Gene Symbol: ADRA1A
Description: adrenoceptor alpha 1A
Alias: ADRA1C, ADRA1L1, ALPHA1AAR, alpha-1A adrenergic receptor, G protein coupled receptor, adrenergic, alpha-1A-, receptor, alpha-1A adrenoceptor, alpha-1A adrenoreceptor, alpha-1C adrenergic receptor
Species: human
Products:     ADRA1A

Top Publications

  1. Keffel S, Alexandrov A, Goepel M, Michel M. alpha(1)-adrenoceptor subtypes differentially couple to growth promotion and inhibition in Chinese hamster ovary cells. Biochem Biophys Res Commun. 2000;272:906-11 pubmed
    ..We conclude that within a given cell type alpha(1)-adrenoceptor subtypes can have opposite effects on cellular growth, although their proximal signal transduction displays only quantitative differences. ..
  2. Jiang S, Mao G, Zhang S, Hong X, Tang G, Li Z, et al. Individual and joint association of alpha1A-adrenergic receptor Arg347Cys polymorphism and plasma irbesartan concentration with blood pressure therapeutic response in Chinese hypertensive subjects. Clin Pharmacol Ther. 2005;78:239-48 pubmed
    ..The association of the Arg347Cys polymorphism with the BP therapeutic response was more pronounced in those patients with higher plasma concentrations of irbesartan. ..
  3. Rudner X, Berkowitz D, Booth J, Funk B, Cozart K, D Amico E, et al. Subtype specific regulation of human vascular alpha(1)-adrenergic receptors by vessel bed and age. Circulation. 1999;100:2336-43 pubmed
    ..These findings provide potential novel targets for therapeutic intervention in many clinical settings. ..
  4. Liu F, He K, Yang X, Xu N, Liang Z, Xu M, et al. ?1A-adrenergic receptor induces activation of extracellular signal-regulated kinase 1/2 through endocytic pathway. PLoS ONE. 2011;6:e21520 pubmed publisher
    ..These data suggest that the endocytic pathway is involved in ?(1A)-AR-induced ERK1/2 activation, which is independent of G(q)/PLC/PKC signaling. ..
  5. Hoehe M, Berrettini W, Schwinn D, Hsieh W. A two-allele PstI RFLP for the alpha-1C adrenergic receptor gene (ADRA1C). Hum Mol Genet. 1992;1:349 pubmed
  6. Thebault S, Roudbaraki M, Sydorenko V, Shuba Y, Lemonnier L, Slomianny C, et al. Alpha1-adrenergic receptors activate Ca(2+)-permeable cationic channels in prostate cancer epithelial cells. J Clin Invest. 2003;111:1691-701 pubmed
    ..Collectively, our results suggest that alpha1-ARs play a role in promoting hPCE cell proliferation via TRP channels. ..
  7. Mochtar C, Laan W, van Houwelingen K, Franke B, de la Rosette J, Schalken J, et al. Polymorphisms in the alpha1A-adrenoceptor gene do not modify the short- and long-term efficacy of alpha1-adrenoceptor antagonists in the treatment of benign prostatic hyperplasia. BJU Int. 2006;97:852-5 pubmed
    OBJECTIVE To determine whether a common single nucleotide polymorphism (SNP) in the ADRA1A gene encoding the alpha(1A)-adrenoceptor modifies the short- and long-term efficacy of alpha(1)-adrenoceptor antagonists in the treatment of benign ..
  8. Lei B, Morris D, Smith M, Schwinn D. Lipid rafts constrain basal alpha(1A)-adrenergic receptor signaling by maintaining receptor in an inactive conformation. Cell Signal. 2009;21:1532-9 pubmed publisher
    ..These results strongly suggest that lipid rafts constrain basal alpha(1A)AR activity; however, preassembled receptor/G protein complexes could still provide a mechanism for accelerating alpha(1A)AR signaling following stimulation. ..
  9. Shibata K, Hirasawa A, Moriyama N, Kawabe K, Ogawa S, Tsujimoto G. Alpha 1a-adrenoceptor polymorphism: pharmacological characterization and association with benign prostatic hypertrophy. Br J Pharmacol. 1996;118:1403-8 pubmed
    ..The study did not provide any evidence to support the hypothesis that alpha 1a-adrenoceptor gene polymorphism is associated with BPH. ..

More Information

Publications132 found, 100 shown here

  1. Iacoviello M, Forleo C, Sorrentino S, Romito R, De Tommasi E, Lucarelli K, et al. Alpha- and beta-adrenergic receptor polymorphisms in hypertensive and normotensive offspring. J Cardiovasc Med (Hagerstown). 2006;7:316-21 pubmed
    ..The Arg492Cys polymorphism of the alpha1a-AR gene, although not associated with a family history of hypertension, was strongly related to autonomic control of heart rate. ..
  2. Oganesian A, Yarov Yarovoy V, Parks W, Schwinn D. Constitutive coupling of a naturally occurring human alpha1a-adrenergic receptor genetic variant to EGFR transactivation pathway. Proc Natl Acad Sci U S A. 2011;108:19796-801 pubmed publisher
    ..These findings raise the possibility of a previously unexplored mechanism for sympathetically mediated human hypertension triggered by a naturally occurring human genetic variant. ..
  3. Hirasawa A, Horie K, Tanaka T, Takagaki K, Murai M, Yano J, et al. Cloning, functional expression and tissue distribution of human cDNA for the alpha 1C-adrenergic receptor. Biochem Biophys Res Commun. 1993;195:902-9 pubmed
    ..The data show that the clone P2C4 encodes a human alpha 1C-adrenergic receptor cDNA, and the receptor subtype is expressed not widely but localized in several human tissues. ..
  4. Snapir A, Koskenvuo J, Toikka J, Orho Melander M, Hinkka S, Saraste M, et al. Effects of common polymorphisms in the alpha1A-, alpha2B-, beta1- and beta2-adrenoreceptors on haemodynamic responses to adrenaline. Clin Sci (Lond). 2003;104:509-20 pubmed
    ..These results suggest that, upon acute adrenaline infusion, the alpha(2B)-AR D/D genotype confers increased vasoconstriction and that the beta(2)-AR GG genotype confers reduced vasodilatation. ..
  5. Pediani J, Colston J, Caldwell D, Milligan G, Daly C, McGrath J. Beta-arrestin-dependent spontaneous alpha1a-adrenoceptor endocytosis causes intracellular transportation of alpha-blockers via recycling compartments. Mol Pharmacol. 2005;67:992-1004 pubmed
    ..We conclude that alpha(1a)-ARs recycle rapidly by an agonist-independent, constitutive, beta-arrestin-dependent process and that this can transport "alpha-blockers" into cells carrying these receptors. ..
  6. Stanasila L, Abuin L, Dey J, Cotecchia S. Different internalization properties of the alpha1a- and alpha1b-adrenergic receptor subtypes: the potential role of receptor interaction with beta-arrestins and AP50. Mol Pharmacol. 2008;74:562-73 pubmed publisher
  7. Gimpl G, Fahrenholz F. The oxytocin receptor system: structure, function, and regulation. Physiol Rev. 2001;81:629-83 pubmed
    ..One has to conclude that the physiological regulation of the OT system will remain puzzling as long as the molecular mechanisms of genomic and nongenomic actions of steroids have not been clarified...
  8. Hua F, Shang S, Yang Y, Zhang H, Xu T, Yu J, et al. TRIB3 Interacts With β-Catenin and TCF4 to Increase Stem Cell Features of Colorectal Cancer Stem Cells and Tumorigenesis. Gastroenterology. 2019;156:708-721.e15 pubmed publisher
    ..Knockdown of TRIB3 decreases colon neoplasia in mice, migration of CRC cells, and their growth as xenograft tumors in mice. Strategies to block TRIB3 activity might be developed for treatment of CRC. ..
  9. Ubuka T, Tsutsui K. Evolution of gonadotropin-inhibitory hormone receptor and its ligand. Gen Comp Endocrinol. 2014;209:148-61 pubmed publisher
  10. Rayner B, Ramesar R. The importance of G protein-coupled receptor kinase 4 (GRK4) in pathogenesis of salt sensitivity, salt sensitive hypertension and response to antihypertensive treatment. Int J Mol Sci. 2015;16:5741-9 pubmed publisher
    ..It may also underlie the difference in hypertension between different geographically derived population groups, and form a basis for pharmacogenomic approaches to treatment of hypertension. ..
  11. Prud homme G, Glinka Y, Wang Q. Immunological GABAergic interactions and therapeutic applications in autoimmune diseases. Autoimmun Rev. 2015;14:1048-56 pubmed publisher
    ..However, the immune effects of GABAergic drugs in patients are not well documented. GABAergic immunobiology is a recent area of research, which shows potential for the development of new therapies for autoimmune diseases. ..
  12. Connor E, Evock Clover C, Walker M, Elsasser T, Kahl S. COMPARATIVE GUT PHYSIOLOGY SYMPOSIUM: Comparative physiology of glucagon-like peptide-2: Implications and applications for production and health of ruminants. J Anim Sci. 2015;93:492-501 pubmed publisher
    ..g., through specific feed additives), which are more likely to achieve consumer acceptance, are needed. Opportunities to address these challenges are discussed. ..
  13. Polhemus D, Gao J, Scarborough A, Trivedi R, McDonough K, Goodchild T, et al. Radiofrequency Renal Denervation Protects the Ischemic Heart via Inhibition of GRK2 and Increased Nitric Oxide Signaling. Circ Res. 2016;119:470-80 pubmed publisher
    ..These findings provide new insights into the remote cardioprotective effects of RF-RDN acting directly on cardiac myocytes to attenuate cell death and protect against ischemic injury. ..
  14. Khan T, Ahmad R, Azad I, Raza S, Joshi S, Khan A. Computer-aided drug design and virtual screening of targeted combinatorial libraries of mixed-ligand transition metal complexes of 2-butanone thiosemicarbazone. Comput Biol Chem. 2018;75:178-195 pubmed publisher
  15. Ambrożewicz E, Wojcik P, Wroński A, Łuczaj W, Jastrząb A, Zarkovic N, et al. Pathophysiological Alterations of Redox Signaling and Endocannabinoid System in Granulocytes and Plasma of Psoriatic Patients. Cells. 2018;7: pubmed publisher
    ..In addition, increased expression of CB1 receptors leads to increased oxidative stress, lipid modifications, and inflammation, which, in turn, may promote the progression of psoriasis into the advanced, arthritic form of the disease. ..
  16. Seemann S, Lupp A. Administration of AMD3100 in endotoxemia is associated with pro-inflammatory, pro-oxidative, and pro-apoptotic effects in vivo. J Biomed Sci. 2016;23:68 pubmed
  17. Raffetto J, Qiao X, Beauregard K, Khalil R. Estrogen receptor-mediated enhancement of venous relaxation in female rat: implications in sex-related differences in varicose veins. J Vasc Surg. 2010;51:972-81 pubmed publisher
    ..The decreased venous contraction and enhanced E2/ER-mediated venous relaxation would lead to more distensible veins in female rats. ..
  18. 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
  19. Li M, Chen W, Wang L, Sun J, Zhou L, Shi Y, et al. RLA8-A New and Highly Effective Quadruple PPAR-α/γ/δ and GPR40 Agonist to Reverse Nonalcoholic Steatohepatitis and Fibrosis. J Pharmacol Exp Ther. 2019;369:67-77 pubmed publisher
  20. Zhu F, Ji X, Zhong X, Hu H, Liang L, Chen J, et al. [Effects of mild hypothermia on β-adrenergic signaling pathway in a cardiac arrest swine model]. Zhonghua Wei Zhong Bing Ji Jiu Yi Xue. 2018;30:134-139 pubmed publisher
    ..45±0.05 vs. 0.80±0.08, P < 0.05). Mild hypothermia can reduce the degree of cardiac function injury after CPR, and its mechanism may be related to the reduction of impaired myocardial β-AR signaling after CPR. ..
  21. Yue Z, Yu M, Zhang X, Wang J, Ru S. The anti-androgenic effect of chronic exposure to semicarbazide on male Japanese flounder (Paralichthys olivaceus) and its potential mechanisms. Comp Biochem Physiol C Toxicol Pharmacol. 2018;210:30-34 pubmed publisher
  22. 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
    ..This review provides an overview of BA signaling, with the main emphasis on past and present perspectives on UDCA signals in the heart. ..
  23. Fatima A, Waters S, O Boyle P, Seoighe C, Morris D. Alterations in hepatic miRNA expression during negative energy balance in postpartum dairy cattle. BMC Genomics. 2014;15:28 pubmed publisher
    ..This study highlights the potential role of miRNAs in transcription regulation of hepatic gene expression during SNEB in dairy cattle. ..
  24. Kächele M, Hennige A, Machann J, Hieronimus A, Lamprinou A, Machicao F, et al. Variation in the Phosphoinositide 3-Kinase Gamma Gene Affects Plasma HDL-Cholesterol without Modification of Metabolic or Inflammatory Markers. PLoS ONE. 2015;10:e0144494 pubmed publisher
    ..Even though the molecular pathways connecting PI3Kγ and HDL metabolism remain to be further elucidated, this finding could add a novel aspect to the pathophysiological role of PI3Kγ in atherogenesis. ..
  25. 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. ..
  26. Strack J, Heni H, Gilsbach R, Hein L, Aktories K, Orth J. Noncanonical G-protein-dependent modulation of osteoclast differentiation and bone resorption mediated by Pasteurella multocida toxin. MBio. 2014;5:e02190 pubmed publisher
    ..In particular, modulation of G protein-coupled receptor activity in osteoclast progenitors by small molecules might be of specific interest. ..
  27. Howick K, Wallace Fitzsimons S, Kandil D, Chruscicka B, Caliş M, Murphy E, et al. A Dairy-Derived Ghrelinergic Hydrolysate Modulates Food Intake In Vivo. Int J Mol Sci. 2018;19: pubmed publisher
    ..Further mechanistic studies are required in order to confirm efficacy as a ghrelinergic bioactive in susceptible population groups. ..
  28. Mata K, Li W, Reslan O, Siddiqui W, Opsasnick L, Khalil R. Adaptive increases in expression and vasodilator activity of estrogen receptor subtypes in a blood vessel-specific pattern during pregnancy. Am J Physiol Heart Circ Physiol. 2015;309:H1679-96 pubmed publisher
    ..GPER may contribute to aortic relaxation while enhanced ER? expression could mediate other genomic vascular effects during pregnancy. ..
  29. De Buck M, Berghmans N, Pörtner N, Vanbrabant L, Cockx M, Struyf S, et al. Serum amyloid A1α induces paracrine IL-8/CXCL8 via TLR2 and directly synergizes with this chemokine via CXCR2 and formyl peptide receptor 2 to recruit neutrophils. J Leukoc Biol. 2015;98:1049-60 pubmed publisher
    ..g., lipopolysaccharide) inflammatory mediators induce primary chemoattractants such as serum amyloid A that synergize in an autocrine (monocyte) or a paracrine (neutrophil) fashion with secondary chemokines induced in stromal cells. ..
  30. Charron M, Vuguin P. Lack of glucagon receptor signaling and its implications beyond glucose homeostasis. J Endocrinol. 2015;224:R123-30 pubmed publisher
    ..These findings suggest that glucagon signaling plays an important role in multiple organs. Thus, treatment options designed to block Gcgr activation in diabetics may have implications beyond glucose homeostasis. ..
  31. Klein K, Caron K. Adrenomedullin in lymphangiogenesis: from development to disease. Cell Mol Life Sci. 2015;72:3115-26 pubmed publisher
  32. Zaiss M, Rapin A, Lebon L, Dubey L, Mosconi I, Sarter K, et al. The Intestinal Microbiota Contributes to the Ability of Helminths to Modulate Allergic Inflammation. Immunity. 2015;43:998-1010 pubmed publisher
  33. Tenhola S, Voutilainen R, Reyes M, Toiviainen Salo S, Juppner H, Makitie O. Impaired growth and intracranial calcifications in autosomal dominant hypocalcemia caused by a GNA11 mutation. Eur J Endocrinol. 2016;175:211-8 pubmed publisher
    ..Additional features, including short stature and early intracranial calcifications, cosegregated with the mutation. These findings may indicate a wider role for G?11 signaling besides calcium regulation. ..
  34. Kangussu L, Almeida Santos A, Moreira F, Fontes M, Santos R, Aguiar D, et al. Reduced anxiety-like behavior in transgenic rats with chronically overproduction of angiotensin-(1-7): Role of the Mas receptor. Behav Brain Res. 2017;331:193-198 pubmed publisher
    ..Therefore, facilitation of the Ang-(1-7)/Mas receptor signaling may be further investigated as an additional strategy for the treatment of anxiety-related disorders. ..
  35. 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. ..
  36. Rutkowska A, Shimshek D, Sailer A, Dev K. EBI2 regulates pro-inflammatory signalling and cytokine release in astrocytes. Neuropharmacology. 2018;133:121-128 pubmed publisher
    ..These results demonstrate a role for oxysterol/EBI2 signalling in attenuating the response of astrocytes to pro-inflammatory signals as well as limiting the levels of pro-inflammatory cytokines in the brain. ..
  37. Van Ginkel P, Yan M, Bhattacharya S, Polans A, Kenealey J. Natural products induce a G protein-mediated calcium pathway activating p53 in cancer cells. Toxicol Appl Pharmacol. 2015;288:453-62 pubmed publisher
    ..We conclude from our findings that less toxic natural products likely bind to a G protein coupled receptor that activates a G protein-mediated and calcium-dependent pathway resulting selectively in tumor cell ..
  38. Chiang W, Joseph V, Yasumura D, Matthes M, Lewin A, Gorbatyuk M, et al. Ablation of Chop Transiently Enhances Photoreceptor Survival but Does Not Prevent Retinal Degeneration in Transgenic Mice Expressing Human P23H Rhodopsin. Adv Exp Med Biol. 2016;854:185-91 pubmed publisher
    ..We suggest that other modules of the ER stress-induced UPR signaling network may be involved photoreceptor disease induced by P23H rhodopsin. ..
  39. Hohman T, Bush W, Jiang L, Brown Gentry K, Torstenson E, Dudek S, et al. Discovery of gene-gene interactions across multiple independent data sets of late onset Alzheimer disease from the Alzheimer Disease Genetics Consortium. Neurobiol Aging. 2016;38:141-150 pubmed publisher
    ..within 3 gene-gene combinations were identified: SIRT1 × ABCB1, PSAP × PEBP4, and GRIN2B × ADRA1A. In addition, we extend a previously identified interaction from an endophenotype analysis between RYR3 × ..
  40. Zhu H, Guo S, Zhang Y, Yin J, Yin W, Tao S, et al. Proton-sensing GPCR-YAP Signalling Promotes Cancer-associated Fibroblast Activation of Mesenchymal Stem Cells. Int J Biol Sci. 2016;12:389-96 pubmed publisher
    ..Finally, we show that knockdown of GPR68 in MSCs can prevent the CAF activation under cancer microenvironment. Systemic transplantation of GPR68-silenced MSCs suppresses in-situ tumour growth and prolong life span after cancer graft. ..
  41. Horiuchi H, Usami A, Shirai R, Harada N, Ikushiro S, Sakaki T, et al. S-Equol Activates cAMP Signaling at the Plasma Membrane of INS-1 Pancreatic β-Cells and Protects against Streptozotocin-Induced Hyperglycemia by Increasing β-Cell Function in Male Mice. J Nutr. 2017;147:1631-1639 pubmed publisher
    ..05).Conclusions: Our results show that S-equol boosts β-cell function and prevents hypoglycemia in mice, suggesting its potential for T2DM prevention. ..
  42. Hejnova L, Skrabalova J, Novotny J. Prolonged Morphine Treatment Alters Expression and Plasma Membrane Distribution of ?-Adrenergic Receptors and Some Other Components of Their Signaling System in Rat Cerebral Cortex. J Mol Neurosci. 2017;63:364-376 pubmed publisher
    ..However, AC activity stimulated by the beta-AR agonist isoprenaline was markedly increased. This is the first study to demonstrate lipid raft association of key components of the cortical ?-AR system and its sensitivity to morphine. ..
  43. Gu D, Ge D, Snieder H, He J, Chen S, Huang J, et al. Association of alpha1A adrenergic receptor gene variants on chromosome 8p21 with human stage 2 hypertension. J Hypertens. 2006;24:1049-56 pubmed scheme to test the association of the polymorphisms in the human alpha1A adrenergic receptor (ADRA1A) gene, located on chromosome 8p21-p11.2, with essential hypertension in a northern Han Chinese population...
  44. Masyuk T, Masyuk A, Larusso N. TGR5 in the Cholangiociliopathies. Dig Dis. 2015;33:420-5 pubmed publisher
    ..Collectively, these data suggest the involvement of TGR5 in PLD and that TGR5 targeting in cystic cholangiocytes may have therapeutic potential. ..
  45. Kargl J, Andersen L, Hasenöhrl C, Feuersinger D, Stančić A, Fauland A, et al. GPR55 promotes migration and adhesion of colon cancer cells indicating a role in metastasis. Br J Pharmacol. 2016;173:142-54 pubmed publisher
    ..GPR55 is involved in the migratory behaviour of colon carcinoma cells and may serve as a pharmacological target for the prevention of metastasis. © 2015 The British Pharmacological Society. ..
  46. Hussain A, Üçpunar H, Zhang M, Loschek L, Grunwald Kadow I. Neuropeptides Modulate Female Chemosensory Processing upon Mating in Drosophila. PLoS Biol. 2016;14:e1002455 pubmed publisher
    ..Together, our data show that neuropeptide-mediated modulation of peripheral chemosensory neurons increases a gravid female's preference for important nutrients, thereby ensuring optimal conditions for her growing progeny. ..
  47. Jastrzebska B, Comar W, Kaliszewski M, Skinner K, Torcasio M, Esway A, et al. A G Protein-Coupled Receptor Dimerization Interface in Human Cone Opsins. Biochemistry. 2017;56:61-72 pubmed publisher
    ..This last observation has the potential to open up new lines of inquiry regarding the functional role of dimerization for red cone opsin. ..
  48. Seemann W, Wenzel D, Schrage R, Etscheid J, Bödefeld T, Bartol A, et al. Engineered Context-Sensitive Agonism: Tissue-Selective Drug Signaling through a G Protein-Coupled Receptor. J Pharmacol Exp Ther. 2017;360:289-299 pubmed publisher
    ..Designed context-sensitive agonism opens an avenue toward postreceptor pharmacologic selectivity, which even works in target tissues operated by the same subtype of pharmacologic receptor. ..
  49. Taguchi K, Bessho N, Hasegawa M, Narimatsu H, Matsumoto T, Kobayashi T. Co-treatment with clonidine and a GRK2 inhibitor prevented rebound hypertension and endothelial dysfunction after withdrawal in diabetes. Hypertens Res. 2018;41:263-274 pubmed publisher
    ..These results suggest that suppression of GRK2 activity affects rebound hypertension-associated vascular endothelial dysfunction by targeting the Akt/eNOS signaling pathway. ..
  50. Patriarchi T, Shen A, He W, Baikoghli M, Cheng R, Xiang Y, et al. Nanodelivery of a functional membrane receptor to manipulate cellular phenotype. Sci Rep. 2018;8:3556 pubmed publisher
  51. Lieberman P, Garvey L. Mast Cells and Anaphylaxis. Curr Allergy Asthma Rep. 2016;16:20 pubmed publisher
  52. Ullah R, Shen Y, Zhou Y, Huang K, Fu J, Wahab F, et al. Expression and actions of GnIH and its orthologs in vertebrates: Current status and advanced knowledge. Neuropeptides. 2016;59:9-20 pubmed publisher
    ..GnIH and its orthologs form a member of the RFamide peptide family. GnIH signals via its canonical G protein coupled receptor 147 (GPR147). Both GnIH and GPR147 are expressed in hypothalamus and other brain regions...
  53. Yun H, Park K, Hong J, Kim E. Peripheral serotonin-mediated system suppresses bone development and regeneration via serotonin 6 G-protein-coupled receptor. Sci Rep. 2016;6:30985 pubmed publisher
    ..Therefore, our findings indicate a key role of 5-HT6R in bone formation through serotonin originating in the peripheral system, and suggest that it is a novel therapeutic target for drug development in the bone repair and bone diseases. ..
  54. Kaczorek E, Szarek J, Mikiewicz M, Terech Majewska E, Schulz P, Małaczewska J, et al. Effect of feed supplementation with kynurenic acid on the morphology of the liver, kidney and gills in rainbow trout (Oncorhynchus mykiss Walbaum, 1792), healthy and experimentally infected with Yersinia ruckeri. J Fish Dis. 2017;40:873-884 pubmed publisher
    ..In the fish experimentally infected, KYNA caused aggravation of the signs in the liver, kidneys and gills, and the effect was dose dependent. The results implicate that KYNA may be a stressor for fish. ..
  55. Schäfer Somi S, Ay S, Kaya D, Sozmen M, Beceriklisoy H, Agaoglu A, et al. Kisspeptin-10 and the G protein-coupled receptor 54 are differentially expressed in the canine pregnant uterus and trophoblast cells. Reprod Domest Anim. 2017;52 Suppl 2:123-129 pubmed publisher
    ..We conclude that KP-10 and GPR54 are expressed in the canine uterus and trophoblast cells. However, during pregnancy, expression of both proteins seems to be differentially regulated. ..
  56. Nag J, Rudina T, Maoz M, Grisaru Granovsky S, Uziely B, Bar Shavit R. Cancer driver G-protein coupled receptor (GPCR) induced β-catenin nuclear localization: the transcriptional junction. Cancer Metastasis Rev. 2018;37:147-157 pubmed publisher
    ..We discuss recent advances in understanding the molecular path leading to β-catenin nuclear localization and transcriptional activity and their implications for future cancer therapy research. ..
  57. Spigolon G, Fisone G. Signal transduction in L-DOPA-induced dyskinesia: from receptor sensitization to abnormal gene expression. J Neural Transm (Vienna). 2018;125:1171-1186 pubmed publisher
    ..This article provides an overview of the intracellular modifications occurring in SPN and associated with LID. ..
  58. Wang Y, Guo X, Wei A, Zhu W, Li W, Lian S. Identification of a novel mutation in a Chinese family with X-linked ocular albinism. Eur J Ophthalmol. 2009;19:124-8 pubmed
    ..The purpose of the study was to evaluate the GPR143 gene (G-protein coupled receptor 143) in a Chinese three-generation family with OA1, including four carriers and a proband with clinical features of X-linked ocular albinism...
  59. Cordomí A, Navarro G, Aymerich M, Franco R. Structures for G-Protein-Coupled Receptor Tetramers in Complex with G Proteins. Trends Biochem Sci. 2015;40:548-51 pubmed publisher
    ..Here, we use available 3D structures and biochemical considerations to present and evaluate experimentally testable structural models for GPCR oligomers and associated G proteins. ..
  60. Heifetz A, Aldeghi M, Chudyk E, Fedorov D, Bodkin M, Biggin P. Using the fragment molecular orbital method to investigate agonist-orexin-2 receptor interactions. Biochem Soc Trans. 2016;44:574-81 pubmed publisher
  61. Rajala A, Wang Y, Rajala R. Activation of oncogenic tyrosine kinase signaling promotes insulin receptor-mediated cone photoreceptor survival. Oncotarget. 2016;7:46924-46942 pubmed publisher
    ..This is the first study demonstrating the molecular mechanism of a novel signaling pathway in photoreceptor cells, which provides a window of opportunity to save the dying cones in retinal degenerative diseases. ..
  62. Kitagaki J, Miyauchi S, Asano Y, Imai A, Kawai S, Michikami I, et al. A Putative Association of a Single Nucleotide Polymorphism in GPR126 with Aggressive Periodontitis in a Japanese Population. PLoS ONE. 2016;11:e0160765 pubmed publisher
    ..The GPR126 SNP rs536714306 negatively influences this homeostasis, leading to the development of AgP, suggesting that it is a candidate genetic risk factor for AgP in the Japanese population. ..
  63. van Keulen S, Solano A, Rothlisberger U. How Rhodopsin Tunes the Equilibrium between Protonated and Deprotonated Forms of the Retinal Chromophore. J Chem Theory Comput. 2017;13:4524-4534 pubmed publisher
    ..Besides the retinal moiety and Glu113, also two water molecules as well as Thr94 and Gly90 that are related to congenital night blindness are part of this essential HB network. ..
  64. Li Z, Chen X, Wang T, Gao Y, Li F, Chen L, et al. The Corticostriatal Adenosine A2A Receptor Controls Maintenance and Retrieval of Spatial Working Memory. Biol Psychiatry. 2018;83:530-541 pubmed publisher
    ..The procognitive effect of KW6002 in nonhuman primates provides the preclinical data to translate A2AR antagonists for improving cognitive impairments in Parkinson's disease. ..
  65. Duyck K, DuTell V, Ma L, Paulson A, Yu C. Pronounced strain-specific chemosensory receptor gene expression in the mouse vomeronasal organ. BMC Genomics. 2017;18:965 pubmed publisher
    ..Moreover, noncoding RNA may offer a potential regulatory mechanism controlling the differential expression patterns. ..
  66. Claes S, D huys T, Van Hout A, Schols D, Van Loy T. A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators. J Vis Exp. 2018;: pubmed publisher
    ..Most likely this assay can be implemented, with minimal adaptations, as a generic drug discovery assay for many other GPCRs of which the activation leads to a release of intracellular Ca2+. ..
  67. Nuber S, Zabel U, Lorenz K, Nuber A, Milligan G, Tobin A, et al. β-Arrestin biosensors reveal a rapid, receptor-dependent activation/deactivation cycle. Nature. 2016;531:661-4 pubmed publisher
    ..Thus, GPCRs trigger a rapid, receptor-specific activation/deactivation cycle of β-arrestins, which permits their active signalling. ..
  68. Kim M, Biag J, Fass D, Lewis M, Zhang Q, Fleishman M, et al. Functional analysis of rare variants found in schizophrenia implicates a critical role for GIT1-PAK3 signaling in neuroplasticity. Mol Psychiatry. 2017;22:417-429 pubmed publisher
    ..Taken together, we propose that rare variants in GIT1, along with other genetic and environmental factors, cause dysregulation of PAK3 leading to synaptic deficits in SCZ. ..
  69. Cho N, Seo S, Kim D, Shin J, Ju J, Seong J, et al. Pharmacophore-based virtual screening, biological evaluation and binding mode analysis of a novel protease-activated receptor 2 antagonist. J Comput Aided Mol Des. 2016;30:625-37 pubmed publisher
    ..In conclusion, we identified new a PAR2 antagonist together with its binding mode, which provides useful insights for the design and development of PAR2 ligands. ..
  70. Chang I, Jiang S, Yang J, Su W, Chien L, Hsiao C, et al. Genetic Modifiers of Progression-Free Survival in Never-Smoking Lung Adenocarcinoma Patients Treated with First-Line Tyrosine Kinase Inhibitors. Am J Respir Crit Care Med. 2017;195:663-673 pubmed publisher
    ..Genetic variants in 4q12 merit further investigation to assess their potential as pharmacogenomic predictors for and to understand the biology underlying its influence on PFS in patients treated with TKI therapy. ..
  71. Pan B, Wang X, Kojima S, Nishioka C, Yokoyama A, Honda G, et al. The Fifth Epidermal Growth Factor-like Region of Thrombomodulin Alleviates Murine Graft-versus-Host Disease in a G-Protein Coupled Receptor 15 Dependent Manner. Biol Blood Marrow Transplant. 2017;23:746-756 pubmed publisher
    ..Our findings suggested that inducing Tregs as well as blocking activation of DCs in vivo by using TME5 is a potential therapeutic option for preventing GVHD in allo-HSCT. ..
  72. Kulkarni A, Garai S, Janero D, Thakur G. Design and Synthesis of Cannabinoid 1 Receptor (CB1R) Allosteric Modulators: Drug Discovery Applications. Methods Enzymol. 2017;593:281-315 pubmed publisher
  73. Enomoto R, Kurosawa A, Nikaido Y, Mashiko M, Saheki T, Nakajima N, et al. A novel partial agonist of GPBA reduces blood glucose level in a murine glucose tolerance test. Eur J Pharmacol. 2017;814:130-137 pubmed publisher
    ..We concluded that GUM2 is a good candidate for research on GPBA signaling under physiological conditions and for the development of GPBA-targeting therapeutic compounds. ..
  74. Singh A, Nunes J, Ateeq B. Role and therapeutic potential of G-protein coupled receptors in breast cancer progression and metastases. Eur J Pharmacol. 2015;763:178-83 pubmed publisher
  75. Miyamoto A, Mikoshiba K. Probes for manipulating and monitoring IP3. Cell Calcium. 2017;64:57-64 pubmed publisher
  76. Liu Y, Bai J, Xu X, Chen Z, Spicer L, Feng T. Effects of N-carbamylglutamate and l-arginine on gonadotrophin-releasing hormone (GnRH) gene expression and secretion in GT1-7 cells. Reprod Fertil Dev. 2017;: pubmed publisher
    ..0mM) and ARG (4.0mM) may act both directly and indirectly to regulate GnRH neuron function by downregulating genes related to GnRH synthesis and secretion to slow GnRH production while stimulating GT1-7 cell proliferation...
  77. Zhang Y, Sun B, Feng D, Hu H, Chu M, Qu Q, et al. Cryo-EM structure of the activated GLP-1 receptor in complex with a G protein. Nature. 2017;546:248-253 pubmed publisher
    ..These results provide a structural framework for understanding class B GPCR activation through hormone binding. ..
  78. Freyer L, Hsu C, Nowotschin S, Pauli A, Ishida J, Kuba K, et al. Loss of Apela Peptide in Mice Causes Low Penetrance Embryonic Lethality and Defects in Early Mesodermal Derivatives. Cell Rep. 2017;20:2116-2130 pubmed publisher
    ..Double-mutant analyses showed that loss of Apela signaling impacts early Aplnr-expressing mesodermal populations independently of the alternative ligand Apelin, leading to lethal cardiac defects in some Apela null embryos. ..
  79. Lee S, Booe J, Gingell J, Sjoelund V, Hay D, Pioszak A. N-Glycosylation of Asparagine 130 in the Extracellular Domain of the Human Calcitonin Receptor Significantly Increases Peptide Hormone Affinity. Biochemistry. 2017;56:3380-3393 pubmed publisher
    ..These results reveal an important role for N-linked glycosylation in the peptide hormone binding of a clinically relevant class B GPCR. ..
  80. Uddin M, Naider F, Becker J. Dynamic roles for the N-terminus of the yeast G protein-coupled receptor Ste2p. Biochim Biophys Acta Biomembr. 2017;1859:2058-2067 pubmed publisher
  81. Shkurin A, Vellido A. Using random forests for assistance in the curation of G-protein coupled receptor databases. Biomed Eng Online. 2017;16:75 pubmed publisher
    ..The individual identification of consistently misclassified sequences should provide a tool for quality control to GPCR database curators. ..
  82. Copik A, Baldys A, Nguyen K, Sahdeo S, Ho H, Kosaka A, et al. Isoproterenol acts as a biased agonist of the alpha-1A-adrenoceptor that selectively activates the MAPK/ERK pathway. PLoS ONE. 2015;10:e0115701 pubmed publisher
    ..Data are presented that indicate that Iso represents a novel type of α1A-AR partial agonist with signaling bias toward MAPK/ERK signaling cascade that is likely independent of coupling to Gαq. ..
  83. Liu J, Siemian J, Seaman R, Zhang Y, Li J. Role of TAAR1 within the Subregions of the Mesocorticolimbic Dopaminergic System in Cocaine-Seeking Behavior. J Neurosci. 2017;37:882-892 pubmed publisher
    ..Then, by using a local pharmacological activation method, we demonstrated that TAAR1 in different subregions of the mesocorticolimbic system distinctly contributes to cue- and drug-induced reinstatement of cocaine-seeking behavior. ..
  84. Cannavo A, Komici K, Bencivenga L, D amico M, Gambino G, Liccardo D, et al. GRK2 as a therapeutic target for heart failure. Expert Opin Ther Targets. 2017;:1-9 pubmed publisher
    ..Herein, we will update the readers about the 'state-of-art' of GRK2 inhibition as a potent therapeutic strategy in HF...
  85. Wardman J, Gomes I, Bobeck E, Stockert J, Kapoor A, Bisignano P, et al. Identification of a small-molecule ligand that activates the neuropeptide receptor GPR171 and increases food intake. Sci Signal. 2016;9:ra55 pubmed publisher
    ..Together, these results suggest that MS0015203 is a useful tool to probe the pharmacological and functional properties of GPR171 and that ligands targeting GPR171 may eventually lead to therapeutics for food-related disorders. ..
  86. Gabl M, Holdfeldt A, Sundqvist M, Lomei J, Dahlgren C, Forsman H. FPR2 signaling without ?-arrestin recruitment alters the functional repertoire of neutrophils. Biochem Pharmacol. 2017;145:114-122 pubmed publisher
    ..In summary, we provide experimental evidence of biased agonism for FPR2 and our data disclose critical roles of ?-arrestin in neutrophil chemotaxis and reactivation of desensitized receptors. ..
  87. Anbazhagan A, Priyamvada S, Gujral T, Bhattacharyya S, Alrefai W, Dudeja P, et al. A novel anti-inflammatory role of GPR120 in intestinal epithelial cells. Am J Physiol Cell Physiol. 2016;310:C612-21 pubmed publisher
    ..Our studies for the first time demonstrated a GPR120-mediated novel anti-inflammatory pathway in specific intestinal epithelial cell types that could be of therapeutic relevance to intestinal inflammatory disorders. ..
  88. Felce J, Davis S, Klenerman D. Single-Molecule Analysis of G Protein-Coupled Receptor Stoichiometry: Approaches and Limitations. Trends Pharmacol Sci. 2018;39:96-108 pubmed publisher
    ..We also emphasize that attempts to resolve the debate ought to rely on orthogonal approaches to measuring receptor stoichiometry. ..
  89. Piekielna Ciesielska J, Ferrari F, Calo G, Janecka A. Cyclopeptide Dmt-[D-Lys-p-CF3-Phe-Phe-Asp]NH2, a novel G protein-biased agonist of the mu opioid receptor. Peptides. 2018;101:227-233 pubmed publisher
    ..Such biased ligands are able to separate the biological actions of an activated receptor and have the potential to become more effective drug candidates with fewer side effects. ..
  90. Morris J, Norris P, Moore J, Jenkins J, Williams A, Canter J. Genetic variation in the autonomic nervous system affects mortality: a study of 1,095 trauma patients. J Am Coll Surg. 2009;208:663-8; discussion 668-70 pubmed publisher the adrenergic pathway were evaluated: beta-2 adrenergic receptor (ADBR2: Q27E), alpha-1a adrenergic receptor (ADRA1A:R347C), and catechol-O-methyl transferase (COMT: V158M)...
  91. Narita T, Schaap P, Saito T. Effects of deletion of the receptor CrlA on Dictyostelium aggregation and MPBD-mediated responses are strain dependent and not evident in strain Ax2. FEMS Microbiol Lett. 2017;364: pubmed publisher
    ..When transformed with PkaC, both Ax2 and Ax2/crlA- similarly responded to MPBD in vitro with spore encapsulation. Our data make it doubtful that CrlA acts as the receptor for MPBD signalling during the development of D. discoideum Ax2...
  92. Nakajima A, Nakatani A, Hasegawa S, Irie J, Ozawa K, Tsujimoto G, et al. The short chain fatty acid receptor GPR43 regulates inflammatory signals in adipose tissue M2-type macrophages. PLoS ONE. 2017;12:e0179696 pubmed publisher
    ..This newly identified facet of GPR43 in macrophages may have clinical implications for immune-metabolism related episodes. ..