therapeutic interventions. ..
  6. Liu S, Marcelin G, Blouet C, Jeong J, Jo Y, Schwartz G, et al. A gut-brain axis regulating glucose metabolism mediated by bile acids and competitive fibroblast growth factor actions at the hypothalamus. Mol Metab. 2018;8:37-50 pubmed publisher
    Bile acids have been implicated as important regulators of glucose metabolism via activation of FXR and GPBAR1. We have previously shown that FGF19 can modulate glucose handling by suppressing the activity of hypothalamic AGRP/NPY neurons...
  7. Scharfstein J, Ramos P, Barral Netto M. G Protein-Coupled Kinin Receptors and Immunity Against Pathogens. Adv Immunol. 2017;136:29-84 pubmed publisher
  8. Hanafi N, Mohamed A, Sheikh Abdul Kadir S, Othman M. Overview of Bile Acids Signaling and Perspective on the Signal of Ursodeoxycholic Acid, the Most Hydrophilic Bile Acid, in the Heart. Biomolecules. 2018;8: pubmed publisher
    ..Recently, BAs have been shown to bind to muscarinic receptor and Takeda G-protein-coupled receptor 5 (TGR5), both G-protein-coupled receptor (GPCR), independent of the nuclear hormone receptors...
  9. Mittal S, Khole S, Jagadish N, Ghosh D, Gadgil V, Sinkar V, et al. Andrographolide protects liver cells from H2O2 induced cell death by upregulation of Nrf-2/HO-1 mediated via adenosine A2a receptor signalling. Biochim Biophys Acta. 2016;1860:2377-2390 pubmed publisher
    ..We speculate that andrographolide can be used as a therapeutic drug to combat oxidative stress implicated in pathogenesis of various diseases such as diabetes, osteoporosis, neurodegenerative diseases etc. ..
  10. Couvineau A, Laburthe M. The family B1 GPCR: structural aspects and interaction with accessory proteins. Curr Drug Targets. 2012;13:103-15 pubmed
    ..Here, we review the current knowledge regarding: i) the structure of family B1 GPCR binding domain for natural ligands and ii) the interaction of family B1 GPCRs with accessory proteins. ..
  11. Su Y. Regulation of endothelial nitric oxide synthase activity by protein-protein interaction. Curr Pharm Des. 2014;20:3514-20 pubmed
    ..Regulation of eNOS by protein-protein interactions would provide potential targets for pharmacological interventions in NO-compromised cardiovascular diseases. ..
  12. Chen Y, Liu H, Lee T. Ursodeoxycholic Acid Regulates Hepatic Energy Homeostasis and White Adipose Tissue Macrophages Polarization in Leptin-Deficiency Obese Mice. Cells. 2019;8: pubmed publisher
    ..mitochondria biogenesis, and incorporation of bile acid metabolism (Abca1, Abcg1 mRNA and BSEP, FGFR4, and TGR5 protein)...
  13. Garcia V, Gilani A, Shkolnik B, Pandey V, Zhang F, Dakarapu R, et al. 20-HETE Signals Through G-Protein-Coupled Receptor GPR75 (Gq) to Affect Vascular Function and Trigger Hypertension. Circ Res. 2017;120:1776-1788 pubmed publisher
    ..The discovery of 20-HETE-GPR75 pairing presented here provides the molecular basis for the signaling and pathophysiological functions mediated by 20-HETE in hypertension and cardiovascular diseases. ..
  14. Parker B, Wertz S, Pollard C, Desimine V, Maning J, McCrink K, et al. Novel Insights into the Crosstalk between Mineralocorticoid Receptor and G Protein-Coupled Receptors in Heart Adverse Remodeling and Disease. Int J Mol Sci. 2018;19: pubmed publisher
    ..Novel findings revealing non-conventional roles of GPCR signaling molecules, specifically of GPCR-kinase (GRK)-5, in cardiac MR regulation are also highlighted. ..
  15. George M, Vijayakumar A, Dhanesh S, James J, Shivakumar K. Molecular basis and functional significance of Angiotensin II-induced increase in Discoidin Domain Receptor 2 gene expression in cardiac fibroblasts. J Mol Cell Cardiol. 2016;90:59-69 pubmed publisher
    ..A reciprocal regulatory relationship between DDR2 and collagen, involving cross-talk between the GPCR and RTK pathways, is central to Angiotensin II-induced increase in collagen expression in cardiac fibroblasts. ..
  16. Kuhre R, Wewer Albrechtsen N, Larsen O, Jepsen S, Balk Møller E, Andersen D, et al. Bile acids are important direct and indirect regulators of the secretion of appetite- and metabolism-regulating hormones from the gut and pancreas. Mol Metab. 2018;11:84-95 pubmed publisher
    ..secondary to intestinal absorption and depended on activation of basolateral membrane Takeda G-protein receptor 5 (TGR5) receptors on the L-cells in the following order of potency: Lithocholic acid (LCA) >Deoxycholicacid (DCA)>..
  17. Audsley N, Down R. G protein coupled receptors as targets for next generation pesticides. Insect Biochem Mol Biol. 2015;67:27-37 pubmed publisher
    ..Hence fundamental knowledge of the roles and functions of receptors is vital for development to proceed. ..
  18. Liu H, Pathak P, Boehme S, Chiang J. Cholesterol 7?-hydroxylase protects the liver from inflammation and fibrosis by maintaining cholesterol homeostasis. J Lipid Res. 2016;57:1831-1844 pubmed
    ..Bile acids activate farnesoid X receptor (FXR) and Takeda G protein-coupled receptor 5 (TGR5) to regulate lipid, glucose, and energy metabolism...
  19. Cipolla E, Fisher A, Gu H, Mickler E, Agarwal M, Wilke C, et al. IL-17A deficiency mitigates bleomycin-induced complement activation during lung fibrosis. FASEB J. 2017;31:5543-5556 pubmed publisher
    ..Cipolla, E., Fisher, A. J., Gu, H., Mickler, E. A., Agarwal, M., Wilke, C. A., Kim, K. K., Moore, B. B., Vittal, R. IL-17A deficiency mitigates bleomycin-induced complement activation during lung fibrosis. ..
  20. Patel J, Chuaiphichai S, Douglas G, Gorvin C, Channon K. Vascular wall regulator of G-protein signalling-1 (RGS-1) is required for angiotensin II-mediated blood pressure control. Vascul Pharmacol. 2018;108:15-22 pubmed publisher
    ..These findings indicate RGS1 is a novel regulator of blood pressure homeostasis and highlight RGS1-controlled signalling pathways in the vasculature that may be new drug development targets for hypertension. ..
  21. Ocal O, Pashkov V, Kollipara R, Zolghadri Y, Cruz V, Hale M, et al. A rapid in vivo screen for pancreatic ductal adenocarcinoma therapeutics. Dis Model Mech. 2015;8:1201-11 pubmed publisher
    ..This screening strategy can potentially be applied to identify improved therapeutics for other cancers. ..
  22. Park M, Kim N, Wu L, Yu G, Park K. Role of flotillins in the endocytosis of GPCR in salivary gland epithelial cells. Biochem Biophys Res Commun. 2016;476:237-244 pubmed publisher
    ..Our results suggest that flot-1 and -2 are partially involved in CME of M3R by facilitating its internalization. ..
  23. Li Y, Zhu H, Zhang D, Li H, Ma P, Huang L. Novel endogenous negative modulators of platelet function as potential anti-thrombotic targets. Eur Rev Med Pharmacol Sci. 2017;21:3146-3158 pubmed
    ..This review highlights the recent findings on the endogenous negative regulatory molecules released from platelets and their impact on platelet thrombus formation. ..
  24. Jing Y, Liu W, Wang J, Zhao X. The steroid hormone 20-hydroxyecdysone via nongenomic pathway activates Ca2+/calmodulin-dependent protein kinase II to regulate gene expression. J Biol Chem. 2015;290:8469-81 pubmed publisher
    ..Results suggest that 20E (via GPCR activation and calcium signaling) activates CaMKII phosphorylation and nuclear translocation, which regulate USP1 lysine acetylation to form an EcRB1-USP1 complex for 20E response gene transcription. ..
  25. Díaz Soto G, Rocher A, Garcia Rodriguez C, Nunez L, Villalobos C. The Calcium-Sensing Receptor in Health and Disease. Int Rev Cell Mol Biol. 2016;327:321-369 pubmed publisher
    ..Here we review the role of CaSR in health and disease in calciotropic tissues and others beyond the extracellular calcium homeostatic system. ..
  26. Wang X, Edelstein M, Gafter U, Qiu L, Luo Y, Dobrinskikh E, et al. G Protein-Coupled Bile Acid Receptor TGR5 Activation Inhibits Kidney Disease in Obesity and Diabetes. J Am Soc Nephrol. 2016;27:1362-78 pubmed publisher
    ..In this study, we determined the regulation and role of the G protein-coupled bile acid receptor TGR5, previously shown to be regulated by high glucose and/or fatty acids, in obesity-related glomerulopathy (ORG) and ..
  27. Matsubara T, Li F, Gonzalez F. FXR signaling in the enterohepatic system. Mol Cell Endocrinol. 2013;368:17-29 pubmed publisher
    ..FXR; NR1H4), pregnane X receptor (PXR; NR1I2), vitamin D receptor (VDR; NR1I1), G protein coupled receptor TGR5, and other cell signaling pathways (JNK1/2, AKT and ERK1/2)...
  28. Pols T, Noriega L, Nomura M, Auwerx J, Schoonjans K. The bile acid membrane receptor TGR5: a valuable metabolic target. Dig Dis. 2011;29:37-44 pubmed publisher
    ..organs of the enterohepatic axis, increasing evidence points to a crucial role of the G-protein-coupled receptor TGR5 in mediating systemic actions of BAs...
  29. Serfling R, Coin I. Incorporation of Unnatural Amino Acids into Proteins Expressed in Mammalian Cells. Methods Enzymol. 2016;580:89-107 pubmed publisher
    ..We describe a simple and efficient two-plasmid system to incorporate a photoactivatable Uaa into a class B GPCR, and demonstrate cross-linking to its nonmodified natural ligand. ..
  30. Kiselev E, Balasubramanian R, Uliassi E, Brown K, Trujillo K, KATRITCH V, et al. Design, synthesis, pharmacological characterization of a fluorescent agonist of the P2Y₁₄ receptor. Bioorg Med Chem Lett. 2015;25:4733-4739 pubmed publisher
    ..Such conjugates will be useful tools in expanding the SAR of this receptor, which still lacks chemical diversity in its collective ligands. ..
  31. Kiss L, Cselenyák A, Varga Ã, Visegrády A. A novel cell-based duplex high-throughput screening assay combining fluorescent Ca(2+) measurement with homogeneous time-resolved fluorescence technology. Anal Biochem. 2016;507:33-9 pubmed publisher
  32. Wang C, Zeng X, Zhou Z, Zhao J, Pei G. β-arrestin-1 contributes to brown fat function and directly interacts with PPARα and PPARγ. Sci Rep. 2016;6:26999 pubmed publisher
    ..Further mechanistic studies showed that β-arrestin-1 promotes PPARα- but represses PPARγ-mediated transcriptional activities, providing potential regulatory pathway for BAT function. ..
  33. Wang Y, Xu X, Pan M, Jin T. ELMO1 Directly Interacts with G?? Subunit to Transduce GPCR Signaling to Rac1 Activation in Chemotaxis. J Cancer. 2016;7:973-83 pubmed publisher
    ..Our results suggest that chemokine GPCR-mediated interaction between G?? and ELMO1/Dock1 complex might serve as an evolutionarily conserved mechanism for Rac activation to regulate actin cytoskeleton for chemotaxis of human cells. ..
  34. Coly P, Perzo N, Le Joncour V, Lecointre C, Schouft M, Desrues L, et al. Chemotactic G protein-coupled receptors control cell migration by repressing autophagosome biogenesis. Autophagy. 2016;12:2344-2362 pubmed
    ..Altogether, our data reveal a new link between GPCR signaling and the autophagy machinery, and may help to envisage therapeutic strategies in pathological processes such as cancer cell invasion. ..
  35. Kumar R, Hazan A, Geron M, Steinberg R, Livni L, Matzner H, et al. Activation of transient receptor potential vanilloid 1 by lipoxygenase metabolites depends on PKC phosphorylation. FASEB J. 2017;31:1238-1247 pubmed publisher
    ..Kumar R., Hazan, A., Geron, M., Steinberg, R., Livni, L., Matzner, H., Priel, A. Activation of transient receptor potential vanilloid 1 by lipoxygenase metabolites depends on PKC phosphorylation. ..
  36. Lee K, Lu X, Nguyen C, Feng Q, Chidiac P. Cardiomyocyte specific overexpression of a 37 amino acid domain of regulator of G protein signalling 2 inhibits cardiac hypertrophy and improves function in response to pressure overload in mice. J Mol Cell Cardiol. 2017;108:194-202 pubmed publisher
    ..Notably, cardiomyocyte cell size was significantly decreased in TG compared to WT TAC mice. These results suggest that RGS2 may limit pathological cardiac hypertrophy at least in part via the function of its eIF2B-binding domain. ..
  37. Storme J, Cannaert A, Van Craenenbroeck K, Stove C. Molecular dissection of the human A3 adenosine receptor coupling with β-arrestin2. Biochem Pharmacol. 2018;148:298-307 pubmed publisher
    ..In conclusion, other parts of the human A3AR, either cytosolic or exposed upon receptor activation, rather than the C-terminus alone, are responsible for βarr2 recruitment in a complementary or synergistic way. ..
  38. Keitel V, Spomer L, Marin J, Williamson C, Geenes V, Kubitz R, et al. Effect of maternal cholestasis on TGR5 expression in human and rat placenta at term. Placenta. 2013;34:810-6 pubmed publisher
    b>TGR5 (Gpbar-1) is a plasma membrane-bound bile acid receptor expressed in several tissues, including liver, intestine and brain...
  39. Balogh A, Shimizu Y, Lee S, Norman D, Gangwar R, Bavaria M, et al. The autotaxin-LPA2 GPCR axis is modulated by γ-irradiation and facilitates DNA damage repair. Cell Signal. 2015;27:1751-62 pubmed publisher
    ..These findings identify ATX and LPA2 as radiation-regulated genes that appear to play a physiological role in DNA repair. ..
  40. Kim M, Cho A. Incorporating QM and solvation into docking for applications to GPCR targets. Phys Chem Chem Phys. 2016;18:28281-28289 pubmed
    ..The results of a test on all solved GPCR cocrystals show a significant improvement over the conventional docking method. ..
  41. Ludwig M, Seuwen K, Bridges J. Adhesion GPCR Function in Pulmonary Development and Disease. Handb Exp Pharmacol. 2016;234:309-327 pubmed
    ..Although this field is still in its infancy, this chapter will review all available data regarding aGPCRs in pulmonary biology, with a particular focus on the aGPCR for which the most substantial data to date exist: Adgrf5. ..
  42. Guinzberg R, Díaz Cruz A, Acosta Trujillo C, Vilchis Landeros M, Vázquez Meza H, Lozano Flores C, et al. Newly synthesized cAMP is integrated at a membrane protein complex signalosome to ensure receptor response specificity. FEBS J. 2017;284:258-276 pubmed publisher
    ..Thus, each signalosome is devoted to ensure the transmission of a unique and unequivocal message through the cell. ..
  43. Riddy D, Delerive P, Summers R, Sexton P, Langmead C. G Protein-Coupled Receptors Targeting Insulin Resistance, Obesity, and Type 2 Diabetes Mellitus. Pharmacol Rev. 2018;70:39-67 pubmed publisher
  44. Muntean B, Zucca S, MacMullen C, Dao M, Johnston C, Iwamoto H, et al. Interrogating the Spatiotemporal Landscape of Neuromodulatory GPCR Signaling by Real-Time Imaging of cAMP in Intact Neurons and Circuits. Cell Rep. 2018;22:255-268 pubmed publisher
    ..This offers a resource for studying native neuronal GPCR signaling in real time. ..
  45. Bala V, Rajagopal S, Kumar D, Nalli A, Mahavadi S, Sanyal A, et al. Release of GLP-1 and PYY in response to the activation of G protein-coupled bile acid receptor TGR5 is mediated by Epac/PLC-ε pathway and modulated by endogenous H2S. Front Physiol. 2014;5:420 pubmed publisher
    Activation of plasma membrane TGR5 receptors in enteroendocrine cells by bile acids is known to regulate gastrointestinal secretion and motility and glucose homeostasis...
  46. Shigemori T, Kuroda K, Ueda M. Screening of randomly mutagenized glucagon-like peptide-1 library by using an integrated yeast-mammalian assay system. J Biotechnol. 2015;209:96-101 pubmed publisher
  47. Nakajima K, Cui Z, Li C, Meister J, Cui Y, Fu O, et al. Gs-coupled GPCR signalling in AgRP neurons triggers sustained increase in food intake. Nat Commun. 2016;7:10268 pubmed publisher
    ..Our data suggest that drugs able to inhibit this signalling pathway may become useful for the treatment of obesity. ..
  48. Traynham C, Hullmann J, Koch W. "Canonical and non-canonical actions of GRK5 in the heart". J Mol Cell Cardiol. 2016;92:196-202 pubmed publisher
    ..Further, we will also present potential therapeutic strategies (i.e. small molecule inhibition, gene therapy) that may have potential in combating the deleterious effects of GRK5 in HF. ..
  49. Lappano R, Rigiracciolo D, De Marco P, Avino S, Cappello A, Rosano C, et al. Recent Advances on the Role of G Protein-Coupled Receptors in Hypoxia-Mediated Signaling. AAPS J. 2016;18:305-10 pubmed publisher
    ..Here, we describe the role exerted by GPCR-mediated signaling in low oxygen conditions, discussing, in particular, the involvement of GPER by a hypoxic microenvironment. ..
  50. Zhang Y, Pan Y, Lin C, Zheng Y, Sun H, Zhang H, et al. Bile acids evoke placental inflammation by activating Gpbar1/NF-?B pathway in intrahepatic cholestasis of pregnancy. J Mol Cell Biol. 2016;8:530-541 pubmed
    ..Herein, we report that bile acids induce NF-?B pathway activation via G protein-coupled bile acid receptor 1 (Gpbar1), with consequent upregulation of inflammatory genes in trophoblasts, leading to aberrant leukocyte infiltration ..
  51. Vass M, Kooistra A, Ritschel T, Leurs R, de Esch I, de Graaf C. Molecular interaction fingerprint approaches for GPCR drug discovery. Curr Opin Pharmacol. 2016;30:59-68 pubmed publisher
  52. Xiang J, Chun E, Liu C, Jing L, Al Sahouri Z, Zhu L, et al. Successful Strategies to Determine High-Resolution Structures of GPCRs. Trends Pharmacol Sci. 2016;37:1055-1069 pubmed publisher
    ..By comparing the success rates of different strategies used in the past, we wish to pave the road for more successful structure-function research for GPCRs in the future. ..
  53. Stockley J, Nisar S, Leo V, Sabi E, Cunningham M, Eikenboom J, et al. Identification and Characterization of Novel Variations in Platelet G-Protein Coupled Receptor (GPCR) Genes in Patients Historically Diagnosed with Type 1 von Willebrand Disease. PLoS ONE. 2015;10:e0143913 pubmed publisher
    ..The enrichment of single nucleotide variations in G protein-coupled receptor genes among type 1 von Willebrand disease patients supports the view of type 1 von Willebrand disease as a polygenic disorder. ..
  54. Camp N, Lee K, Cherry A, Wacker Mhyre J, Kountz T, Park J, et al. Dynamic mass redistribution reveals diverging importance of PDZ-ligands for G protein-coupled receptor pharmacodynamics. Pharmacol Res. 2016;105:13-21 pubmed publisher
    ..e. LPAR2, SSTR5). These results demonstrate the utility of label-free functional assays to tease apart the contributions of conserved protein interaction domains for GPCR signal-transduction coupling in cultured cells. ..
  55. Hasegawa H, Patel N, Ettehadieh E, Li P, Lim A. Topogenesis and cell surface trafficking of GPR34 are facilitated by positive-inside rule that effects through a tri-basic motif in the first intracellular loop. Biochim Biophys Acta. 2016;1863:1534-51 pubmed publisher
  56. Sindhu T, Srinivasan P. Pharmacophore modeling, comprehensive 3D-QSAR, and binding mode analysis of TGR5 agonists. J Recept Signal Transduct Res. 2017;37:109-123 pubmed publisher
    Takeda G-protein-coupled receptor 5 (TGR5) is emerging as an important and promising target for the development of anti-diabetic drugs...
  57. Fiorucci S, Distrutti E. Targeting the transsulfuration-H2S pathway by FXR and GPBAR1 ligands in the treatment of portal hypertension. Pharmacol Res. 2016;111:749-756 pubmed publisher
    ..farnesoid X receptor (FXR), and G-protein-coupled receptors (GPCRs), such as the G-protein bile acid receptor 1 (GPBAR1)...
  58. Serafimidis I, Rodriguez Aznar E, Lesche M, Yoshioka K, Takuwa Y, Dahl A, et al. Pancreas lineage allocation and specification are regulated by sphingosine-1-phosphate signalling. PLoS Biol. 2017;15:e2000949 pubmed publisher
    ..Understanding lineage allocation and specification in the pancreas will shed light in the origins of pancreatic diseases and may suggest novel therapeutic approaches. ..
  59. Wang Y, Huang J, Liu X, Niu Y, Zhao L, Yu Y, et al. ?-Arrestin-biased AT1R stimulation promotes extracellular matrix synthesis in renal fibrosis. Am J Physiol Renal Physiol. 2017;313:F1-F8 pubmed publisher
    ..Targeting ?-arrestin-2 may be a potential therapeutic agent for renal fibrosis. ..
  60. Schreier S, Bozelli J, Marín N, Vieira R, Nakaie C. The spin label amino acid TOAC and its uses in studies of peptides: chemical, physicochemical, spectroscopic, and conformational aspects. Biophys Rev. 2012;4:45-66 pubmed publisher
    ..The growth of the number of TOAC-related publications suggests that this unnatural amino acid will find increasing applications in the future. ..
  61. Muroi T, Matsushima Y, Kanamori R, Inoue H, Fujii W, Yogo K. GPR62 constitutively activates cAMP signaling but is dispensable for male fertility in mice. Reproduction. 2017;154:755-764 pubmed publisher
  62. Doyen P, Vergouts M, Pochet A, Desmet N, van Neerven S, Brook G, et al. Inflammation-associated regulation of RGS in astrocytes and putative implication in neuropathic pain. J Neuroinflammation. 2017;14:209 pubmed publisher
  63. Fang W, Wang Z, Li Q, Wang X, Zhang Y, Sun Y, et al. Gpr97 Exacerbates AKI by Mediating Sema3A Signaling. J Am Soc Nephrol. 2018;29:1475-1489 pubmed publisher
    ..b>Conclusions Gpr97 is an important mediator of AKI, and pharmacologic targeting of Gpr97-mediated Sema3A signaling at multiple levels may provide a novel approach for the treatment of AKI. ..
  64. Camilleri M, Shin A, Busciglio I, Carlson P, Acosta A, Bharucha A, et al. Genetic variation in GPBAR1 predisposes to quantitative changes in colonic transit and bile acid excretion. Am J Physiol Gastrointest Liver Physiol. 2014;307:G508-16 pubmed publisher
    ..associations of candidate genes controlling BA metabolism (KLB rs17618244 and FGFR4 rs351855), BA receptor (GPBAR1 rs11554825), serotonin (5-HT) reuptake (SLC6A4 through rs4795541 which encodes for the 44-bp insert in 5HTTLPR), ..
  65. Mendoza Torres E, Oyarzún A, Mondaca Ruff D, Azocar A, Castro P, Jalil J, et al. ACE2 and vasoactive peptides: novel players in cardiovascular/renal remodeling and hypertension. Ther Adv Cardiovasc Dis. 2015;9:217-37 pubmed publisher
  66. Zaid H, Raiyn J, Osman M, Falah M, Srouji S, Rayan A. In silico modeling techniques for predicting the tertiary structure of human H4 receptor. Front Biosci (Landmark Ed). 2016;21:597-619 pubmed
  67. Nakamura Y, Hashimoto T, Ishii J, Kondo A. Dual-color reporter switching system to discern dimer formations of G-protein-coupled receptors using Cre/loxP site-specific recombination in yeast. Biotechnol Bioeng. 2016;113:2178-90 pubmed publisher
    ..Biotechnol. Bioeng. 2016;113: 2178-2190. © 2016 Wiley Periodicals, Inc. ..
  68. Qiao Y, Tam J, Tan S, Tai Y, Chin C, Stewart A, et al. CD151, a laminin receptor showing increased expression in asthmatic patients, contributes to airway hyperresponsiveness through calcium signaling. J Allergy Clin Immunol. 2017;139:82-92.e5 pubmed publisher
    ..These observations have significant implications in understanding the mechanism for AHR and the efficacy of new and emerging therapeutics. ..
  69. Eliás O, Kovacs Z, Wágner G, Némethy Z, Tarcsay A, Greiner I. Charting the chemical space around the (iso)indoline scaffold, a comprehensive approach towards multitarget directed ligands. Bioorg Med Chem Lett. 2016;26:4211-5 pubmed publisher
  70. Kechele D, Blue R, Zwarycz B, Espenschied S, Mah A, Siegel M, et al. Orphan Gpr182 suppresses ERK-mediated intestinal proliferation during regeneration and adenoma formation. J Clin Invest. 2017;127:593-607 pubmed publisher
    ..Together, these results implicate Gpr182 as a negative regulator of intestinal MAPK signaling-induced proliferation, particularly during regeneration and adenoma formation. ..
  71. Cunningham M, Aungraheeta R, Mundell S. Pathophysiological consequences of receptor mistraffic: Tales from the platelet P2Y12 receptor. Mol Cell Endocrinol. 2017;449:74-81 pubmed publisher
  72. Huhtinen A, Hongisto V, Laiho A, Löyttyniemi E, Pijnenburg D, Scheinin M. Gene expression profiles and signaling mechanisms in α2B-adrenoceptor-evoked proliferation of vascular smooth muscle cells. BMC Syst Biol. 2017;11:65 pubmed publisher
    ..While many of the identified individual signals were relatively small in terms of effect size, many of them were validated by combining pathway analysis and our integrated screening approach. ..
  73. Tunaru S, Chennupati R, Nusing R, Offermanns S. Arachidonic Acid Metabolite 19(S)-HETE Induces Vasorelaxation and Platelet Inhibition by Activating Prostacyclin (IP) Receptor. PLoS ONE. 2016;11:e0163633 pubmed publisher
    ..These results identify a novel mechanism of action for the CYP450-dependent arachidonic acid metabolite 19(S)-HETE and point to the existence of a broader spectrum of naturally occurring prostanoid receptor agonists. ..
  74. Wang D, Guo M, Yu J, Wang X, Zhang Q, Yang X, et al. Glioma targeting peptide in combination with the P53 C terminus inhibits glioma cell proliferation in vitro. Cytotechnology. 2018;70:153-161 pubmed publisher
    ..Flow cytometric analysis showed increase apoptosis. Our findings suggest that the P53C in the fusion protein ZZ-GPcR can enter into glioma cells to exert its inhibitory effect. ..
  75. Marco H, Verlinden H, Vanden Broeck J, Gäde G. Characterisation and pharmacological analysis of a crustacean G protein-coupled receptor: the red pigment-concentrating hormone receptor of Daphnia pulex. Sci Rep. 2017;7:6851 pubmed publisher
    ..Mainly amino acids in positions 1 to 4 and 8 of Dappu-RPCH appear responsible for effective activation of Dappu-RPCHR. The substitution of Phe4 in Dappu-RPCH had the most damaging effect on its agonistic activity. ..
  76. Galoian K, Abrahamyan S, Chailyan G, Qureshi A, Patel P, Metser G, et al. Toll like receptors TLR1/2, TLR6 and MUC5B as binding interaction partners with cytostatic proline rich polypeptide 1 in human chondrosarcoma. Int J Oncol. 2018;52:139-154 pubmed publisher
    ..Experimental data indicated that in this cellular context the mentioned receptors had tumor suppressive function...
  77. Younis S, Rashid S. Alpha conotoxin-BuIA globular isomer is a competitive antagonist for oleoyl-L-alpha-lysophosphatidic acid binding to LPAR6; A molecular dynamics study. PLoS ONE. 2017;12:e0189154 pubmed publisher
  78. DeVree B, Mahoney J, Velez Ruiz G, Rasmussen S, Kuszak A, Edwald E, et al. Allosteric coupling from G protein to the agonist-binding pocket in GPCRs. Nature. 2016;535:182-6 pubmed
    ..The effects of nucleotide-free G protein on ligand-binding kinetics are shared by other members of the superfamily of GPCRs, suggesting that a common mechanism may underlie G-protein-mediated enhancement of agonist affinity. ..
  79. Xu L, Li L, Yang P, Ma Z. Calmodulin as a downstream gene of octopamine-OAR ?1 signalling mediates olfactory attraction in gregarious locusts. Insect Mol Biol. 2017;26:1-12 pubmed publisher
    ..Overall, this study provides novel insights into the mechanism of OA-OAR ?1 signalling involved in olfactory attraction of gregarious locusts...
  80. Sun N, Zhang X, Zhang X, Kim K. The EGF receptor inhibits the signaling of dopamine D3 receptor through the phosphorylation of GRK2 on tyrosine residues. Biochem Biophys Res Commun. 2017;489:515-522 pubmed publisher
    ..Considering that both EGFR and D3R are closely related to schizophrenia, this study could provide new molecular insight into the etiology of the disorder. ..
  81. Foster S, Brauner Osborne H. Investigating Internalization and Intracellular Trafficking of GPCRs: New Techniques and Real-Time Experimental Approaches. Handb Exp Pharmacol. 2018;245:41-61 pubmed publisher
  82. Ciancetta A, Jacobson K. Breakthrough in GPCR Crystallography and Its Impact on Computer-Aided Drug Design. Methods Mol Biol. 2018;1705:45-72 pubmed publisher
    ..Thus, computational modeling has become an essential tool for the design of purine receptor ligands. ..
  83. Bartuzi D, Kaczor A, Matosiuk D. Opportunities and Challenges in the Discovery of Allosteric Modulators of GPCRs. Methods Mol Biol. 2018;1705:297-319 pubmed publisher
    ..In this chapter, we focus on nuances of targeting GPCR allosteric sites in computational drug design efforts, in particular with application of docking, virtual screening, and molecular dynamics. ..
  84. Persaud S. Islet G-protein coupled receptors: therapeutic potential for diabetes. Curr Opin Pharmacol. 2017;37:24-28 pubmed publisher
    ..This review explores pharmaceutical development of drugs that activate individual or multiple ?-cell GPCRs and explains how our knowledge of GPCR expression by human islets may inform direction on novel GPCR targets. ..
  85. Winther M, Holdfeldt A, Sundqvist M, Rajabkhani Z, Gabl M, Bylund J, et al. Formyl peptide derived lipopeptides disclose differences between the receptors in mouse and men and call the pepducin concept in question. PLoS ONE. 2017;12:e0185132 pubmed publisher
  86. Tutunea Fatan E, Caetano F, Gros R, Ferguson S. GRK2 targeted knock-down results in spontaneous hypertension, and altered vascular GPCR signaling. J Biol Chem. 2015;290:5141-55 pubmed publisher
    ..Consequently, therapeutic strategies that target GRK2 activity, not expression, may be more effective for the treatment of hypertension. ..
  87. Di Pizio A, Kruetzfeldt L, Cheled Shoval S, Meyerhof W, Behrens M, Niv M. Ligand binding modes from low resolution GPCR models and mutagenesis: chicken bitter taste receptor as a test-case. Sci Rep. 2017;7:8223 pubmed publisher
    ..The integrated approach validated here may be applicable to additional cases where the sequence identity of the GPCR of interest and the existing experimental structures is low. ..
  88. Renu K, Madhyastha H, Madhyastha R, Maruyama M, Arunachlam S, V G A. Role of arsenic exposure in adipose tissue dysfunction and its possible implication in diabetes pathophysiology. Toxicol Lett. 2018;284:86-95 pubmed publisher
    ..Few studies indicate that arsenic might induces lipodystrophy condition. Further research is needed to evaluate the mechanistic link between arsenic and adipose tissue dysfunction which leads to insulin resistance. ..
  89. Liu D, Wuthrich K. Ring current shifts in (19)F-NMR of membrane proteins. J Biomol NMR. 2016;65:1-5 pubmed publisher
    ..It will then also be interesting to see if the presently indicated role of ring current shifts in membrane protein studies with (19)F-NMR markers can be substantiated by a more extensive data base resulting from future studies. ..
  90. Wanka L, Babilon S, Burkert K, Mörl K, Gurevich V, Beck Sickinger A. C-terminal motif of human neuropeptide Y4 receptor determines internalization and arrestin recruitment. Cell Signal. 2017;29:233-239 pubmed publisher
    ..Thus, we identified the internalization motif for the human neuropeptide Y4 receptor, which regulates arrestin-3 recruitment and receptor endocytosis. ..
  91. Cariello M, Peres C, Zerlotin R, Porru E, Sabba C, Roda A, et al. Long-term Administration of Nuclear Bile Acid Receptor FXR Agonist Prevents Spontaneous Hepatocarcinogenesis in Abcb4-/- Mice. Sci Rep. 2017;7:11203 pubmed publisher
    ..we tested chemical FXR activation by administering for 15 months the dual FXR/ membrane G protein-coupled receptor (TGR5) agonist INT-767 (6α-ethyl-3α,7α,23-trihydroxy-24-nor-5β-cholan-23-sulphate) to Fxr-/- and Abcb4..
  92. Houslay D, Anderson K, Chessa T, Kulkarni S, Fritsch R, Downward J, et al. Coincident signals from GPCRs and receptor tyrosine kinases are uniquely transduced by PI3Kβ in myeloid cells. Sci Signal. 2016;9:ra82 pubmed publisher