Skip to main content
SpringerLink
Log in

Molecular pharmacology of somatostatin receptor subtypes

  • Review Article
  • Published:
Journal of Endocrinological Investigation Aims and scope Submit manuscript

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

References

  1. Brazeau P., Vale W., Burgus R., Ling N., Butcher M., Rivier J., Guillemin R. Hypothalamic polypeptide that inhibits the secretion of immunoreactive pituitary growth hormone. Science 179: 77, 1973.

    Article  PubMed  CAS  Google Scholar 

  2. Pradayrol L., Jornvall H., Mutt V., Ribet A. N-terminally extended somatostatin: the primary structure of somatostatin 28. FEBS Lett. 109: 55, 1980.

    Article  PubMed  CAS  Google Scholar 

  3. Patel Y.C. General aspects of the biology and function of somatostatin. In: Müller, E.E., Thorner, M.O., Weil, C. (Eds.), The role of somatostatin: basic and clinical aspects of neuroscience series. Springer-Verlag, Berlin, Vol. 4, 1992, pp. 1–16.

    Chapter  Google Scholar 

  4. Patel Y.C, J-L Liu, A.S. Galanopoulou, D.N. Papachristou. Production, action, and degradation of somatostatin. In: Jefferson L.S., Cherrington A.D. (Eds.), The Handbook of Physiology, The endocrine pancreas and regulation of metabolism, Oxford University Press, N.Y. 1997 (in press).

    Google Scholar 

  5. Patel Y.C, O’Neil W. Peptides derived from cleavage of prosomatostatin at carboxy and amino terminal segments: characterization of tissue and secreted forms in the rat. J. Biol. Chem. 263: 745, 1988.

    PubMed  CAS  Google Scholar 

  6. Reichlin S. Somatostatin. N. Engl. J. Med. 309: 1495, 1556, 1983.

    Article  PubMed  CAS  Google Scholar 

  7. Aguila M.C., Dees W.L., Haensly W.E., McCann S.M. Evidence that somatostatin is localized and synthesized in lymphoid organs. Proc. Natl. Acad. Sci. (USA) 88: 11485, 1991.

    Article  CAS  Google Scholar 

  8. De Lecea L., Criado J.R., Prospero-Garcia O., Gautvik K.M., Schweitzer P., Danielson P.E., Dunlop C.L.M., Siggins G.R., Henriksen S.J., Sutcliffe J.G. A cortical neuropeptide with neuronal depressant and sleep-modulating properties. Nature 381: 242, 1996.

    Article  PubMed  Google Scholar 

  9. Fukusumi S., Kitada C, Takekawa S., Kizawa H., Sakomoto J., Miyamoto M., Hinuma S., Kitano K., Fujino M. Identification and characterization of a novel human corticostatin like peptide. Biochem. Biophys. Res. Commun. 232: 157, 1997.

    Article  PubMed  CAS  Google Scholar 

  10. Kanatsuka A., Makino H., Matsushima Y., Kasanuki J., Osegawa M., Kumagai A. Effect of calcium on the secretion of somatostatin and insulin from pancreatic islets. Endocrinology 108: 22547, 1981.

    Article  Google Scholar 

  11. Montminy M.R., Low M.J., Tapia-Arancibia L., Reichlin S., Mandel G., Goodman R.H. Cyclic AMP regulates somatostatin mRNA accumulation in primary diencephalic cultures and in transfected fibroblast cells. J. Neurosci. 6: 1171, 1986.

    PubMed  CAS  Google Scholar 

  12. Patel Y.C, Papachristou D.N., Zingg H.H., Farkas E.M. Regulation of islet somatostatin secretion and gene expression: selective effects of adenosine 3′, 5′ monophosphate and phorbol esters in normal islets of Langerhans and in a somatostatin producing rat islet clonal cell line 1027B2. Endocrinology 128: 1754, 1991.

    Article  PubMed  CAS  Google Scholar 

  13. Aguila M.C. Growth hormone-releasing factor increases somatostatin release and mRNA levels in the rat periventricular nucleus via nitric oxide by activation of guanylate cyclase. Proc. Natl. Acad. Sci. (USA) 91: 782, 1994.

    Article  CAS  Google Scholar 

  14. Patel Y.C, Greenwood M.T., Panetta R., Demchyshyn L, Niznik H., Srikant C.B. Mini Review: The somatostatin receptor family. Life Sciences 57: 1249, 1995.

    Article  PubMed  CAS  Google Scholar 

  15. Reisine T., Bell G.I. Molecular biology of somatostatin receptors. Endocrinol. Rev. 16: 427, 1995.

    CAS  Google Scholar 

  16. Epelbaum J., Dournaud P., Fodor M., Viollet C. The neurobiology of somatostatin. Crit. Rev. Neurobiol. 8: 25, 1994.

    PubMed  CAS  Google Scholar 

  17. Patel Y.C, Greenwood M.T., Panetta R., Hukovic N., Grigorakis S., Robertson L-A, Srikant C.B. Molecular biology of somatostatin receptor subtypes. Metabolism 45: 31, 1996.

    Article  PubMed  CAS  Google Scholar 

  18. Da Cunha A., Rausch D.M., Eiden L.E. An early increase in somatostatin mRNA expression in the frontal cortex of Rhesus monkeys infected with simian immunodeficiency virus. Proc. Natl. Acad. Sci. (USA) 92: 1371, 1995.

    Article  Google Scholar 

  19. Hoyer D., Lubbert H., Bruns C. Molecular pharmacology of somatostatin receptors. Arch. Pharmacol. 850: 441, 1994.

    Google Scholar 

  20. Violett C, Prevost G., Maubert E., Faivre-Bauman A., Gardette R., Kordon C, Loudes C, Slama A., Epelbaum J. Molecular pharmacology of somatostatin receptors. Fundam. Clin. Pharmacol. 9: 107, 1995.

    Article  Google Scholar 

  21. Lamberts S.W.J., Van Der Lely A-J., de Herder W.W. Drug therapy: octreotide. N. Engl. J. Med. 334: 246, 1996.

    Article  PubMed  CAS  Google Scholar 

  22. Patel Y.C, Murthy K.K., Escher E., Banville D., Spiess J., Srikant C.B. Mechanism of action of somatostatin: an overview of receptor function and studies of the molecular characterization and purification of somatostatin receptor proteins. Metabolism 39(Suppl. 2): 63, 1990.

    Article  PubMed  CAS  Google Scholar 

  23. Schonbrunn A., Tashjian A.H. Jr. Characterization of functional receptors for somatostatin in rat pituitary cells in culture. J. Biol. Chem. 253: 6473, 1978.

    PubMed  CAS  Google Scholar 

  24. Srikant C.B., Patel Y.C. Somatostatin receptors: identification and characterization in rat brain membranes. Proc. Natl. Acad. Sci. (USA) 78: 3930, 1981.

    Article  CAS  Google Scholar 

  25. Srikant C.B., Patel Y.C Receptor binding of somatostatin-28 is tissue specific. Nature 294: 259, 1981.

    Article  PubMed  CAS  Google Scholar 

  26. Reubi J-C., Cortes R., Maurer R., Probst A., Palacios J.M. Distribution of somatostatin receptors in the human brain: an autoradiographic study. Neuroscience. 18: 329, 1986.

    Article  PubMed  CAS  Google Scholar 

  27. Thermos, K., Reisine T. Somatostatin receptor subtypes in the clonal anterior pituitary cell lines AtT-20 and GH3. Mol. Pharmacol. 33: 370, 1988.

    PubMed  CAS  Google Scholar 

  28. Srikant C.B., Murthy K.K., Escher E., Patel Y.C. Photoaffinity labelling of the somatostatin receptor: Identification of molecular subtypes. Endocrinology 130: 2937, 1992.

    PubMed  CAS  Google Scholar 

  29. Brown P.J., Lee A.B., Norman M.G., Presky D.H., Schonbrunn A. Identification of somatostatin receptors by covalent labeling with a novel photoreactive somatostatin analog. J. Biol. Chem. 265: 17995, 1990.

    PubMed  CAS  Google Scholar 

  30. He H.T., Johnson K., Thermos K., Reisine T. Purification of a putative brain somatostatin receptor. Proc. Natl. Acad. Sci. (USA) 86: 1480, 1989.

    Article  CAS  Google Scholar 

  31. Eppler CM., Zysk J.R., Corbett M., Shieh H-M. Purification of a pituitary receptor for somatostatin. The utility of biotinylated somatostatin analogs. J. Biol. Chem. 267: 15603, 1992.

    PubMed  CAS  Google Scholar 

  32. Maletti M., Andersson M., Marie J-C, Rosselin G., Mutt V. Solubilization and partial purification of somatostatin-28 preferring receptors from hamster pancreatic beta cells. J. Biol. Chem. 267: 15620, 1992.

    PubMed  CAS  Google Scholar 

  33. Sullivan S.J., Schonbrunn A. Distribution of somatostatin receptors in RINm5F insulinoma cells. Endocrinology 122: 1137, 1988.

    Article  PubMed  CAS  Google Scholar 

  34. Liebow C, Reilly C, Serrano M., Schally A.V. Somatostatin analogues inhibit growth of pancreatic cancer by stimulating tyrosine phosphatase. Proc. Natl. Acad. Sci. (USA) 86: 2003, 1989.

    Article  CAS  Google Scholar 

  35. Zeggari M., Esteve J-P., Rauly I., Cambillau C, Mazarguil H., Dufresne M., Pradayrol L, Chayvialle J-A., Vaaysse N., Susini C. Copurification of a protein tyrosine phosphatase with activated somatostatin receptors from rat pancreatic acinar membranes. Biochem. J. 303: 441, 1994.

    PubMed Central  PubMed  CAS  Google Scholar 

  36. Pagliacci M.C, Tognellinin R., Grignani F., Nicoletti F. Inhibition of human breast cancer cell (MCF-7) growth in vitro by the somatostatin analog SMS201-995: effects on cell cycle parameters and apoptotic cell death. Endocrinology 129: 2555, 1991.

    Article  PubMed  CAS  Google Scholar 

  37. Nilsson L., Folkesson R. Coexistence of somatostatin receptor subtypes in the human neuroblastoma cell line LA-N-2. FEBS Lett. 401: 838, 1997.

    Article  Google Scholar 

  38. Feindt J., Becker I., Blomer U., Hugo H.H., Mehdorn H.M., Kritsch B., Mentlein R. Expression of somatostatin receptor subtypes in cultured astrocytes and gliomas. J. Neurochem. 65: 1997, 1995.

    Article  PubMed  CAS  Google Scholar 

  39. Sreedharan S.P., Kodama K.T., Peterson K.E., Goetzl E.J. Distinct subsets of somatostatin receptors on cultured human lymphocytes. J. Biol. Chem. 264: 949, 1989.

    PubMed  CAS  Google Scholar 

  40. Yamada Y., Post S.R., Wang K., Tager H.S., Bell G.I., Seino S. Cloning and functional characterization of a family of human and mouse somatostatin receptors expressed in brain, gastrointestinal tract, and kidney. Proc. Natl. Acad. Sci. (USA) 89: 251, 1992.

    Article  CAS  Google Scholar 

  41. Kluxen F.W., Bruns CH., Lubbert H. Expression cloning of a rat brain somatostatin receptor cDNA. Proc. Natl. Acad. Sci. (USA) 39: 4618, 1992.

    Article  Google Scholar 

  42. Li X-J., Forte M., North R.A., Ross C.A., Snyder S.H. Cloning and expression of a rat somatostatin receptor enriched in brain. J. Biol. Chem. 267: 21307, 1992.

    PubMed  CAS  Google Scholar 

  43. Yasuda K., Rens-Domiano S., Breder C.D., Law S.F, Saper C.B., Reisine T., Bell G.I. Cloning of a novel somatostatin receptor, SSTR3, coupled to adenylyl cyclase. J. Biol. Chem. 267: 20422, 1992.

    PubMed  CAS  Google Scholar 

  44. Meyerhof W., Wulfsen I., Schonrock C, Fehr S., Richter D. Molecular cloning of a somatostatin-28 receptor and comparison of its expression pattern with that of a somatostatin 14 receptor in rat brain. Proc. Natl. Acad. Sci. (USA) 89: 10267, 1992.

    Article  CAS  Google Scholar 

  45. Yamada Y., Reisine T., Law S.F., Ihara Y., Kubota A., Kagimoto S., Seino M., Seino Y., Bell G.I., Seino S. Somatostatin receptors, an expanding gene family: cloning and functional characterization of human SSTR3, a protein coupled to adenylate cyclase. Mol. Endocrinol. 6: 2136, 1992.

    PubMed  CAS  Google Scholar 

  46. Bruno J.F., Xu Y., Song J., Berelowitz M. Molecular cloning and functional expression of a brain-specific somatostatin receptor. Proc. Natl. Acad. Sci. (USA) 89: 11151, 1992.

    Article  CAS  Google Scholar 

  47. Rohrer L, Raulf F., Bruns C, Buettner R., Hofstaedter F., Schule R. Cloning and characterization of a fourth human somatostatin receptor. Proc. Natl. Acad. Sci. (USA) 90: 4196, 1993.

    Article  CAS  Google Scholar 

  48. Demchyshyn L.L., Srikant C.B., Sunahara R.K., Kent G., Seeman P., Van Tol H.H.M., Panetta R., Patel Y.C., Niznik H.B. Cloning and expression of a human somatostatin-14 selective receptor variant (SSTR4) located on chromosome 20. Mol. Pharmacol. 43: 894, 1993.

    PubMed  CAS  Google Scholar 

  49. Corness J.D., Demchyshyn L.L, Seeman P., Van Tol H.H.M., Srikant C.B., Kent G., Patel Y.C, Niznik H.B. A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides. FEBS Lett. 321: 279, 1993.

    Article  PubMed  CAS  Google Scholar 

  50. O’Carroll A.M., Lolait S.J., König M., Mahan L.C. Molecular cloning and expression of a pituitary somatostatin receptor with preferential affinity for somatostatins. Mol. Pharmacol. 42: 939, 1992.

    PubMed  Google Scholar 

  51. Panetta R., Greenwood M.T., Warszynska A., Demchyshyn L.L., Day R., Niznik H.B., Srikant C.B., Patel Y.C. Molecular cloning, functional characterization, and chromosomal localization of a human somatostatin receptor (somatostatin receptor type 5) with preferential affinity for somatostatin-28. Mol. Pharmacol. 45: 417, 1994.

    PubMed  CAS  Google Scholar 

  52. Vanetti M., Kouba M., Wang X., Vogt G., Hollt V. Cloning and expression of a novel mouse somatostatin receptor (SSTR2B). FEBS Lett. 311: 290, 1992.

    Article  PubMed  CAS  Google Scholar 

  53. Patel Y.C, Greenwood M.T., Kent G., Panetta R., Srikant C.B. multiple gene transcripts of the somatostatin receptor SSTR2: tissue selective distribution and cAMP regulation. Biochem. Biophys. Res. Commun. 192: 28, 1993.

    Article  Google Scholar 

  54. Evans C.J., Keith D.E. Jr., Morrison H., Magendzo K., Edwards R.H. Cloning of a delta opioid receptor by functional expression. Science 258: 1952, 1992.

    Article  PubMed  CAS  Google Scholar 

  55. Wilson R., Ainscough R., Anderson K., Baaynes C., Berks M., Bonfield J., Burton J., Connell M., Copsey T., Cooper J. et al. Nature 368: 32, 1994.

    Article  PubMed  CAS  Google Scholar 

  56. Jung B.P., Nguyen T., Kolakowski L.F. Jr., Lynch K.R., Heng H.H.Q., George S.R., O’Dowd B.F. Discovery of a novel human G protein coupled receptor gene (GPR25) located on chromosome 1. Biochem. Biophys. Res. Commun. 230: 69, 1997.

    Article  PubMed  CAS  Google Scholar 

  57. Kolakowski F.L., Jung B.P., Nguyen T., Johnson M.P., Lynch K.R., Cheng R., Heng H.H.Q., George S.R., O’Dowd B.F. Characterization of a human gene related to genes encoding somatostatin receptors. FEBS Lett. 303: 253, 1996.

    Article  Google Scholar 

  58. Veber D., Saperstein R., Nutt R., Friedinger R., Brady S., Curley P., Perlow D., Palveda W., Colton C, Zacchei A., Tocco D., Hoff D., Vandlen R., Gerich J., Hall L., Mandarino L., Cordes E., Anderson P., Hirschmann R. A superactive cyclic hexapeptide analog of somatostatin. Life Sci. 34: 1371, 1984.

    Article  PubMed  CAS  Google Scholar 

  59. Bauer W., Briner U., Doepfner W., Halber R., Huguenin R., Marbach P., Petcher T.J., Pless J. SMS 201–995: a very potent and selective octapeptide analogue of somatostatin with prolonged action. Life Sci. 37: 1133, 1982.

    Article  Google Scholar 

  60. Taylor J.E., Bogden A.E., Moreau J.-P., Coy D.H. In vitro and in vivo inhibition of human small cell lung carcinoma (NCI-H69) growth by a somatostatin analogue. Biochem. Biophys. Res. Commun. 153: 81, 1988.

    Article  PubMed  CAS  Google Scholar 

  61. Raynor K., Murphy W.A., Coy D.H., Taylor J.E., Moreau J.-P., Yasuda K., Bell G.I., Reisine T. Cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linea peptides. Mol. Pharmacol. 43: 838, 1993

    PubMed  CAS  Google Scholar 

  62. Patel Y.C, Srikant C.B. Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstrl-5). Endocrinology 735: 2814, 1994.

    Google Scholar 

  63. Bruns C, Raulf F., Hoyer D., Schloos J., Lubbert H., Weckbecker G. Binding properties of somatostatin receptor subtypes. Metabolism 45(Suppl. 1): 17, 1996.

    Article  PubMed  CAS  Google Scholar 

  64. Shimon I., Taylor J.E., Dong J.Z., Bitonte R.A., Kim S., Morgan B., Coy D.H., Culler M.D, Melmed S. Somatostatin receptor subtype specificity in human fetal pituitary culture. J. Clin. Invest. 99: 789, 1997.

    Article  PubMed Central  PubMed  CAS  Google Scholar 

  65. Liapakis G., Haeger C, Rivier J., Reisine T. Development of a selective agonist at the somatostatin receptor subtype SSTR1. J. PET 276: 1089, 1996.

    CAS  Google Scholar 

  66. Bass R.T., Buckwalter B.L., Patel B.P., Pausch M.H., Price L.A., Strnad J., Hadcock J.R. Identification and characterization of novel somatostatin antagonists. Mol. Pharmacol. 50: 709, 1996.

    PubMed  CAS  Google Scholar 

  67. Baldwin J.M. Structure and function of receptors coupled to G proteins. Curr. Opin. Cell Biol. 6: 180, 1994.

    Article  PubMed  CAS  Google Scholar 

  68. Strader C.D., Fong T.M., Graziano M.P., Tota M.R. The family of G protein coupled receptors. FASEB J. 9: 745, 1995.

    PubMed  CAS  Google Scholar 

  69. Schwartz T.W., Rosenkilde M.M. Is there a lock for all agonist keys in 7 TM receptors. TIPS 77: 213, 1996.

    Google Scholar 

  70. Gether U., Johansen T.E., Snider R.M., Lowe J.A., Edmons-Alt X., Yokota Y., Nakamishi S., Schwartzz T.W. Binding epitopes for peptide and nonpeptide ligands on the NK1 (substance P) receptor. Regul. Pept. 46: 49, 1993.

    Article  PubMed  CAS  Google Scholar 

  71. Hjorth S.A., Schambye H.T., Greenlee W.J., Schwartz T.W. Identification of peptide binding residues in the extracellular domains of the AT1 receptor. J. Biol. Chem. 269: 30953, 1994.

    PubMed  CAS  Google Scholar 

  72. Flanagan CA., Becker I.I., Davidson J.S., Wakefield I.K., Zhou W., Sealfon SC., Miller R.P. Glutamate 301 of the mouse gonadotrophin releasing hormone receptor confers specificity for arginine 8 of mammalian gonadotrophin releasing hormone. J. Biol. Chem. 269: 22636, 1994.

    PubMed  CAS  Google Scholar 

  73. Kaupman K., Bruns C, Raulf F., Weber H.P., Mattes H., Lubbert H. Two amino acids, located in transmembrane domains VI and VII, determine the selectivity of the peptide agonist SMS201-995 for the SSTR2 somatostatin receptor. EMBO J. 14: 727, 1995.

    Google Scholar 

  74. Nehring R.B., Meyerhof W., Richter D. Aspartic acid residue 124 in the third transmembrane domain of the somatostatin receptor subtype 3 is essential for somatostatin 14 binding. DNA and Cell Biol. 14: 939, 1995.

    Article  CAS  Google Scholar 

  75. Strnad J., Hadcock J.R. Identification of a critical aspartate residue in transmembrane domain three necessary for the binding of somatostatin to the somatostatin receptor SSTR2. Biochem. Biophys. Res. Commun. 276: 913, 1995.

    Article  Google Scholar 

  76. Fitz-Patrick V.D., Vandlen R.L 6 agonist selectivity determinants in somatostatin receptor subtypes I and II. J. Biol. Chem. 269: 24621, 1994.

    CAS  Google Scholar 

  77. Greenwood M.T., Hukovic N., Kumar U., Panetta R., Hjorth S.A., Srikant C.B., Patel Y.C Ligand binding pocket of the human somatostatin receptor 5 (hsstr5): mutational analysis of the extracellular domains. Mol. Pharmacol. 1997 (in press).

  78. Luthin D.R., Eppler CM., Linden J. Identification and quantification of Gi-type GTPbinding proteins that copurify with a pituitary somatostatin receptor. J. Biol. Chem. 268: 5990, 1993.

    PubMed  CAS  Google Scholar 

  79. Law S.F., Yasuda K., Bell G.I., Reisine T. Gi alpha 3 and G (o) alpha selectively associate with cloned somatostatin in receptor subtypes SSTR2. J. Biol. Chem. 268: 10721, 1993.

    PubMed  CAS  Google Scholar 

  80. Tallent M., and Reisine T. Gi alpha 1 selectively couples somatostatin receptors to adenylyl cyclase in pituitary-derived AtT-20 cells. Mol. Pharmacol. 41: 452, 1992.

    PubMed  CAS  Google Scholar 

  81. Liu Y.F., Jacobs K.H., Rosewick M.M., Albert P.R. G protein specificity in receptor effector coupling: analysis of the roles of Go and Gi in GH4CI pituitary cells. J. Biol. Chem. 269: 13880, 1994.

    PubMed  CAS  Google Scholar 

  82. Senogles S.E. The D2 dopamine receptor isoforms signal through distinct Gi alpha proteins to inhibit adenylyl cyclase. A study with site-directed mutant Gi alpha proteins. J. Biol. Chem. 269: 23120, 1994.

    PubMed  CAS  Google Scholar 

  83. Wang H.L., Bogen C, Reisine T., Dichter M. Somatostatin-14 and somatostatin-28 induce opposite effects on potassium currents in rat neocortical neurons. Proc. Natl. Acad. Sei. (USA) 86: 9616, 1989.

    Article  CAS  Google Scholar 

  84. Sims S.M., Lussier BT., Kraicer J. Somatostatin activates an inwardly rectifying K+ conductance in freshly dispersed rat somatotrophs. J. Physiol. 441: 615, 1991.

    PubMed Central  PubMed  CAS  Google Scholar 

  85. De Weille J.R., Schmid-Antomarchi H., Fosset M., Lazdunski M. Regulation of ATPsensitive K+ channels in insulinoma cells: activation by somatostatin and protein kinase C and the role of cAMP. Proc. Natl. Acad. Sci. (USA) 86: 2971, 1989.

    Article  Google Scholar 

  86. White R.E., Schonbrunn A., Armstrong D.L. Somatostatin stimulates Ca2+ -activated K+ channels through protein dephosphorylation. Nature 351: 570, 1991.

    Article  PubMed  CAS  Google Scholar 

  87. Yatani A., Codina J., Sekura R.D., Birnbaumer L., Brown A.M. Reconstitution of somatostatin and muscarinic receptor mediated stimulation of K+ channels by isolated GK protein in clonal rat anterior pituitary cell membranes. Mol. Endocrinol. 1: 283, 1987.

    Article  PubMed  CAS  Google Scholar 

  88. Koch B.D., Schonbrunn A. Characterization of the cyclic AMP-independent actions of somatostatin in GH cells. J. Biol. Chem. 263: 226, 1988.

    PubMed  CAS  Google Scholar 

  89. Ikeda S.R., Schofield G.G. Somatostatin blocks a calcium current in rat sympathetic ganglion neurons. J. Physiol. 469: 221, 1989.

    Google Scholar 

  90. Kleuss C, Heschefeler J., Ewel C, Rosenthal W., Schultz G., Wittig B. Assignment of G protein subtypes to specific receptors inducing inhibition of calcium currents. Nature 353: 43, 1991.

    Article  PubMed  CAS  Google Scholar 

  91. Meriney S.D., Gray D.B., Pilar G.R. Somatostatin-induced inhibition of neuronal Ca2+ current modulated by cGMP-dependent protein kinase. Nature 369: 336, 1994.

    Article  PubMed  CAS  Google Scholar 

  92. Renstrom E., Ding W-G., Bokvist K., Rorsman P. Neurotransmitter-induced inhibition of exocytosis in insulin-secreting β cells by activation of calcineurin. Neuron 17: 513, 1996.

    Article  PubMed  CAS  Google Scholar 

  93. Barber, D.L., M.E. McGuire, M.B. Ganz. Beta-adrenergic and somatostatin receptors regulate Na-H exchange independent of cAMP. J. Biol. Chem. 264: 21038, 1989.

    PubMed  CAS  Google Scholar 

  94. Schweitzer R., Madamba S., Siggins G.R. Arachidonic acid metabolites as mediators of somatostatin-induced increase of neuronal M-current. Nature 346: 464, 1990.

    Article  PubMed  CAS  Google Scholar 

  95. Schonbrunn A. Somatostatin action in pituitary cells involves two independent transduction mechanisms. Metabolism 39(Suppl. 2): 96, 1990.

    Article  PubMed  CAS  Google Scholar 

  96. Brown P., Schonbrunn A. Affinity purification of a somatostatin receptor-G-protein complex demonstrates specificity in receptor-G-protein coupling. J. Biol. Chem. 268: 6668, 1993.

    PubMed  CAS  Google Scholar 

  97. Patel Y.C, Greenwood M.T., Warszynska A., Panetta R., Srikant C.B. All five cloned human somatostatin receptors (hSSTR1-5) are functionally coupled to adenylyl cyclase. Biochem. Biophys. Res. Commun. 798: 605, 1994.

    Article  Google Scholar 

  98. Florio T., Rim C, Hershberger R.E., Loda M., Stork P.J. The somatostatin receptor SSTR1 is coupled to phosphotyrosine phosphatase activity in CHO-K1 cells Mol. Endocrinol. 8: 1289, 1994.

    CAS  Google Scholar 

  99. Buscail L, Esteve J.-P., Saint-Laurent N., Bertrand V., Reisine T., O’Carroll A.-M., Bell G.I., Schally A.V., Vaysse N., Susini C. Inhibition of cell proliferation by the somatostatin analogue RC-160 is mediated by somatostatin receptor subtypes SSTR2 and SSTR5 through different mechanisms. Proc. Natl. Acad. Sci. (USA) 92: 1580, 1995.

    Article  CAS  Google Scholar 

  100. Reardon D.B., Wood S.L, Brautigan D.L., Bell G.I., Dent P., Sturgill T.W. Activation of a protein tyrosine phosphate and inactivation of Raf-1 by somatostatin. Biochem. J. 314: 401, 1996.

    PubMed Central  PubMed  CAS  Google Scholar 

  101. Florio T., Scarziello A., Fattore M., Dalto V., Salzano S., Rossi G., Berlingieri M.T., Fusco A., Schettini G. Somatostatin inhibits PC C13 thyroid cell proliferation through the modulation of phosphotyrosine phosphatase activity-impairment of the somatostatinergic effects by stable expression of EIA viral oncogene. J. Biol. Chem. 271: 6129, 1996.

    Article  PubMed  CAS  Google Scholar 

  102. Sharma K., Patel Y.C, Srikant C.B. Subtype selective human somatostatin receptor (hSSTR) mediated cytostatin and cytotoxic actions involve different signalling mechanisms. Program Annual Meeting US Endocrine Society, Minneapolis, June 1997 (abstract).

  103. Hou C, Gilbert R.L., Barber D.L. Subtype-specific signalling mechanisms of somatostatin receptors SSTR1 and SSTR2. J. Biol. Chem. 269: 10357, 1994.

    PubMed  CAS  Google Scholar 

  104. Fujii Y., Gonoi T., Yamada Y., Chihara K., Inagaki N., Seino S. Somatostatin receptor subtype SSTR2 mediates the inhibition of high voltage activated calcium channels by somatostatin and its analogue SMS201-995. FEBS Lett. 355: 117, 1994.

    Article  PubMed  CAS  Google Scholar 

  105. Viana F., Hille B. Modulation of high voltage-activated calcium channels by somatostatin in acutely isolated rat amygdaloid neurons. J. Neurosci. 76: 6000, 1996.

    Google Scholar 

  106. Bito H., Mori M., Sakanaka C, Takano T., Honda Z., Gotoh Y., Nishida E., Shimizu T. Functional coupling of SSTR4, a major hippocampal somatostatin receptor, to adenylate cyclase inhibition, arachidonate release and activation of the mitogen-activated protein kinase cascade. J.Biol. Chem. 269: 12722, 1994.

    PubMed  CAS  Google Scholar 

  107. Akbar M., Okajima F., Tomura H., Majid M.A., Yamada Y., Seino S., Kondo Y. Phospholipase C activation and Ca2+ mobilization by cloned human somatostatin receptor subtypes 1–5 in transfected COS-7 cells. FEBS Lett. 348: 192, 1994.

    Article  PubMed  CAS  Google Scholar 

  108. Luini A., de Matteis M.A. Evidence that receptor-linked G protein inhibits exocytosis by a post-second messenger mechanism in AtT-20 cells. J. Neurochem. 54: 30, 1990.

    Article  PubMed  CAS  Google Scholar 

  109. Wollheim C.B., Winiger B.P., Ullrich S., Wuarin F., Schlegel W. Somatostatin inhibition of hormone release: effects on cytosolic Cal and interference with distal secretory events. Metabolism (Suppl. 11) 39: 101, 1990.

    Article  PubMed  CAS  Google Scholar 

  110. Pan M.G., Florio T., Stork P.J.S. G protein activation of a hormone-stimulated phosphatase in human tumor cells. Science 256: 1215, 1992.

    Article  PubMed  CAS  Google Scholar 

  111. Srikant C.B., Shen S.H. Octapeptide somatostatin analog SMS 201–995 induces translocation of intracellular PTPIC to membranes in MCF-7 human breast cancer adenocarcinoma cells. Endocrinology 137: 3461, 1996.

    PubMed  CAS  Google Scholar 

  112. Srikant C.B. Cell cycle dependent induction of apoptosis by somatostatin analog SMS201995 in AtT-20 mouse pituitary tumor cells. Biochem. Biophys. Res. Commun. 209: 400, 1995.

    Article  PubMed  CAS  Google Scholar 

  113. Sharma K., Patel Y.C, Srikant C.B. Subtype selective induction of p53-dependent apoptosis but not bell cycle arrest by human somatostatin receptor 3. Mol. Endocrinol. 10: 1688, 1996.

    PubMed  CAS  Google Scholar 

  114. Bruno J.F., Xu Y., Song J., Berelowitz M. Tissue distribution of somatostatin receptor subtype messenger ribonucleic acid in the rat. Endocrinology 133: 2561, 1993.

    PubMed  CAS  Google Scholar 

  115. Breder C.D., Yamada Y.Y., Yasuda K., Seino S., Saper C.B., Bell G.I. Differential expression of somatostatin receptor subtypes in brain. J. Neurosci. 12: 3920, 1992.

    PubMed  CAS  Google Scholar 

  116. Kong H., DePaoli A.M., Breder C.D., Yasuda K., Bell G.I., Reisine T. Differential expression of messenger RNAs for somatostatin receptor subtypes SSTR1, SSTR2, and SSTR3 in adult rat brain: analysis by RNA blotting and in situ hybridization histochemistry. Neuroscience 59: 175, 1994.

    Article  PubMed  CAS  Google Scholar 

  117. Thoss V.S., Perez J., Duc D., Hoyer D. Embryonic and postnatal mRNA distribution of five somatostatin receptor subtypes in the rat brain. Neuropharmacology 34: 1673, 1995.

    Article  PubMed  CAS  Google Scholar 

  118. Thoss V.S., Perez J., Probat A., Hoyer D. Expression of five somatostatin receptor mRNAs in the human brain and pituitary. Arch. Pharmacol. 354: 411–419, 1996.

    Article  CAS  Google Scholar 

  119. Dournaud P., Gu Y.Z., Schonbrunn A., Mazella J., Tannenbaum G.S., Beaudet A. Localization of the somatostatin receptor SST2A in rat brain using a specific antipeptide antibody. J. Neurosci. 76: 4468, 1996.

    Google Scholar 

  120. Patel Y.C, Panetta R., Escher E., Greenwood M., Srikant C.B. Expression of multiple somatostatin receptor genes in AtT-20 cells: evidence for a novel somatostatin-28 selective receptor subtype. J. Biol. Chem. 269: 1506, 1994.

    PubMed  CAS  Google Scholar 

  121. Day R., Dong W., Panetta R., Kraicer J., Greenwood M.T., Patel Y.C. Expression of mRNA for somatostatin receptor (sstr) types 2 and 5 in individual rat pituitary cells. A double labeling in situ hybridization analysis. Endocrinology 136: 5232, 1995.

    PubMed  CAS  Google Scholar 

  122. O’Carroll A., Krempels K. Widespread distribution of somatostatin receptor messenger ribonucleic acids in rat pituitary. Endocrinology 136: 5224, 1995.

    PubMed  Google Scholar 

  123. Panetta R., Patel Y.C. Expression of mRNA for all 5 human somatostatin receptor (hSSTR1-5) in pituitary tumors. Life Sci. 56: 333, 1994.

    Article  CAS  Google Scholar 

  124. Grigorakis S.I., Panetta R., Patel Y.C Expression of mRNA for somatostatin receptor (sstr) subtypes 1–5 in islets and differential down-regulation of sstr2 mRNA by SST agonists. Program Annual Meeting American Diabetes Association, June 10–13, 1995, Atlanta, Georgia, Abstr. no. 485, p. 132A.

  125. Amherdt M., Patel Y.C, Orci L. Selective binding of somatostatin-14 and somatostatin −28 to islet cells revealed by quantitative electron microscopic autoradiography. J. Clin. Invest. 80: 1455, 1987.

    Article  PubMed Central  PubMed  CAS  Google Scholar 

  126. Le Romancer M., Cherifi Y., Levasseur S., Laigneau J.P., Peranzi G., Jois P., Lewin M.J., Reyl-Desmars F. Messenger RNA expression of somatostatin receptor subtypes in human and rat gastric mucosae. Life Sci. 53: 1091, 1996.

    Article  Google Scholar 

  127. Lamberts S.W.J., Krenning E.P., and Reubi J.-C. The role of somatostatin and its analogs in the diagnosis and treatment of tumors. Endocr. Rev. 12: 450, 1991.

    Article  PubMed  CAS  Google Scholar 

  128. Greenman Y., Melmed S. Heterogeneous expression of two somatostatin receptor subtypes in pituitary tumors. J. Clin. Endocrinol. Metab. 78: 398, 1994.

    PubMed  CAS  Google Scholar 

  129. Greenman Y., Melmed S. Expression of three somatostatin receptor subtypes in pituitary adenomas: evidence for preferential SSTR5 expression in the mammosomatotroph lineage. J. Clin. Endocrinol. Metab. 79: 724, 1994.

    PubMed  CAS  Google Scholar 

  130. Miller G., Alexander M.J.M., Bikkel H.A. Somatostatin receptor subtype gene expression in pituitary adenomas. J. Clin. Endocrinol. Metab. 80: 1386, 1995.

    PubMed  CAS  Google Scholar 

  131. Vikic-Topic S., Reisch K.P., Kvols L.K., Vuk-Pavlovic S. Expression of somatostatin receptor subtypes in breast carcinoma, carcinoid tumor, and renal cell carcinoma. J. Clin. Endocrinol. Metab. 80: 2974, 1995.

    PubMed  CAS  Google Scholar 

  132. Kubota A., Yamada Y., Kagimoto S., Shimatsu A., Imamura M., Tsuda K., Imura H., Seino S., Seino Y. Identification of somatostatin receptor subtypes and an implication for the efficacy of somatostatin analogue SMS201-995 in treatment of human endocrine tumors. J. Clin. Invest. 93: 1321, 1994.

    Article  PubMed Central  PubMed  CAS  Google Scholar 

  133. Epelbaum J., Bertherat J., Prevost G., Kordon C, Meyerhof W., Wulfsen I., Richter D., Plouin P-F. Molecular and pharmacological characterization of somatostatin receptor subtypes in adrenal, extra-adrenal and malignant phaeochromocytomas. J. Clin. Endocrinol. Metab. 80: 1837, 1995.

    PubMed  CAS  Google Scholar 

  134. Dutour A., Panetta R., Kumar U., Ouafik L, Furin F., Patel Y.C Expression of somatostatin receptor subtypes (1–5) in human brain tumors. J. Clin. Endocrinol. Metab. 1997 (submitted).

  135. Krejs G.J., Orci L., Conlon J.M., Ravazzola M., Davis G.R., Raskin P., Collins S.M., McCarthy D.M., Baetens D., Rubinstein A., Aldor T.A.M., Unger R.H. Somatostatinoma syndrome. N. Engl. J. Med. 301: 285, 1979.

    Article  PubMed  CAS  Google Scholar 

  136. Dohlman H.G., Thorner J., Caron M.G., Lelkowitz R.J. Model systems for the study of seven transmembrane segment receptors. J. Biol. Chem. 268: 337, 1991.

    Google Scholar 

  137. Reisine T.D., Axelrod J. Prolonged somatostatin treatment desensitizes somatostatin’s inhibition of receptor-mediated release of adrenocorticotropin hormone and sensitizes adenylate cyclase. Endocrinology 113: 811, 1983.

    Article  PubMed  CAS  Google Scholar 

  138. Morel G., Leroux P., Pelletier G. Ultrastructural autoradiographic localization of so-matostatin-28 in the rat pituitary gland. Endocrinology 116: 1615, 1985.

    Article  PubMed  CAS  Google Scholar 

  139. Amherdt M., Patel Y.C, Orci L. Binding and internalization of somatostatin, insulin, and glucagon by cultured rat islet cells. J. Clin. Invest. 84: 412, 1989.

    Article  PubMed Central  PubMed  CAS  Google Scholar 

  140. Hofland L.J., Van Koetsveld P.M., Waaijers M., Zzuyderwijkk J., Breeman W.A.P., Lamberts S.W.J. Internalization of the radioiodinated somatostatin analog [125l-Tyr3 ] octreotide by mouse and human pituitary tumor cells: increase by unlabelled octreotide. Endocrinology 136: 3698, 1995.

    PubMed  CAS  Google Scholar 

  141. Presky D.H., Schonbrunn A. Somatostatin pretreatment increases the number of somatostatin receptors in GH4C1 pituitary cells and does not reduce cellular responsiveness to somatostatin. J. Biol. Chem. 263: 714, 1988

    PubMed  CAS  Google Scholar 

  142. Hukovic N., Panetta R., Kumar U., Patel Y.C. Agonist-dependent regulation of cloned human somatostatin receptor types 1–5 (hSSTR1-5): subtype selective internalization or upregulation. Endocrinology 137: 4046, 1996.

    PubMed  CAS  Google Scholar 

  143. Nouel D., Gaudriault G., Houle M., Reisine T., Vincent J-P., Mazella J., Beaudet A. Differential internalization of somatostatin in COS-7 cells transfected with SST1 and SST2 receptor subtypes: a confocal microscopic study using novel fluorescent somatostatin derivatives. Endocrinology 138: 296, 1997.

    PubMed  CAS  Google Scholar 

  144. Roth A., Kreienkamp H.J., Nehring R.B., Roosterman D., Meyerhof W., Richter D. Endocytosis of the rat somatostatin receptors — subtype discrimination, ligand specificity and delineation of carboxyterminal positive and negative sequence motifs. DNA and Cell Biology 16: 111, 1997.

    Article  PubMed  CAS  Google Scholar 

  145. Vidal C, Rauly I., Zeggari M., Delesque N., Esteve J.-P., Saint-Lauient N., Vaysse N., Susini C. Up-regulation of somatostatin receptors by epidermal growth factor and gastrin in pancreatic cancer cells. Mol. Pharmacol. 46: 97, 1994.

    PubMed  CAS  Google Scholar 

  146. Bruno J.F., Xu Y., Berelowitz M. Somatostatin regulates somatostatin receptor subtype mRNA expression in GH3 cells. Biochem. Biophys. Res. Commun. 202: 1738, 1994.

    Article  PubMed  CAS  Google Scholar 

  147. Xu Y., Berelowitz M., Brunod J.F. Dexamethasone regulates somatostatin receptor subtype messenger ribonucleic acid expression in rat pituitary GH4C1 cells. Endocrinology 136: 5070, 1995.

    PubMed  CAS  Google Scholar 

  148. Kimura N., Hayafiji C, Konagaye H., Takahashi K. 17β estradiol induces somatostatin (SRIF) inhibition of prolactin release and regulates SRIF receptors in rat anterior pituitary cells. Endocrinology 119: 1028, 1986.

    Article  PubMed  CAS  Google Scholar 

  149. Xu Y.X., Song J., Berelowitz M., Bruno J.F. Estrogen regulates somatostatin receptor subtype 2 messenger ribonucleic acid expression in human breast cancer cells. Endocrinology 5634, 1996.

  150. Visser-Wisselaar H.A., Van Uffelen C.J.C., Van Koetsveld P.M., Lichtenauer Kaligis E.G.R., Waaijers A.M., Uitterlinden P., Movy D.M., Lamberts S.W.J., Hofland L.J. 17β estradiol dependent regulation of somatostatin receptor subtype expression in the 7315 b prolactin secreting rat pituitary tumor in vitro and in vivo. Endocrinology 138: 1180, 1997.

    PubMed  CAS  Google Scholar 

  151. James R.A., Sarapura V.D., Bruns C, Raulf F., Dowding J.M., Gordon D.F., Wood W.M., Ridgway EC. Thyroid hormone induced expression of specific somatostatin receptor subtypes correlates with involution of the TtT-97 murine thyrotrope tumor. Endocrinology 138: 719, 1997.

    PubMed  CAS  Google Scholar 

  152. Bruno J.F., Xu Y., Song J., Berelowitz M. Pituitary and hypothalamic somatostatin receptor subtype messenger ribonucleic acid expression in the food-deprived and diabetic rat. Endocrinology 135: 1787, 1994.

    PubMed  CAS  Google Scholar 

  153. Hauser F., Meyerhof W., Wulfsen I., Schonrock C., Richter D. Sequence analysis of the promoter region of the rat somatostatin receptor subtype 1 gene. FEBS Lett. 345: 225, 1994.

    Article  PubMed  CAS  Google Scholar 

  154. Greenwood M.T., Robertson L.-A., Patel Y.C. Cloning of the gene encoding the human somatostatin receptor 2: sequence analysis of the 5′ flanking promoter region. Gene 159: 291, 1995.

    Article  PubMed  CAS  Google Scholar 

  155. Pscherer A., Dorflinger U., Kirfel J., Gawlas K., Ruschoff J., Buettner R., Schule R. The helix-loop-helix transcription factor SEF2 regulates the activity of a novel initiator element in the promoter of the human somatostatin receptor II gene. EMBO J. 15: 6680, 1996.

    PubMed Central  PubMed  CAS  Google Scholar 

  156. Xu Y., Bruno J.F., Berelowitz M. Characterization of the proximal region of the rat somatostatin receptor gene, SSTR4. Biochem. Biophys. Res. Commun. 206: 935, 1995.

    Article  PubMed  CAS  Google Scholar 

  157. Greenwood M.T., Panetta R., Robertson L.A., Liu J-L, Patel Y.C. Sequence analysis of the 5′-flanking promoter region of the human somatostatin receptor 5. Biochem. Biophys. Res. Commun. 205: 1883, 1994.

    Article  PubMed  CAS  Google Scholar 

  158. Sanford R., Sgotto B., Burn T., Brenner S. The tuberin (TSC2) autosomal dominant polycystic kidney disease (PKD1) and somatostatin type V receptor (SSTR5) genes form a synteny group in the fugu genome. Genomics 38: 84, 1996.

    Article  Google Scholar 

  159. Brassier J., Henske E.P. Loss of the polycystic kidney (PKD 1) region of chromosome 1 6pl 3 in renal cyst cells support a loss of function model for cyst pathogenesis. J. Clin. Invest. 99: 194, 1997.

    Article  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Fraser Laboratories, McGill University, Departments of Medicine and Neurology and Neurosurgery, Royal Victoria Hospital and the Montreal Neurological Institute, Montreal, Quebec, H3A 1A1, Canada

    Y. C. Patel

Authors
  1. Y. C. Patel
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Patel, Y.C. Molecular pharmacology of somatostatin receptor subtypes. J Endocrinol Invest 20, 348–367 (1997). https://doi.org/10.1007/BF03350317

Download citation

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF03350317

Key-words

Search

Navigation