Glp1r

Summary

Gene Symbol: Glp1r
Description: glucagon-like peptide 1 receptor
Alias: Glip, RATGL1RCP, glucagon-like peptide 1 receptor, GLP-1 receptor, GLP-1-R, GLP-1R, pancreatic beta cell receptor for the gluco-incretin hormone glucagon-like peptide 1
Species: rat

Top Publications

  1. pmc Glucagon-like peptide-1 receptor stimulation increases blood pressure and heart rate and activates autonomic regulatory neurons
    Hiroshi Yamamoto
    Department of Medicine and Division of Endocrinology, Beth Israel Deaconess Medical Center, Harvard Medical School, 99 Brookline Avenue, Boston, MA 02215, USA
    J Clin Invest 110:43-52. 2002
  2. ncbi Met-204 and Tyr-205 are together important for binding GLP-1 receptor agonists but not their N-terminally truncated analogues
    Rakel Lopez de Maturana
    Faculty of Biological Sciences, University of Leeds, Leeds LS2 9JT, UK
    Protein Pept Lett 11:15-22. 2004
  3. pmc Endogenous hindbrain glucagon-like peptide-1 receptor activation contributes to the control of food intake by mediating gastric satiation signaling
    Matthew R Hayes
    Graduate Groups of Psychology and Neuroscience, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    Endocrinology 150:2654-9. 2009
  4. pmc GLP-1 neurons in the nucleus of the solitary tract project directly to the ventral tegmental area and nucleus accumbens to control for food intake
    Amber L Alhadeff
    Department of Psychiatry, School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    Endocrinology 153:647-58. 2012
  5. pmc Hippocampal GLP-1 receptors influence food intake, meal size, and effort-based responding for food through volume transmission
    Ted M Hsu
    1 Neuroscience Program, University of Southern California, Los Angeles, CA, USA 2 Department of Biological Sciences, University of Southern California, Los Angeles, CA, USA
    Neuropsychopharmacology 40:327-37. 2015
  6. pmc The Aversive Agent Lithium Chloride Suppresses Phasic Dopamine Release Through Central GLP-1 Receptors
    Samantha M Fortin
    Graduate Program in Neuroscience, University of Illinois at Chicago, Chicago, IL, USA
    Neuropsychopharmacology 41:906-15. 2016
  7. pmc Cardioprotection Resulting from Glucagon-Like Peptide-1 Administration Involves Shifting Metabolic Substrate Utilization to Increase Energy Efficiency in the Rat Heart
    Karpagam Aravindhan
    Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, GlaxoSmithKline, King of Prussia, Pennsylvania, United States of America
    PLoS ONE 10:e0130894. 2015
  8. pmc Nutrient induced type 2 and chemical induced type 1 experimental diabetes differently modulate gastric GLP-1 receptor expression
    Olga Bloch
    Diabetes and Immunology Research Laboratory, Assaf Harofeh Medical Center affiliated to the Sackler Faculty of Medicine, Tel Aviv University, 70300 Zerifin, Israel
    J Diabetes Res 2015:561353. 2015
  9. pmc Activation of the GLP-1 receptors in the nucleus of the solitary tract reduces food reward behavior and targets the mesolimbic system
    Jennifer E Richard
    Department of Physiology, Institute of Neuroscience and Physiology, The Sahlgrenska Academy at the University of Gothenburg, Gothenburg, Sweden
    PLoS ONE 10:e0119034. 2015
  10. doi Hyperglycemia-induced GLP-1R downregulation causes RPE cell apoptosis
    Dong Il Kim
    College of Veterinary Medicine, Chonnam National University, Gwangju, 500 757, Republic of Korea
    Int J Biochem Cell Biol 59:41-51. 2015

Research Grants

  1. How does DHEA improve diabetic microvascular dysfunction
    JOSEPH DILLON; Fiscal Year: 2004
  2. Nephrology Training Grant
    Scott Thomson; Fiscal Year: 2008
  3. DEHYDROEPIANDROSTERONE SULFATE AND INSULIN SECRETION
    JOSEPH DILLON; Fiscal Year: 2004

Patents

  1. RECEPTOR FOR THE GLUCAGON-LIKE-PEPTIDE-1 (GLP-1)

Scientific Experts

  • Matthew R Hayes
  • Jean Philippe Krieger
  • Stephanie Sisley
  • S Thomson
  • P M Hellstrom
  • Jian Hui Liu
  • Karolina P Skibicka
  • Marco Marzioni
  • K A Al Barazanji
  • Matthew J During
  • Atsushi Nakagawa
  • D D'ALESSIO
  • JOSEPH DILLON
  • Matthew J Mahon
  • Megan J Dailey
  • C C Tseng
  • Amber L Alhadeff
  • Dong Il Kim
  • Mi Jin Moon
  • Hye Jung Kwon
  • David J Reiner
  • Samantha M Fortin
  • Baoming Mi
  • Jingru Meng
  • You Qin Jiang
  • Scott E Kanoski
  • Vaibhav R Konanur
  • Soo Hyun Park
  • Min Jung Park
  • Karpagam Aravindhan
  • Elisa P Jensen
  • Ted M Hsu
  • Olga Bloch
  • Sergiy V Korol
  • Jennifer E Richard
  • Xin Li
  • Harvey J Grill
  • Patricia Vazquez
  • Michela Riz
  • Taichi Nakamura
  • Amanda M Dossat
  • Marina Romaní-Pérez
  • Rozita Shirazi
  • Craig W Younce
  • Yan Chen
  • Lene Jessen
  • Yan Yang
  • Jae Young Seong
  • B Roger
  • Jong Ik Hwang
  • Hee Young Kim
  • Gianluca Svegliati-Baroni
  • Ye Hwang Cheong
  • Shiying Shao
  • R J Mann
  • Stephen C Woods
  • Randy J Seeley
  • V Bucinskaite
  • Ditte Tornehave
  • Carmen Sanz
  • Gang Xu
  • Torsten P Vahl
  • S Wan
  • Elvira Alvarez
  • Enrique Blazquez
  • Alfred Aziz
  • Dan Donnelly
  • Rakel Lopez de Maturana
  • Suleiman Al-Sabah
  • Iwona Bogacka
  • Gerlinda E Hermann
  • Yiwei Wu
  • Dong Ying Zhang
  • Huinan Zhang
  • Yazhou Li
  • Ho Chan Cho
  • Yunying Wang
  • Mingkai Li
  • Chunjing Yu
  • Xiaoxing Luo
  • Yuping Xu
  • Ying Zhou
  • Derek J Zimmer
  • Meeyul Hwang
  • Elizabeth G Mietlicki-Baase
  • Lizhen Wang
  • Long Bi
  • Su Kyung Shin
  • Min Jia
  • Gregory L Sousa

Detail Information

Publications73

  1. pmc Glucagon-like peptide-1 receptor stimulation increases blood pressure and heart rate and activates autonomic regulatory neurons
    Hiroshi Yamamoto
    Department of Medicine and Division of Endocrinology, Beth Israel Deaconess Medical Center, Harvard Medical School, 99 Brookline Avenue, Boston, MA 02215, USA
    J Clin Invest 110:43-52. 2002
    ..These findings suggest that the central GLP-1 system represents a regulator of sympathetic outflow leading to downstream activation of cardiovascular responses in vivo...
  2. ncbi Met-204 and Tyr-205 are together important for binding GLP-1 receptor agonists but not their N-terminally truncated analogues
    Rakel Lopez de Maturana
    Faculty of Biological Sciences, University of Leeds, Leeds LS2 9JT, UK
    Protein Pept Lett 11:15-22. 2004
    ..This suggests that the locus is important for the formation of the binding site for the N-terminal residues of peptide agonists...
  3. pmc Endogenous hindbrain glucagon-like peptide-1 receptor activation contributes to the control of food intake by mediating gastric satiation signaling
    Matthew R Hayes
    Graduate Groups of Psychology and Neuroscience, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    Endocrinology 150:2654-9. 2009
    ..We conclude that endogenous NTS GLP-1R activation driven by gastric satiation signals contributes to the control of normal feeding...
  4. pmc GLP-1 neurons in the nucleus of the solitary tract project directly to the ventral tegmental area and nucleus accumbens to control for food intake
    Amber L Alhadeff
    Department of Psychiatry, School of Medicine, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    Endocrinology 153:647-58. 2012
    ..Current data highlight these nuclei within the MRS as novel sites for GLP-1R-mediated control of food intake and body weight...
  5. pmc Hippocampal GLP-1 receptors influence food intake, meal size, and effort-based responding for food through volume transmission
    Ted M Hsu
    1 Neuroscience Program, University of Southern California, Los Angeles, CA, USA 2 Department of Biological Sciences, University of Southern California, Los Angeles, CA, USA
    Neuropsychopharmacology 40:327-37. 2015
    ..Collectively these findings illuminate novel neuronal and behavioral mechanisms mediating food intake reduction by GLP-1...
  6. pmc The Aversive Agent Lithium Chloride Suppresses Phasic Dopamine Release Through Central GLP-1 Receptors
    Samantha M Fortin
    Graduate Program in Neuroscience, University of Illinois at Chicago, Chicago, IL, USA
    Neuropsychopharmacology 41:906-15. 2016
    ..By delivering Ex-9 to either the lateral or fourth ventricle, we highlight a population of central GLP-1 receptors rostral to the hindbrain that are involved in the LiCl-mediated suppression of NAc dopamine release. ..
  7. pmc Cardioprotection Resulting from Glucagon-Like Peptide-1 Administration Involves Shifting Metabolic Substrate Utilization to Increase Energy Efficiency in the Rat Heart
    Karpagam Aravindhan
    Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, GlaxoSmithKline, King of Prussia, Pennsylvania, United States of America
    PLoS ONE 10:e0130894. 2015
    ....
  8. pmc Nutrient induced type 2 and chemical induced type 1 experimental diabetes differently modulate gastric GLP-1 receptor expression
    Olga Bloch
    Diabetes and Immunology Research Laboratory, Assaf Harofeh Medical Center affiliated to the Sackler Faculty of Medicine, Tel Aviv University, 70300 Zerifin, Israel
    J Diabetes Res 2015:561353. 2015
    ..These results suggest that induced T1DM and T2DM may differently modulate GLP-1R system in enteropancreatic axis. ..
  9. pmc Activation of the GLP-1 receptors in the nucleus of the solitary tract reduces food reward behavior and targets the mesolimbic system
    Jennifer E Richard
    Department of Physiology, Institute of Neuroscience and Physiology, The Sahlgrenska Academy at the University of Gothenburg, Gothenburg, Sweden
    PLoS ONE 10:e0119034. 2015
    ..These data reveal a food reward-suppressing role of the NTS GLP-1R and indicate that the neurobiological targets underlying food reward control are not limited to the mesolimbic system, instead they are distributed throughout the CNS. ..
  10. doi Hyperglycemia-induced GLP-1R downregulation causes RPE cell apoptosis
    Dong Il Kim
    College of Veterinary Medicine, Chonnam National University, Gwangju, 500 757, Republic of Korea
    Int J Biochem Cell Biol 59:41-51. 2015
    ..Our data suggested that regulation of GLP-1R expression is a promising approach for the treatment of diabetic retinopathy. ..
  11. pmc Expression of CTRP3, a novel adipokine, in rats at different pathogenic stages of type 2 diabetes mellitus and the impacts of GLP-1 receptor agonist on it
    Xin Li
    Department of Endocrinology, Zhongnan Hospital, Wuhan University, Wuhan 430071, China
    J Diabetes Res 2014:398518. 2014
    ....
  12. doi GLP-1 and exendin-4 transiently enhance GABAA receptor-mediated synaptic and tonic currents in rat hippocampal CA3 pyramidal neurons
    Sergiy V Korol
    Department of Neuroscience, Uppsala University, Uppsala, Sweden
    Diabetes 64:79-89. 2015
    ..The results demonstrate GLP-1 receptor regulation of hippocampal function and are consistent with GLP-1 receptor agonists enhancing GABAA signaling by pre- and postsynaptic mechanisms...
  13. doi Activation of GLP-1 receptors on vascular smooth muscle cells reduces the autoregulatory response in afferent arterioles and increases renal blood flow
    Elisa P Jensen
    Department of Biomedical Sciences, Faculty of Health Sciences, University of Copenhagen, Copenhagen, Denmark NNF Center for Basic Metabolic Research, Panum Institute, University of Copenhagen, Copenhagen, Denmark and
    Am J Physiol Renal Physiol 308:F867-77. 2015
    ..Activation of these receptors reduces the autoregulatory response of afferent arterioles to acute pressure increases and increases RBF in normotensive rats. ..
  14. pmc Nucleus accumbens GLP-1 receptors influence meal size and palatability
    Amanda M Dossat
    Department of Psychology and Program in Neuroscience, Florida State University, Tallahassee, Florida
    Am J Physiol Endocrinol Metab 304:E1314-20. 2013
    ..Together, our results suggest that NAcC Ex9 influences taste evaluation. We conclude that GLP-1 released in NAcC in response to gastrointestinal nutrients reduces the hedonic value of food. ..
  15. pmc Glucagon-like peptide 1 receptor induced suppression of food intake, and body weight is mediated by central IL-1 and IL-6
    Rozita Shirazi
    Department of Physiology, Institute of Neuroscience and Physiology, Sahlgrenska Academy at the University of Gothenburg, SE 405 30 Gothenburg, Sweden
    Proc Natl Acad Sci U S A 110:16199-204. 2013
    ..These data outline a previously unidentified role of the central IL-1 and IL-6 in mediating the anorexic and body weight loss effects of GLP-1 receptor activation. ..
  16. pmc PSCs and GLP-1R: occurrence in normal pancreas, acute/chronic pancreatitis and effect of their activation by a GLP-1R agonist
    Taichi Nakamura
    1 Department of Medicine and Bioregulatory Science, Kyushu University, Fukuoka, Japan 2 Department of Cell Biology Section, NIDDK, National Institutes of Health, Bethesda, MD, USA
    Lab Invest 94:63-78. 2014
    ..These results suggest chronic treatment with GLP-1R agonists could lead to proliferation/chronic activation of PSCs, which may lead to important effects in the pancreas. ..
  17. doi Minimal modeling of insulin secretion in the perfused rat pancreas: a drug effect case study
    Michela Riz
    Department of Information Engineering, University of Padua, Paduaa, Italy and
    Am J Physiol Endocrinol Metab 306:E627-34. 2014
    ..7- vs. 13.1-fold increase in ΦD and 2.3- vs. 2.8-fold increase in ΦS) and demonstrated that SAR1 leads to an additional improvement of β-cell function in the presence of postprandial GLP-1 levels. ..
  18. pmc Glucagon-like Peptide-1 receptor signaling in the lateral parabrachial nucleus contributes to the control of food intake and motivation to feed
    Amber L Alhadeff
    Department of Psychology, University of Pennsylvania, Philadelphia, PA, USA
    Neuropsychopharmacology 39:2233-43. 2014
    ..Taken together, these data establish the lPBN as a novel site of action for GLP-1R-mediated control of food intake and reward. ..
  19. pmc Differences in acute anorectic effects of long-acting GLP-1 receptor agonists in rats
    Stephanie Sisley
    Department of Pediatrics, Division of Endocrinology, Cincinnati Children s Hospital Medical Center, Cincinnati, OH, United States Electronic address
    Peptides 58:1-6. 2014
    ..Additionally, we show here that the glucose lowering properties of acute administration of GLP-1R agonists are not accounted for by their central effects...
  20. pmc Hindbrain nucleus tractus solitarius glucagon-like peptide-1 receptor signaling reduces appetitive and motivational aspects of feeding
    Amber L Alhadeff
    Department of Psychology, University of Pennsylvania, Philadelphia, Pennsylvania
    Am J Physiol Regul Integr Comp Physiol 307:R465-70. 2014
    ..Together, these data demonstrate that the intake inhibitory effects of mNTS GLP-1R signaling extend beyond satiation and include effects on food reward and motivation that are typically ascribed to midbrain and forebrain neurons. ..
  21. doi Geniposide Prevents Hypoxia/Reoxygenation-Induced Apoptosis in H9c2 Cells: Improvement of Mitochondrial Dysfunction and Activation of GLP-1R and the PI3K/AKT Signaling Pathway
    You Qin Jiang
    Department of Cardiology, First Affiliated Hospital of Chongqing Medical University, Chongqing Key Laboratory of Ophthalmology, Chongqing, China
    Cell Physiol Biochem 39:407-21. 2016
    ..Ellis, on cardiomyocyte apoptosis induced by hypoxia/reoxygenation (H/R) in H9c2 cells, and their underlying mechanisms...
  22. doi Non-invasive glucagon-like peptide-1 receptor imaging in pancreas with (18)F-Al labeled Cys(39)-exendin-4
    Baoming Mi
    Department of Nuclear Medicine, The First Affiliated Hospital of Soochow University, Suzhou, Jiangsu, 215006, China Department of Nuclear Medicine, Affiliated Hospital of Jiangnan University Wuxi 4th People s Hospital, Wuxi, Jiangsu, 214062, China
    Biochem Biophys Res Commun 471:47-51. 2016
    ..In the present study, (18)F-Al labeled exendin-4 analog, (18)F-Al-NOTA-MAL-Cys(39)-exendin-4, was evaluated for PET imaging GLP-1R in the pancreas...
  23. doi Metformin ameliorates lipotoxicity-induced mesangial cell apoptosis partly via upregulation of glucagon like peptide-1 receptor (GLP-1R)
    Dong Il Kim
    College of Veterinary Medicine, Chonnam National University, Gwangju 500 757, South Korea Life Science Institute, University of Michigan, Ann Arbor, MI 48109, USA Electronic address
    Arch Biochem Biophys 584:90-7. 2015
    ..Our data suggested that regulation of GLP-1R expression could be a promising approach to treat diabetic nephropathy and the novel mechanism of metformin mediated GLP-1R regulation. ..
  24. pmc Activation of GLP-1 Receptor Promotes Bone Marrow Stromal Cell Osteogenic Differentiation through β-Catenin
    Jingru Meng
    Department of Pharmacology, School of Pharmacy, Fourth Military Medical University, Xi an 710032, China
    Stem Cell Reports 6:579-91. 2016
    ..These findings reveal that GLP-1 receptor regulates BMSC osteogenic differentiation and provide a molecular basis for therapeutic potential of GLP-1 against osteoporosis...
  25. doi Evidence for glucagon-like peptide-1 receptor signaling to activate ATP-sensitive potassium channels in pancreatic beta cells
    Hye Jung Kwon
    Department of Physiology and Obesity mediated Disease Research Center, Keimyung University School of Medicine, 1095 Dalgubeoldae ro, Dalseo Gu, Daegu 42601, South Korea
    Biochem Biophys Res Commun 469:216-21. 2016
    ..This alternative mechanism of GLP-1 function may act as a negative feedback pathway, modulating the glucose-dependent GLP-1 inhibition on KATP channel activity. ..
  26. pmc Astrocytes Regulate GLP-1 Receptor-Mediated Effects on Energy Balance
    David J Reiner
    Translational Neuroscience Program, Department of Psychiatry, Perelman School of Medicine, and
    J Neurosci 36:3531-40. 2016
    ..Collectively, data demonstrate a role for NTS astrocytic GLP-1R signaling in energy balance control...
  27. doi Knockdown of GLP-1 Receptors in Vagal Afferents Affects Normal Food Intake and Glycemia
    Jean Philippe Krieger
    Physiology and Behavior Laboratory, Institute of Food, Nutrition, and Health, ETH Zurich, Zurich, Switzerland
    Diabetes 65:34-43. 2016
    ..Collectively, our results highlight a crucial role for the VANs in mediating the effects of endogenous GLP-1 on food intake and glycemia and may promote the further development of GLP-1-based therapies...
  28. ncbi Mutations to the third cytoplasmic domain of the glucagon-like peptide 1 (GLP-1) receptor can functionally uncouple GLP-1-stimulated insulin secretion in HIT-T15 cells
    A M Salapatek
    Department of Medicine and Physiology, University of Toronto, Ontario, Canada
    Mol Endocrinol 13:1305-17. 1999
    ....
  29. ncbi Effect of GIP and GLP-1 antagonists on insulin release in the rat
    C C Tseng
    Section of Gastroenterology, Boston University School of Medicine, Boston, Massachusetts 02118, USA
    Am J Physiol 276:E1049-54. 1999
    ..The results of these studies suggest that GIP and GLP-1 may share a common mechanism in stimulating pancreatic insulin release. Furthermore, the GIP receptor appears to play a role in facilitating glucose uptake in the small intestine...
  30. doi Pulmonary GLP-1 receptor increases at birth and exogenous GLP-1 receptor agonists augmented surfactant-protein levels in litters from normal and nitrofen-treated pregnant rats
    Marina Romaní-Pérez
    Endocrinology Laboratory, Biomedical Research Centre Centro Investigaciones Biomédicas, University of Vigo, Campus As Lagoas Marcosende, E 36310 Vigo, Spain
    Endocrinology 154:1144-55. 2013
    ..Taken together, our results demonstrate the importance of the GLP-1 system in regulating SP production and lung development...
  31. doi Role of glucagon-like peptide-1 in the pathogenesis of experimental irritable bowel syndrome rat models
    Yan Chen
    Department of Gastroenterology, The First Affiliated Hospital of Nanjing Medical University, Nanjing, Jiangsu 210029, PR China
    Int J Mol Med 31:607-13. 2013
    ..In conclusion, these results indicated that GLP-1 and GLP-1R are implicated in the pathogenesis of IBS-C and IBS-D...
  32. ncbi Glucose intolerance but normal satiety in mice with a null mutation in the glucagon-like peptide 1 receptor gene
    L A Scrocchi
    Department of Medicine, University of Toronto, Ontario
    Nat Med 2:1254-8. 1996
    ..behavior and insulin secretion, we have generated mice with a targeted disruption of the GLP1 receptor gene (GLP1R)...
  33. doi Exendin-4 attenuates high glucose-induced cardiomyocyte apoptosis via inhibition of endoplasmic reticulum stress and activation of SERCA2a
    Craig W Younce
    Metabolic Signaling and Disease Program, Diabetes and Obesity Research Center, Sanford Burnham Medical Research Institute at Lake Nona, 6400 Sanger Rd, Orlando, FL 32837, USA
    Am J Physiol Cell Physiol 304:C508-18. 2013
    ..Glucagon-like peptide-1 (Glp1) receptor (Glp1r) agonists improve cardiac function and survival in response to ischemia-reperfusion and myocardial infarction...
  34. pmc Suppression of food intake by glucagon-like peptide-1 receptor agonists: relative potencies and role of dipeptidyl peptidase-4
    Lene Jessen
    Division of Endocrinology, University of Cincinnati, Cincinnati, OH 45237, USA
    Endocrinology 153:5735-45. 2012
    ..These findings suggest distinct potencies of GLP-1 receptor agonists on food intake that cannot be explained by plasma pharmacokinetics...
  35. pmc Glucagon-like peptide-1 receptor stimulation increases GFR and suppresses proximal reabsorption in the rat
    Scott C Thomson
    Department of Medicine, University of California and Veterans Affairs San Diego Healthcare System, San Diego, California 92161, USA
    Am J Physiol Renal Physiol 304:F137-44. 2013
    ....
  36. doi Receptor-mediated inhibition of small bowel migrating complex by GLP-1 analog ROSE-010 delivered via pulmonary and systemic routes in the conscious rat
    P M Hellstrom
    Department of Medical Sciences, Uppsala University, Uppsala, Sweden
    Regul Pept 179:71-6. 2012
    ..Accordingly, we investigated whether ROSE-010 works through GLP-1 receptors in gut musculature and its effectiveness when administered by pulmonary inhalation...
  37. ncbi Glucagon-like peptide-1 (GLP-1) releases thyrotropin (TSH): characterization of binding sites for GLP-1 on alpha-TSH cells
    S A Beak
    Department of Medicine, Royal Postgraduate Medical School, Hammersmith Hospital, London, United Kingdom
    Endocrinology 137:4130-8. 1996
    ..h; control, 35 +/- 1 fmol/10(6) cells.h; P < 0.0005), but had no effect on basal PRL, GH, or LH release...
  38. pmc Evolutionarily conserved residues at glucagon-like peptide-1 (GLP-1) receptor core confer ligand-induced receptor activation
    Mi Jin Moon
    Graduate School of Medicine, Korea University, Seoul 136 705, Korea
    J Biol Chem 287:3873-84. 2012
    ..insulinotropic polypeptide (GIP) play important roles in insulin secretion through their receptors, GLP1R and GIPR...
  39. ncbi The third cytoplasmic domain of the GLP-1[7-36 amide] receptor is required for coupling to the adenylyl cyclase system
    S Takhar
    Department of Medicine, University of Toronto, ON, Canada
    Endocrinology 137:2175-8. 1996
    ..01). These results strongly suggest that within the IC3 domain the N-terminal KLK sequence or a portion thereof (specifically K-334) is required for the efficient coupling of the tGLP-1 receptor to the AC system...
  40. pmc Expression of the GLP-1 receptor in mouse, rat, and human pancreas
    Ditte Tornehave
    Department of Developmental Biology, Hagedorn Research Institute, Niels Steensensvej 6, DK2820 Gentofte, Denmark
    J Histochem Cytochem 56:841-51. 2008
    ..This manuscript contains online supplemental material at http://www.jhc.org. Please visit this article online to view these materials...
  41. ncbi The recombinant rat glucagon-like peptide-1 receptor, expressed in an alpha-cell line, is coupled to adenylyl cyclase activation and intracellular calcium release
    J S Dillon
    Division of Endocrinology, Department of Internal Medicine, University of Iowa, Iowa City, IA 52246, USA
    Exp Clin Endocrinol Diabetes 113:182-9. 2005
    ..Finally this study describes a cell line that can be used as a model system for evaluation of GLP-1 signaling in alpha-cells...
  42. ncbi Glucagon-like peptide-1 excites pancreas-projecting preganglionic vagal motoneurons
    S Wan
    Dept of Neuroscience, Pennington Biomedical Research Center, Louisiana State Univ System, Baton Rouge, LA 70808, USA
    Am J Physiol Gastrointest Liver Physiol 292:G1474-82. 2007
    ..e., putative endocrine secretion-controlling neurons) could be distinguished from neurons responsive to PP (i.e., putative exocrine secretion-controlling neurons)...
  43. ncbi Downregulation of GLP-1 and GIP receptor expression by hyperglycemia: possible contribution to impaired incretin effects in diabetes
    Gang Xu
    Section of Islet Transplantation and Cell Biology, Joslin Diabetes Center, Harvard Medical School, Boston, MA 02215, USA
    Diabetes 56:1551-8. 2007
    ..Taken together, GLP-1 and GIP receptor expression is decreased with chronic hyperglycemia, and this decrease likely contributes to the impaired incretin effects found in diabetes...
  44. ncbi Glucagon-like peptide-1 (GLP-1) receptors expressed on nerve terminals in the portal vein mediate the effects of endogenous GLP-1 on glucose tolerance in rats
    Torsten P Vahl
    Department of Internal Medicine, Division of Endocrinology and Metabolism, University of Cincinnati, 2170 East Galbraith Road, Cincinnati, Ohio 45267, USA
    Endocrinology 148:4965-73. 2007
    ..These data are consistent with an important component of neural mediation of GLP-1 action...
  45. ncbi Calmodulin interacts with the cytoplasmic tails of the parathyroid hormone 1 receptor and a sub-set of class b G-protein coupled receptors
    Matthew J Mahon
    Endocrine Unit, Massachusetts General Hospital, 50 Blossom Street, Wellman 501, Boston, MA 02114 2696, USA
    FEBS Lett 579:803-7. 2005
    ..Fluphenazine, a calmodulin antagonist, enhances PTH-mediated accumulation of total inositol phosphates, suggesting that calmodulin regulates signaling via phospholipase C...
  46. ncbi Glucagon-like peptide-1 and its receptor agonist exendin-4 modulate cholangiocyte adaptive response to cholestasis
    Marco Marzioni
    Department of Gastroenterology, Universita Politecnica delle Marche, Ancona, Italy
    Gastroenterology 133:244-55. 2007
    ..GLP-1 receptor (GLP-1R) selective agonist exendin-4 is used in humans as a novel therapeutic tool for diabetes. The aim of this study was to define if GLP-1 modulates cholangiocyte biologic response to cholestasis...
  47. pmc Jejunal linoleic acid infusions require GLP-1 receptor signaling to inhibit food intake: implications for the effectiveness of Roux-en-Y gastric bypass
    Megan J Dailey
    Department of Psychiatry and Behavioral Sciences, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
    Am J Physiol Endocrinol Metab 301:E1184-90. 2011
    ..Whether increased secretion of additional gut peptides is also necessary for such suppressions remains to be determined...
  48. doi Receptor-mediated activation of gastric vagal afferents by glucagon-like peptide-1 in the rat
    V Bucinskaite
    Department of Physiology and Pharmacology, Karolinska Institutet, Stockholm, Sweden
    Neurogastroenterol Motil 21:978-e78. 2009
    ..GLP-2 receptors appear not be functionally expressed on vagal afferents...
  49. ncbi Receptor gene expression of glucagon-like peptide-1, but not glucose-dependent insulinotropic polypeptide, in rat nodose ganglion cells
    Atsushi Nakagawa
    Department of Internal Medicine, Kanazawa Medical University, Daigaku 1 1, Uchinada 920 0293, Japan
    Auton Neurosci 110:36-43. 2004
    ..The present results offer, for the first time, the molecular basis for the vagal chemoreception of GLP-1 via its specific receptor...
  50. doi SREBP-1c, Pdx-1, and GLP-1R involved in palmitate-EPA regulated glucose-stimulated insulin secretion in INS-1 cells
    Shiying Shao
    Division of Endocrinology, Tongji Hospital, Tongji Medical College of Huazhong University of Science and Technology, Wuhan 430030, PR China
    J Cell Biochem 111:634-42. 2010
    ..These results suggested that sequent SREBP-1c-Pdx-1-GLP-1R signal pathway was involved in the palmitate-caused GSIS impairment in beta cells...
  51. ncbi Glucagon-like peptide-1 receptor is involved in learning and neuroprotection
    Matthew J During
    Department of Molecular Medicine and Pathology, University of Auckland, Private Bag 92019, Auckland 86716, New Zealand
    Nat Med 9:1173-9. 2003
    ..GLP-1R-deficient mice have a phenotype characterized by a learning deficit that is restored after hippocampal Glp1r gene transfer. In addition, rats overexpressing GLP-1R in the hippocampus show improved learning and memory...
  52. ncbi Glucagon-like peptide-1 receptor signaling modulates beta cell apoptosis
    Yazhou Li
    Department of Medicine, Banting and Best Diabetes Centre, Toronto General Hospital, University of Toronto, Ontario M5G 2C4, Canada
    J Biol Chem 278:471-8. 2003
    ....
  53. pmc Expression cloning of the pancreatic beta cell receptor for the gluco-incretin hormone glucagon-like peptide 1
    B Thorens
    Institute of Pharmacology and Toxicology, University of Lausanne, Switzerland
    Proc Natl Acad Sci U S A 89:8641-5. 1992
    ..Sequence homology is found only with the receptors for secretin, calcitonin, and parathyroid hormone, which form a newly characterized family of G-coupled receptors...
  54. doi Glucagon-like peptide-1 receptor activation stimulates hepatic lipid oxidation and restores hepatic signalling alteration induced by a high-fat diet in nonalcoholic steatohepatitis
    Gianluca Svegliati-Baroni
    Department of Gastroenterology, Polytechnic University of Marche, Ancona, Italy
    Liver Int 31:1285-97. 2011
    ..The aim of this study was to investigate the presence of hepatic GLP-1r and the effect of exenatide, a GLP-1 analogue, on hepatic signalling...
  55. doi Adenylyl cyclase 8 is central to glucagon-like peptide 1 signalling and effects of chronically elevated glucose in rat and human pancreatic beta cells
    B Roger
    Universite de Bordeaux 1, Institut Europeen de Chimie et Biologie, UMR CNRS 5248, 2 Av Robert Escarpit, 33607 Pessac, France
    Diabetologia 54:390-402. 2011
    ..We therefore investigated long-term effects of glucose on this pathway with special regard to the incretin glucagon-like peptide 1 (GLP-1)...
  56. ncbi Geniposide, a novel agonist for GLP-1 receptor, prevents PC12 cells from oxidative damage via MAP kinase pathway
    Jianhui Liu
    Research Center of Pharmaceutical Chemistry and Chemobiology, Chongqing Technology and Business University, Chongqing 400067, China
    Neurochem Int 51:361-9. 2007
    ..All these data demonstrate that geniposide, an agonist for GLP-1 receptor, regulates expression of anti-oxidative proteins including HO-1 and Bcl-2 by activating the transcriptor of p90RSK via MAPK signaling pathway in PC12 cells...
  57. ncbi Molecular cloning of a cDNA encoding for the GLP-1 receptor expressed in rat lung
    B Lankat-Buttgereit
    Clinical Research Unit for Gastrointestinal Endocrinology, Philipps University of Marburg, Germany
    Exp Clin Endocrinol 102:341-7. 1994
    ....
  58. ncbi Exendin-4 stimulates both beta-cell replication and neogenesis, resulting in increased beta-cell mass and improved glucose tolerance in diabetic rats
    G Xu
    Elliott P Joslin Research Laboratories, Joslin Diabetes Center, Boston, Massachusetts 02215, USA
    Diabetes 48:2270-6. 1999
    ..Thus, GLP-I and analogs thereof hold promise as a novel therapy to stimulate beta-cell growth and differentiation when administered to diabetic individuals with reduced beta-cell mass...
  59. ncbi Central exendin-4 infusion reduces body weight without altering plasma leptin in (fa/fa) Zucker rats
    K A Al-Barazanji
    SmithKline Beecham Pharmaceuticals, Department of Vascular Biology, New Frontiers Science Park, Harlow, Essex, United Kingdom
    Obes Res 8:317-23. 2000
    ..To investigate whether chronic administration of the long-acting glucagon-like peptide-1 receptor agonist exendin-4 can elicit sustained reductions in food intake and body weight and whether its actions require an intact leptin system...
  60. pmc Over-expression of the glucagon-like peptide-1 receptor on INS-1 cells confers autocrine stimulation of insulin gene promoter activity: a strategy for production of pancreatic beta-cell lines for use in transplantation
    Oleg G Chepurny
    Department of Physiology and Neuroscience, New York University School of Medicine, New York, NY 10016, USA
    Cell Tissue Res 307:191-201. 2002
    ....
  61. ncbi The primary ligand-binding interaction at the GLP-1 receptor is via the putative helix of the peptide agonists
    Suleiman Al-Sabah
    School of Biomedical Sciences, University of Leeds, Leeds LS2 9JT, UK
    Protein Pept Lett 11:9-14. 2004
    ....
  62. ncbi Expression levels of genes likely involved in glucose-sensing in the obese Zucker rat brain
    Iwona Bogacka
    Pennington Biomedical Research Center, Louisiana State University, 6400 Perkins Road, Baton Rouge, LA 70808, USA
    Nutr Neurosci 7:67-74. 2004
    ..Furthermore, the hindbrain may be an important site for glucose-sensing where major phenotypic changes occur for glucose-sensing genes expression...
  63. ncbi Hyperglycemia after protein ingestion concurrent with injection of a GLP-1 receptor agonist in rats: a possible role for dietary peptides
    Alfred Aziz
    Dept of Nutritional Sciences, Faculty of Medicine, University of Toronto, 3rd floor FitzGerald Bldg, 150 College Street, Toronto, Ontario, Canada M5S 3E2
    Am J Physiol Regul Integr Comp Physiol 289:R688-94. 2005
    ....
  64. ncbi The cytoplasmic domain close to the transmembrane region of the glucagon-like peptide-1 receptor contains sequence elements that regulate agonist-dependent internalisation
    Patricia Vazquez
    Departamento de Bioquimica y Biologia Molecular, Facultad de Medicina, Universidad Complutense, Ciudad Universitaria, 28040 Madrid, Spain
    J Endocrinol 186:221-31. 2005
    ..Our findings indicate that the neighbouring trans-membrane domain of the carboxyl-terminal tail of the GLP-1 receptor contains sequence elements that regulate agonist-dependent internalisation and transmembrane signalling...
  65. doi Glucose exposure pattern determines glucagon-like peptide 1 receptor expression and signaling through endoplasmic reticulum stress in rat insulinoma cells
    Ye Hwang Cheong
    Research Center, Dong A Pharmaceuticals Co Ltd, 47 5 Sanggal dong, Giheung gu, Yongin si, Gyeonggi do 446 905, Republic of Korea
    Biochem Biophys Res Commun 414:220-5. 2011
    ..Collectively, these findings indicated that glucose fluctuation reduces GLP-1R expression through ER stress more profoundly than sustained hyperglycemia, which may contribute to the diminished response of GLP-1...
  66. ncbi Fasting and postprandial concentrations of GLP-1 in intestinal lymph and portal plasma: evidence for selective release of GLP-1 in the lymph system
    David D'Alessio
    Department of Medicine, University of Cincinnati, Cincinnati, Ohio 45267, USA
    Am J Physiol Regul Integr Comp Physiol 293:R2163-9. 2007
    ..In addition, these data raise the possibility that intestinal lymph may serve as a specialized signaling conduit for regulatory peptides secreted by gastrointestinal endocrine cells...
  67. ncbi Leptin but not neuropeptide Y up-regulated glucagon-like peptide 1 receptor expression in GT1-7 cells and rat hypothalamic slices
    Carmen Sanz
    Department of Biochemistry and Molecular Biology, Faculty of Medicine, Complutense University, 28040 Madrid, Spain
    Metabolism 57:40-8. 2008
    ..In addition, the different responses of the VMH and LH may be related to specific functions of these structures, as already known in vivo, highlighting the interest of hypothalamic slices for this kind of study...
  68. pmc Caudal brainstem processing is sufficient for behavioral, sympathetic, and parasympathetic responses driven by peripheral and hindbrain glucagon-like-peptide-1 receptor stimulation
    Matthew R Hayes
    Graduate Groups of Psychology and Neuroscience, University of Pennsylvania, 3720 Walnut Street, Philadelphia, Pennsylvania 19104, USA
    Endocrinology 149:4059-68. 2008
    ..Contrary to the literature, hypothalamic/forebrain processing and forebrain-caudal brainstem communication is not required for the observed responses...
  69. pmc Hindbrain cocaine- and amphetamine-regulated transcript induces hypothermia mediated by GLP-1 receptors
    Karolina P Skibicka
    Graduate Group of Psychology, University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    J Neurosci 29:6973-81. 2009
    ..Data reveal a novel function of CART in temperature regulation and open possibilities for future studies on the clinical potential of the hypothermic effect...
  70. pmc The major determinant of exendin-4/glucagon-like peptide 1 differential affinity at the rat glucagon-like peptide 1 receptor N-terminal domain is a hydrogen bond from SER-32 of exendin-4
    R J Mann
    Institute of Membrane and Systems Biology, Faculty of Biological Sciences, University of Leeds, Leeds, UK
    Br J Pharmacol 160:1973-84. 2010
    ..Our aim was to clarify the pharmacology of GLP-1R in the context of these new structural data...
  71. doi Tyr1 and Ile7 of glucose-dependent insulinotropic polypeptide (GIP) confer differential ligand selectivity toward GIP and glucagon-like peptide-1 receptors
    Mi Jin Moon
    Graduate School of Medicine, Korea University, Seoul 136 705, Korea
    Mol Cells 30:149-54. 2010
    ..insulin secretion from pancreatic beta cells through their distinct yet related G protein-coupled receptors, GLP1R and GIPR...
  72. pmc Intracellular signals mediating the food intake-suppressive effects of hindbrain glucagon-like peptide-1 receptor activation
    Matthew R Hayes
    Department of Psychology, School of Arts and Sciences, University of Pennsylvania, 3720 Walnut Street, Philadelphia, PA 19104, USA
    Cell Metab 13:320-30. 2011
    ..Pharmacotherapies targeting these signaling pathways, which mediate intake-suppressive effects of CNS GLP-1R activation, may prove efficacious in treating obesity...

Research Grants3

  1. How does DHEA improve diabetic microvascular dysfunction
    JOSEPH DILLON; Fiscal Year: 2004
    ..Thus, the successful completion of our project will advance our long-term goal of developing novel therapeutic vasoactive agents, to decrease the morbidity related to diabetic vascular dysfunction. ..
  2. Nephrology Training Grant
    Scott Thomson; Fiscal Year: 2008
    ..An interactive research environment and shared seminar programs between UCSD, Salk Institute, and numerous other research institutes in La Jolla further enhances the training program. ..
  3. DEHYDROEPIANDROSTERONE SULFATE AND INSULIN SECRETION
    JOSEPH DILLON; Fiscal Year: 2004
    ..4) Assess the effects of DHEAS on ACS activity, glucose-stimulated insulin secretion and ACO mRNA expression in human pancreatic islets. ..

Patents1

  1. RECEPTOR FOR THE GLUCAGON-LIKE-PEPTIDE-1 (GLP-1)
    Patent Number: WO9319175-A1; Date:1993-09-30