Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
References
Aguila, M.C., Dees, W.L., Haensly, W.E. & McCann, S.M. (1991). Evidence that somatostatin is localized and synthesized in lymphoid organs. Proc.Natl.Acad.Sci.U.S.A. 88, 11485–11489.
Ankersen, M., Crider, M., Liu, S., Ho, B., Andersen, H.S. & Stidsen, C. (1998). Discovery of a Novel Non-Peptide Somatostatin Agonist with SST4 Selectivity. J.Am.Chem.Soc. 120, 1368–1373.
Bass, R.T., Buckwalter, B.L., Patel, B.P., Pausch, M.H., Price, L.A., Strnad, J. & Hadcock, J.R. (1996). Identification and characterization of novel somatostatin antagonists. Mol.Pharmacol. 50,709–715.
Bauer, W., Briner, U., Doepfner, W., Haller, R., Huguenin, R., Marbach, P., Petcher, T.J. & Pless, J. (1982). SMS 201-995: a very potent and selective octapeptide analog of somatostatin with prolonged action. Life Sci. 31, 1133–1140.
Baumbach, W.R., Carrick, T.A., Pausch, M.H., Bingham, B., Carmignac, D., Robinson, I.C.A.F., Houghten, R., Eppler, C.M., Price, L.A. & Zysk, J.R. (1998). A linear hexapeptide somatostatin antagonist blocks somatostatin activity in vitro and influences growth hormone release in rats. Mol.Pharmacol. 54, 864–873.
Baumeister, H., Kreuzer, O.J., Roosterman, D., Schafer, J. & Meyerhof, W. (1998). Cloning, expression, pharmacology and tissue distribution of the mouse somatostatin receptor subtype 5. J.Neuroendocrinol. 10, 283–290.
Bell, G.I. & Reisine, T. (1993). Molecular biology of somatostatin receptors. Trends Neurosci. 16, 34–38.
Brazeau, P., Vale, W., Burgus, R., Ling, N., Butcher, M., Rivier, J. & Guillemin, R. (1973). Hypothalamic polypeptide that inhibits the secretion of immunoreactive pituitary growth hormone. Science 179,77–79.
Bruno, J.F., Xu, Y., Song, J. & Berelowitz, M. (1992). Molecular cloning and functional expression of a brain-specific somatostatin receptor. Proc.Natl.Acad.Sci.U.S.A. 89, 11151–11155.
Brans, C., Lewis, L., Briner, U., Meno-Tetang, G. & Weckbecker, G. SOM230: a novel somatostatin peptidomimetic with a broad somatotropin release inhibiting factor (SST) receptor binding and a unique antisecretory profile. Eur. J. Endocrinol. 146, 707–716 (2002).
Bruns, C., Raulf, F., Hoyer, D., Schloos, J., Luebbert, H. & Weckbecker, G. (1996). Binding properties of somatostatin receptor subtypes. Metab., Clin.Exp. 44, 17–20.
Bruns, C., Shi, V., Hoyer, D., Schuurman, H. & Weckbecker, G. (2000). Somatostatin receptors and the potential use of Sandostatin to interfere with vascular remodelling. Eur.J.Endocrinol. 143, S3–S7.
Buscail, L., Delesque, N., Esteve, J.P., Saint-Laurent, N., Prats, H., Clerc, P., Robberecht, P., Bell, G.I. & Liebow, C. (1994). Stimulation of tyrosine phosphatase and inhibition of cell proliferation by somatostatin analogs: mediation by human somatostatin receptor subtypes SSTR1 andSSTR2. Proc.Natl.Acad.Sci.U.S.A. 91, 2315–2319.
Buscail, L., Saint-Laurent, N., Chastre, E., Vaillant, J.C., Gespach, C., Capella, G., Kalthoff, H., Lluix, F., Vaysse, N. & Susini, C. (1996). Loss of sst2 somatostatin receptor gene expression in human pancreatic and colorectal cancer. Cancer Res. 56, 1823–1827.
Caron, P., Buscail, L., Beckers, A., Esteve, J.P., Igout, A., Hennen, G. & Susini, C. (1997). Expression of somatostatin receptor SST4 in human placenta and absence of octreotide effect on human placental growth hormone concentration during pregnancy. J.Clin.Endocrinol.Metab. 82 3771–3776.
Carruthers, A.M., Warner, A.J., Michel, A.D., Feniuk, W. & Humphrey, P.P.A. (1999). Activation of adenylate cyclase by human recombinant sst5 receptors expressed in CHO-K1 cells and involvement of G.alpha.s proteins. Br.J.Pharmacol. 126, 1221–1229.
Chisholm, C. & Greenberg, G.R. (2000). Somatostatin receptor subtype-5 mediates inhibition of peptide YY secretion from rat intestinal cultures. Am.J.Physiol. 279, G983–G989.
Chowers, Y., Cahalon, L., ahav, M., Schor, H., Tal, R., Bar-Meir, S. & Levite, M. (2000). Somatostatin through its specific receptor inhibits spontaneous and TNF-.alpha.-and bacteria-induced IL-8 and IL-l.beta. secretion from intestinal epithelial cells. J.Immunol. 165, 2955–2961.
Christopoulos, G., Perry, K.J., Morfis, M., Tilakaratne, N., Gao, Y., Fraser, N.J., Main, M.J., Foord, S.M. & Sexton, P.M. (1999). Multiple amylin receptors arise from receptor activity-modifying protein interaction with the calcitonin receptor gene product. Mol.Pharmacol. 56, 235–242.
Corness, J.D., Demchyshyn, L.L., Seeman, P., Van Tol, H.H.M., Srikant, C.B., Kent, G., Patel, Y.C. & Niznik, H.B. (1993). A human somatostatin receptor (SSTR3), located on chromosome 22, displays preferential affinity for somatostatin-14 like peptides. FEBS Lett. 321,279–284.
Coy, D.H. & Taylor, J.E. (1996). Receptor-specific somatostatin analogs: correlations with biological activity. Metab. Clin.Exp. 44, 21–23.
Coy, D.H. & Taylor, J.E. (1999). Development of somatostatin agonists with high affinity and specificity for the human and rat type 5 receptor subtype. Pept.Proc.Am.Pept.Symp., 15, 559–560.
Curtis, S.B., Chen, J.C., Winkelaar, G., Turnbull, R.G., Hewitt, J., Buchan, A.M. & Hsiang, Y.N. (2000a). Effect of endothelial and adventitial injury on somatostatin receptor expression. Surgery 127, 577–583.
Curtis, S.B., Hewitt, J., Yakubovitz, S., Anzarut, A., Hsiang, Y.N. & Buchan, A.M.J. (2000b). Somatostatin receptor subtype expression and function in human vascular tissue. Am.J.Physiol. 278, H1815–H1822.
Dalm, V.A., van Hagen, M., van Koetsveld, P.M., Langerak, A.W., van der Lely, A.-J., Lamberts, S.W. & Hofland, L.J. Cortistatin rather than somatostatin as a potential endogenous ligand for somatostatin receptors in the human immune system. J. Clin. Endocrinol. Metab. 88, 270–276 (2003).
Dasgupta, P., Singh, A.T. & Mukherjee, R. (2000). Lipophilization of somatostatin analog RC-160 with long chain fatty acid improves its anti-proliferative activity on human oral carcinoma cells in vitro. Life Sci. 66, 1557–1570.
De Lecea, L., Criado, J.R., Prospero-Garcia, O., Gautvik, K.M., Schweitzer, P., Danielson, P.E., Dunlop, C.L., Siggins, G.R., Henriksen, S.J. & Sutcliffe, J.G. (1996). A cortical neuropeptide with neuronal depressant and sleep-modulating properties. Nature 381, 242–245.
Delesque, N., Buscail, L., Esteve, J.P., Saint-Laurent, N., Mueller, C., Weckbecker, G., Bruns, C., Vaysse, N. & Susini, C. (1997). SST2 Somatostatin receptor expression reverses tumorigenicity of human pancreatic cancer cells. Cancer Res. 57, 956–962.
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. (1993). Cloning and expression of a human somatostatin-14-selective receptor variant (somatostatin receptor 4) located on chromosome 20. Mol.Pharmacol. 43, 894–901.
Epelbaum, J. (1986). Somatostatin in the central nervous system: physiology and pathological modifications. Prog.Neurobiol. (Oxford) 27, 63–100.
Epelbaum, J., Dournaud, P., Fodor, M. & Viollet, C. (1994). The neurobiology of somatostatin. Crit.Rev.Neurobiol. 8, 25–44.
Fehlmann, D., Langenegger, D., Schuepbach, E., Siehler, S., Feuerbach, D. & Hoyer, D. (2000). Distribution and characterisation of somatostatin receptor mRNA and binding sites in the brain and periphery. J.Physiol. (Paris) 94, 265–281.
Feniuk, W., Dimech, J. & Humphrey, P.P.A. (1993). Characterization of somatostatin receptors in guinea pig isolated ileum, vas deferens and right atrium. Br.J.Phartnacol. 110, 1156–1164.
Feniuk, W., Jarvie, E., Luo, J. & Humphrey, P P.A. (2000). Selective somatostatin sst2 receptor blockade with the novel cyclic octapeptide, CYN-154806. Neuropharmacology 39, 1443–1450.
Feuerbach, D., Fehlmann, D., Nunn, C., Siehler, S., Langenegger, D., Bouhelal, R., Seuwen, K. & Hoyer, D. (2000). Cloning, expression and pharmacological characterization of the mouse somatostatin sst5 receptor. Neuropharmacology 39, 1451–1462.
Foord, S.M. & Marshall, F.H. (1999). RAMPs: accessory proteins for seven transmembrane domain receptors. Trends Pharmacol.Sci. 20, 184–187.
Froidevaux, S. & Eberle, A.N. Somatostatin analogs and radiopeptides in cancer therapy. Biopolymers 66, 161–183 (2002).
Fukusumi, S., Kitada, C., Takekawa, S., Kizawa, H., Sakamoto, J., Miyamoto, M., Hinuma, S., Kitano, K. & Fujino, M. (1997). Identification and characterization of a novel human cortistatin-like peptide. Biochem.Biophys.Res.Commun. 232, 157–163.
Gademann, K., Kimmerlin, T, Hoyer, D. & Seebach, D. Peptide folding induces high and selective affinity of a linear and small 6-peptide to the human somatostatin receptor 4. J. Med. Chem. 44, 2460–2468 (2001).
Gu, Z.F., Corleto, V.D., Mantey, S.A., Coy, D.H., Maton, P.N. & Jensen, R.T. (1995). Somatostatin receptor subtype 3 mediates the inhibitory action of somatostatin on gastric smooth muscle cells. Am.J.Physiol. 268, G739–G748.
Hocart, S.J., Jain, R., Murphy, W.A., Taylor, J.E. & Coy, D.H. (1999). Highly potent cyclic disulfide antagonists of somatostatin. J.Med.Chem. 42, 1863–1871.
Hofland, L.J., van der Hoek, J., Van Koetsveld, P.M., Bruns, C. Weckbecker, Mooij, D., Waaijers, M., van Aken, M., Beckers, A., de Herder, W.W. & Lamberts, S.W.J. The novel somatostatin analog SOM230 inhibits ACTH release by cultured human corticotroph tumors. Endocrine Soc. Meeting, Abstract P2-499 (June 2003).
Hoyer, D., Bell, G.I., Berelowitz, M., Epelbaum, J., Feniuk, W., Humphrey, P.P., O’Carroll, A.M., Patel, Y.C., Schonbrunn, A., Taylor, J.E. & Reisine, T. (1995a). Classification and nomenclature of somatostatin receptors. Trends.Pharmacol.Sci. 16, 86–88.
Hoyer, D., Dixon, K., Gentsch, C., Vassout, A., Enz, A., Jaton, A., Nunn, C., Schoeffter, P., Neumann, P., Troxler, T. & Pfaeffli, P. NVP-SRA880, a somatostatin sst 1 receptor antagonist promotes social interactions, reduces aggressive behaviour and stimulates learning. The Pharmacologist, 44, 2, suppl. 1, A254 (2002).
Hoyer, D., Epelbaum, J., Feniuk, W., Humphrey, P.P.A., Meyerhof, W., Patel, Y., Reisine, T., Reubi, J.C., Schonbrunn, A. & Vezzani, A. (2000), “Classification of somatostatin receptors”. In: The IUPHAR compendium of receptor characterisation and classification, IUPHAR Media.
Hoyer, D., Luebbert, H. & Bruns, C. (1994). Molecular pharmacology of somatostatin receptors. Naunyn-Schmiedeberg’s Arch.Pharmacol. 350, 441–453.
Hoyer, D., Perez, J., Schoeffter, P., Langenegger, D., Schuepbach, E., Kaupmann, K., Luebbert, H., Bruns, C. & Reubi, J.C. (1995b). Pharmacological identity between somatostatin SS-2 binding sites and SSTR-1 receptors. Eur.J.Pharmacol, Mol.Pharmacol.Sect. 289, 151–161.
Kaupmann, K., Bruns, C., Raulf, F., Weber, H.P., Mattes, H. & Luebbert, H. (1995). Two amino acids, located in transmembrane domains VI and VII, determine the selectivity of the peptide agonist SMS 201–995 for the SSTR2 somatostatin receptor. EMBO J. 14, 727–735.
Kluxen, F.W., Bruns, C. & Luebbert, H. (1992). Expression cloning of a rat brain somatostatin receptor cDNA. Proc.Natl.Acad.Sci.U.S.A. 89, 4618–4622.
Koenig, J.A., Edwardson, J.M. & Humphrey, P.P. (1997). Somatostatin receptors in Neuro2A neuroblastoma cells: ligand internalization. Br.J.Pharmacol. 120, 52–59.
Krenning, E.P., Valkema, R., Kooij, P.P.M., Breeman, W.A.P., Bakker, W.H., De Herder, W.W., Van Eijck, C.H.J., Kwekkeboom, D.J., De Jong, M., Jamar, F. & Pauwels, S. (2000). The role of radioactive somatostatin and its analogues in the control of tumor growth. Recent Results Cancer Res. 153, 1–13.
Lamberts, S.W., Van Der Lely, A.J., De Herder, W.W. & Hofland, L.J. (1996). Octreotide. N.EngJ.Med. 334, 246–254.
Lamberts, S.W.J., Krenning, E.P. & Reubi, J.C. (1991). The role of somatostatin and its analogs in the diagnosis and treatment of tumors. Endocr.Rev. 12, 450–482.
Lanneau, C., Bluet-Pajot, M.T., Zizzari, P., Csaba, Z, Dournaud, P., Helboe, L., Hoyer, D., Pellegrini, E., Tannenbaum, G.S., Epelbaum, J. & Gardette, R. (2000). Involvement of the sst1 somatostatin receptor subtype in the intrahypothalamic neuronal network regulating growth hormone secretion: an in vitro and in vivo antisense study. Endocrinology 141, 967–979.
Lewis, I., Bauer, W., Albert, R., Chandramouli, N., Pless, J., Weckbecker, G. & Bruns, C. A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential. J. Med. Chem. 46, 2334–2344 (2003).
Liapakis, G., Hoeger, C., Rivier, J. & Reisine, T. (1996). Development of a selective agonist at the somatostatin receptor subtype SSTR1. J.Pharmacol.Exp.Ther. 276, 1089–1094.
Lichtenauer-Kaligis, E.G.R., Van Hagen, P.M., Lamberts, S.W.J. & Hofland, L.J. (2000). Somatostatin receptor subtypes in human immune cells. Eur.J.Endocrinol. 143, S21–S25.
Lloyd, K.C.K., Wang, J., Aurang, K., Gronhed, P., Coy, D.H. & Walsh, J.H. (1995). Activation of somatostatin receptor subtype 2 inhibits acid secretion in rats. Am.J.Physiol. 268, G102–G106.
Mandarine, L., Stenner, D., Blanchard, W., Nissen, S., Gerich, J., Ling, N., Brazeau, P., Bohlen, P., Esch, F. & Guillemin, R. (1981). Selective effects of somatostatin-14,-25 and-28 on in vitro insulin and glucagon secretion. Nature 291, 76–77.
Marshall, F.H., Jones, K.A., Kaupmann, K. & Bettler, B. (1999). GABAB receptors-the first 7TM heterodimers. Trends Pharmacol.Sci. 20, 396–399.
Martin, J.L., Chesselet, M.F., Raynor, K., Gonzales, C. & Reisine, T. (1991). Differential distribution of somatostatin receptor subtypes in rat brain revealed by newly developed somatostatin analogs. Neuroscience (Oxford) 41, 581–593.
Martinez, V., Curi, A.P., Torkian, B., Schaeffer, J.M., Wilkinson, H.A., Walsh, J.H. & Tache, Y. (1998). High basal gastric acid secretion in somatostatin receptor subtype 2 knockout mice. Gastroenterology 114, 1125–1132.
McHenry, L., Murthy, K.S., Grider, J.R. & Makhlouf, G.M. (1991). Inhibition of muscle cell relaxation by somatostatin: tissue-specific, cAMP-dependent, pertussis toxin-sensitive. AmJ.Physiol. 261, G45–G49.
McKeen, E.S., Feniuk, W., Michel, A.D., Kidd, E.J. & Humphrey, P.P.A. (1996). Identification and characterization of heterogeneous somatostatin binding sites in rat distal colonie mucosa. Naunyn-Schmiedeberg’s Arch.Pharmacol. 354, 543–549.
Meyerhof, W. (1998). The elucidation of somatostatin receptor functions: a current view. Rev.Physiol, Biochem. Pharmacol. 133, 55–105.
Meyerhof, W., Wulfsen, L, Schoenrock, C., Fehr, S. & Richter, D. (1992). 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.U.S.A. 89, 10267–10271.
Moldovan, S., DeMayo, F. & Brunicardi, F.C. (1998). Cloning of the mouse SSTR5 gene. J.Surg.Res. 76, 57–60.
Mundey, M.K., Ali, A., Mason, R. & Wilson, V.G. (2000). Pharmacological examination of contractile responses of the guinea-pig isolated ileum produced by μ-opioid receptor antagonists in the presence of, and following exposure to, morphine. Br.J.Pharmacol. 131, 893–902.
Nehring, R.B., Richter, D. & Meyerhof, W. (2000). Glycosylation affects agonist binding and signal transduction of the rat somatostatin receptor subtype 3. J.Physiol. (Paris) 94, 185–192.
Nunn, C. Rueping, M., Langenegger, D., Schuepbach, E., Kimmerlin, T., Micuh, P., Hurth, K., Seebach, D. & Hoyer, D. β2/β3-and α/β3-tetrapeptide derivatives as potent agonists at somatostatin sst4 receptors. Ncmnyn Schmiedeberg’s Arch. Pharmacol. 367, 95–103 (2003a).
Nunn, C., Langenegger, D., Hurth, K., Fehlmann, D., Schmidt, K. & Hoyer, D. Agonist properties of putative small molecule somatostatin receptor subtype-2 selective antagonists. Eur. J. Pharmacol., 465, 211–218 (2003c).
Nunn, C., Schoeffter, P., Langenegger, D. & Hoyer, D. Functional characterisation of the putative somatostatin sst2 receptor antagonist CYN 154806. Naunyn Schmiedeberg’s Arch Pharmacol. 367, 1–9 (2003b).
O’Carroll, A.M., Lolait, S.J., Koenig, M. & Mahan, L.C. (1992). Molecular cloning and expression of a pituitary somatostatin receptor with preferential affinity for somatostatin-28. Mol.Pharmacol. 42, 939–946.
Oomen, S.P.M.A., Hofland, L.J., Van Hagen, P.M., Lamberts, S.W.J. & Touw, I.P. (2000). Somatostatin receptors in the haematopoietic system. Eur.J.Endocrinol. 143, S9–S14.
Panetta, R., Greenwood, M.T., Warszynska, A., Demchyshyn, L.L., Day, R., Niznik, H.B., Srikant, C.B. & Patel, Y.C. (1994). 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, 417–427.
Parmar, R.M., Chan, W.W., Dashkevicz, M., Hayes, E.C., Rohrer, S.P., Smith, R.G., Schaeffer, J.M. & Blake, A.D. (1999). Nonpeptidyl somatostatin agonists demonstrate that sst2 and sst5 inhibit stimulated growth hormone secretion from rat anterior pituitary cells. Biochem.Biophys.Res.Commun. 263, 276–280.
Patel, Y.C. & Galanopoulou, A. (1995). Processing and intracellular targeting of prosomatostatin-derived peptides: the role of mammalian endoproteases. Ciba Found.Symp. 190, 26–50.
Patel, Y.C. & O’Neil, W. (1988). Peptides derived from cleavage of prosomatostatin at carboxyl-and amino-terminal segments. Characterization of tissue and secreted forms in the rat. J.Biol.Chem. 263,745–751.
Patel, Y.C. & Srikant, C.B. (1994). Subtype selectivity of peptide analogs for all five cloned human somatostatin receptors (hsstr 1–5). Endocrinology 135, 2814–2817.
Patel, Y.C. & Srikant, C.B. (1997). Somatostatin receptors. Trends Endocrinol.Metab. 8, 398–405.
Patel, Y.C. (1997). Molecular pharmacology of somatostatin receptor subtypes. J.Endocrinol.Invest. 20, 348–367.
Patel, Y.C. (1999). Somatostatin and its receptor family. Front.Neuroendocrinol. 20, 157–198.
Patel, Y.C., Greenwood, M., Kent, G., Panetta, R. & Srikant, C.B. (1993). Multiple gene transcripts of the somatostatin receptor SSTR2: Tissue selective distribution and cAMP regulation. Biochem.Biophys.Res.Commun. 192, 288–294.
Pfeiffer, M., Koch, T., Schroder, H., Klutzny, M., Kirscht, S., Kreienkamp, HJ., Hollt, V., Schulz, S., Homo-and heterodimerization of somatostatin receptor subtypes. Inactivation of sst(3) receptor function by heterodimerization with sst(2A). J. Biol. Chem. 276: 14027–14036 (2001).
Pfeiffer, M., Koch, T., Schroder, H., Laugsch, M., Hollt, V. & Schulz S. Heterodimerization of somatostatin and opioid receptors cross-modulates phosphorylation, internalization, and desensitization. J. Biol. Chem. 277, 19762–19772 (2002).
Piwko, C., Thoss, V.S. & Hoyer, D. (1995). Localization and pharmacological characterization of somatostatin sst2 sites in the rat cerebellum. Naunyn-Schmiedeberg’s Arch Pharmacol. 352, 607–613.
Piwko, C., Thoss, V.S., Probst, A. & Hoyer, D. (1996). Localization and pharmacological characterization of somatostatin recognition sites in human cerebellum. Neuropharmacology 35, 713–723.
Piwko, C., Thoss, V.S., Probst, A. & Hoyer, D. (1997). The elusive nature of cerebellar somatostatin receptors: studies in rat, monkey and human cerebellum. J Recept.Signal Transduction Res. 17, 385–105.
Poitout, L., Roubert, P., Contour-Galcera, M.-O., Moinet, C., Lannoy, J., Pommier, J., Plas, P., Bigg, D. & Thurieau, C. Identification of potent non-peptide somatostatin antagonists with ss3 selectivity. J. Med. Chem. 44, 2990–3000 (2001).
Pradayrol, L., Jornvall, H., Mutt, V. & Ribet, A. (1980). N-terminally extended somatostatin: the primary structure of somatostatin-28. FEBS Lett. 109, 55–58.
Prinz, C., Sachs, G., Walsh, J.H., Coy, D.H. & Wu, S.V. (1994). The somatostatin receptor subtype on rat enterochromaffinlike cells. Gastroenterology 107, 1067–1074.
Puebla, L., Mouchantaf, R., Sasi, R., Khare, S., Bennett, H.P.J., James, S. & Patel, Y.C. (1999). Processing of rat preprocortistatin in mouse AtT-20 cells. J.Neurochem. 73, 1273–1277.
Raynor, K. & Reisine, T. (1992). Somatostatin receptors. Crit.Rev.Neurobiol. 6, 273–289.
Raynor, K., Coy, D.C. & Reisine, T. (1992). Analogs of somatostatin bind selectively to brain somatostatin receptor subtypes. J.Neurochem. 59, 1241–1250.
Raynor, K., Murphy, W.A., Coy, D.H., Taylor, J.E., Moerau, J.P., Yasuda, K., Bell, G.I. & Reisine, T. (1993a). Cloned somatostatin receptors: Identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides. Mol.Pharmacol. 43, 838–844.
Raynor, K., O’Carroll, A.M., Kong, H., Yasuda, K., Mahana, L.C., Bell, G.I. & Reisine, T. (1993b). Characterization of cloned somatostatin receptors SSTR4 and SSTR5. Mol.Pharmacol. 44, 385–392.
Reichlin, S. (1983). Somatostatin. N.Engl.J.Med 309, 1556–1563.
Reisine, T. & Bell, G.I. (1995). Molecular biology of somatostatin receptors. Endocr.Rev. 16, 427–442.
Reubi, J.C. & Maurer, R. (1986). Different ionic requirements for somatostatin receptor subpopulations in the brain. Regul.Pept. 14, 301–311.
Reubi, J.C. (1984). Evidence for two somatostatin-14 receptor types in rat brain cortex. Neurosc.Lett. 49, 259–263.
Reubi, J.C., Schaer, J.C., Waser, B., Hoeger, C. & Rivier, J. (1998). A selective analog for the somatostatin sst1-receptor subtype expressed by human tumors. Eur.J.Pharmacol. 345,103–110.
Reubi, J.C., Schaer, J.C., Wenger, S., Hoeger, C., Erchegyi, J., Waser, B. & Rivier, J. SST3-selective potent peptidic somatostatin receptor antagonists. Proc. Natl. Acad. Sci. U.S.A. 97, 13973–13978 (2000).
Reubi, J:C., Eisenwiener, K.-P., Rink, H., Waser, B., & Macke, H.R. A new peptidic somatostatin agonist with high affinity to all five somatostatin receptors. Eur. J. Pharmacol. 456, 45–49 (2002).
Rocheville, M., Lange, D.C., Kumar, U., Patel, S.C., Patel, R.C. & Patel, Y.C. (2000a). Receptors for dopamine and somatostatin: Formation of hetero-oligomers with enhanced functional activity. Science (Washington, D.C.) 288, 154–157.
Rocheville, M., Lange, D.C., Kumar, U., Sasi, R., Patel, R.C. & Patel, Y.C. (2000b). Subtypes of the somatostatin receptor assemble as functional homo-and heterodimers. J.Biol.Chem. 275, 7862–7869.
Rohrer, L., Raulf, F., Brans, C., Buettner, R., Hofstaedter, F. & Schuele, R. (1993). Cloning and characterization of a fourth human somatostatin receptor. Proc.Natl.Acad.Sci.U.S.A. 90, 4196–4200.
Rohrer, S.P. & Berk, S.C. (1999). Development of somatostatin receptor subtype selective agonists through combinatorial chemistry. Curr.Opin.Drug Discovery Dev. 2, 293–303.
Rohrer, S.P. & Schaeffer, J.M. (2000). Identification and characterization of subtype selective somatostatin receptor agonists. J.Physiol. (Paris) 94, 211–215.
Rohrer, S.P., Birzin, E.T., Mosley, R.T., Berk, S.C., Hutchins, S.M., Shen, D.M., Xiong, Y., Hayes, E.C., Parmar, R.M., Poor, F., Mitra, S.W., Degrade, S.J., Shu, M., Klopp, J.M., Cai, S.J., Blake, A., Chan, W.W.S., Pasternak, A., Yang, L., Patchett, A.A., Smith, R.G., Chapman, K.T. & Schaeffer, J.M. (1998). Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science (Washington, D.C.) 282, 737–740.
Rossowski, W.J. & Coy, D.H. (1994). Specific inhibition of rat pancreatic insulin or glucagon release by receptor-selective somatostatin analogs. Biochem.Biophys.Res.Commun. 205, 341–346.
Rossowski, W.J., Gu, Z.F., Akarca, U.S., Jensen, R.T. & Coy, D.H. (1994). Characterization of somatostatin receptor subtypes controlling rat gastric acid and pancreatic amylase release. Peptides (Tarrytown, N.Y.) 15, 1421–1424.
Schindler, M., Harrington, K.A., Humphrey, P.P.A. & Emson, P.C. (1995). Cellular localization and co-expression of somatostatin receptor messenger RNAs in the human brain. Mol.Brain Res. 34, 321–326.
Schloos, J., Raulf, F., Hoyer, D. & Bruns, C. (1997). Identification and pharmacological characterization of somatostatin receptors in rat lung. Br.J.Pharmacol. 121, 963–971.
Schoeffter, P., Perez, J., Langenegger, D., Schuepbach, E., Bobirnac, I., Luebbert, H., Brans, C. & Hoyer, D. (1995). Characterization and distribution of somatostatin SS-1 and SRIF-1 binding sites in rat brain: identity with SSTR-2 receptors. Eur. J. Pharmacoi, Mol. Pharmacol. Sect. 289, 163–173.
Schwabe, W., Brennan, M.B. & Hochgeschwender, U. (1996). Isolation and characterization of the mouse (Mus musculus) somatostatin receptor type-4-encoding gene (mSSTR4). Gene 168, 233–235.
Seebach, D., Schaeffer, L., Brenner, M. & Hoyer, D. Design and synthesis of □-dipeptide derivatives with submicromolar affinities for human somatostatin receptors. Angew. Chemie, Int. Ed. 42, 776–778 (2003).
Sellers, L.A., Alderton, F., Carruthers, A.M., Schindler, M. & Humphrey, P.P.A. (2000). Receptor isoforms mediate opposing proliferative effects through Gβγ-activated p38 or Akt pathways. Mol. Cell. Biol. 20, 5974–5985.
Seimer, I-S., Schindler, M., Allen, J. P., Humphrey, P. P. A. & Emson, P. C. Advances in understanding neuronal somatostatin receptors. Reg. Pep. 90, 1–18 (2000).
Sharma, K. & Srikant, C.B. (1998). Induction of wild-type p53, Bax, and acidic endonuclease during somatostatin-signaled apoptosis in MCF-7 human breast cancer cells. Int. J. Cancer 76, 259–266.
Shimon, I., Taylor, J.E., Dong, J.Z., Bitonte, R.A., Kim, S., Morgan, B., Coy, D.H., Culler, M.D. & Melmed, S. (1997a). Somatostatin receptor subtype specificity in human fetal pituitary cultures. Differential role of SSTR2 and SSTR5 for growth hormone, thyroid-stimulating hormone, and prolactin regulation. J.Clin.Invest. 99, 789–798.
Shimon, I., Yan, X., Taylor, J.E., Weiss, M.H., Culler, M.D. & Melmed, S. (1997b). Somatostatin receptor (SSTR) subtype-selective analogs differentially suppress in vitro growth hormone and prolactin in human pituitary adenomas: novel potential therapy for functional pituitary tumors. J.Clin.Invest. 100, 2386–2392.
Siehler, S. & Hoyer, D. (1999a). Characterization of human recombinant somatostatin receptors. 2. Modulation of GTP.gamma.S binding. Naunyn-Schmiedeberg’s Arch.Pharmacol. 360, 500–509.
Siehler, S. & Hoyer, D. (1999b). Characterization of human recombinant somatostatin receptors. 3. Modulation of adenylate cyclase activity. Naunyn-Schmiedeberg’s Arch.Pharmacol. 360, 510–521.
Siehler, S. & Hoyer, D. (1999c). Characterization of human recombinant somatostatin receptors. 4. Modulation of phospholipase C activity. Naunyn-Schmiedeberg’s Arch.Pharmacol. 360, 522–532.
Siehler, S., Seuwen, K. & Hoyer, D. (1998a). [125I][Tyr3]octreotide labels human somatostatin sst2 and sst5 receptors. Eur.J.Pharmacol. 348, 311–320.
Siehler, S., Seuwen, K. & Hoyer, D. (1998b). [125I]TyrlO-cortistatinl4 labels all five somatostatin receptors. Naunyn-Schmiedeberg’s Arch.Pharmacol. 357, 483–489.
Siehler, S., Seuwen, K. & Hoyer, D. (1999a). Characterization of human recombinant somatostatin receptors. 1. Radioligand binding studies. Naunyn-Schmiedeberg’s Arch.Pharmacol. 360, 488–499.
Siehler, S., Zupanc, G.K.H., Seuwen, K. & Hoyer, D. (1999b). Characterization of the fish sst3 receptor, a member of the SRIF1 receptor family: atypical pharmacological features. Neuropharmacology 38, 449–462.
Spier, A.D. & De Lecea, L. (2000). Cortistatin: a member of the somatostatin neuropeptide family with distinct physiological functions. Brain Res.Rev. 33, 228–241.
Stolz, B., Weckbecker, G., Smith-Jones, P.M., Albert, R., Raulf, F. & Bruns, C. (1998). The somatostatin receptor-targeted radiotherapeutic [90Y-DOTA-dPhel,Tyr3]octreotide (90Y-SMT 487) eradicates experimental rat pancreatic CA 20948 tumors. Eur. J. Nucl. Med. 25, 668–674.
Strowski, M.Z., Parmar, R.M., Blake, A.D. & Schaeffer, J.M. (2000). Somatostatin inhibits insulin and glucagon secretion via two receptor subtypes: an in vitro study of pancreatic islets from somatostatin receptor 2 knockout mice. Endocrinology 141, 111–117.
Thoss, V.S., Perez, J., Due, D. & Hoyer, D. (1995). Embryonic and postnatal mRNA distribution of five somatostatin receptor subtypes in the rat brain. Neuropharmacology 34, 1673–1688.
Thoss, V.S., Piwko, C. & Hoyer, D. (1996). Somatostatin receptors in the rhesus monkey brain: localization and pharmacological characterization. Naunyn-Schmiedeberg’s Arch.Pharmacol. 353, 648–660.
Thoss, V.S., Piwko, C., Probst, A. & Hoyer, D. (1997). Autoradiographic analysis of somatostatin SRIF1 and SRIF2 receptors in the human brain and pituitary. Naunyn-Schmiedeberg’s Arch. Pharmacol. 355, 168–176.
Tilakaratne, N., Christopoulos, G., Zumpe, E.T., Foord, S.M. & Sexton, P.M. (2000). Amylin receptor phenotypes derived from human calcitonin receptor/RAMP coexpression exhibit pharmacological differences dependent on receptor isoform and host cell environment. J. Pharmacol. Exp. Ther. 294, 61–72.
Tran, V.T., Beal, M.F. & Martin, J.B. (1985). Two types of somatostatin receptors differentiated by cyclic somatostatin analogs. Science (Washington, D.C., 1883-) 228, 492–495.
Vale, W., Rivier, C., Brazeau, P. & Guillemin, R. (1974). Effects of somatostatin on the secretion of thyrotropin and prolactin. Endocrinology 95, 968–977.
Vanetti, M., Kouba, M., Wang, X., Vogt, G. & Hoellt, V. (1992). Cloning and expression of a novel mouse somatostatin receptor (SSTR2B). FEBS Lett. 311, 290–294.
Warhurst, G., Higgs, N.B., Fakhoury, H., Warhurst, A.C., Garde, J. & Coy, D.H. (1996). Somatostatin receptor subtype 2 mediates somatostatin inhibition of ion secretion in rat distal colon. Gastroenterologe 111, 325–333.
Weckbecker, G., Briner, U., Lewis, I. & Bruns, C. SOM230: a new somatostatin peptidomimetic with potent inhibitory effects on the growth hormone/insulin-like growth factor-I axis in rats, primates, and dogs. Endocrinology 143, 4123–4130 (2002).
Weckbecker, G., Raulf, F., Tolesvai, L. & Bruns, C. (1996). Potentiation of the anti-proliferative effects of anti-cancer drugs by octreotide in vitro and in vivo. Digestion 57, 22–28.
Weckbecker, G., Stolz, B., Susini, C. & Bruns, C. (1999), “Antiproliferative somatostatin analogues with potential in oncology”. In: Octreotide, the next decade. St. Lamberts, ed. BioScientifica Bristol, pp. 339–352.
White, J.H., Wise, A., Main, M.J., Green, A., Fraser, N.J., Disney, G.H., Barnes, A.A., Emson, P., Foord, S.M. & Marshall, F.H. (1998). Heterodimerization is required for the formation of a functional GABAB receptor. Nature 396, 679–682.
Wilkinson, G.F., Feniuk, W. & Humphrey, P.P. (1997). Characterization of human recombinant somatostatin sst5 receptors mediating activation of phosphoinositide metabolism. BrJ.Pharmacol. 121, 91–96.
Xu, Y., Song, J., Bruno, J.F. & Berelowitz, M. (1993). Molecular cloning and sequencing of a human somatostatin receptor, hSSTR4. Biochem.Biophys.Res.Commun. 193, 648–652.
Yamada, Y., Kagimoto, S., Kubota, A., Yasuda, K., Masuda, K., Someya, Y., Ihara, Y., Li, Q. & Imura, H. (1993a). Cloning, functional expression and pharmacological characterization of a fourth (hSSTR4) and a fifth (hSSTRS) human somatostatin receptor subtype. Biochem.Biophys.Res.Commun. 195, 844–852.
Yamada, Y., Post, S.R., Wang, K., Tager, H.S., Bell, G.I. & Seino, S. (1992a). Cloning and functional characterization of a family of human and mouse somatostatin receptors expressed in brain, gastrointestinal tract, and kidney. Proc. Natl. Acad. Sci. U.S.A. 89; 251–255.
Yamada, Y., Reisine, T., Law, S.F., Ihara, Y., Kubota, A., Kagimoto, S., Seino, M., Seino, Y., Bell, G.I. & Seino, S. (1992b). Somatostatin receptors, an expanding gene family: Cloning and functional characterization of human SSTR3, a protein coupled to adenylyl cyclase. Mol. Endocrinol. 6, 2136–2142.
Yamada, Y., Stoffel, M., Espinosa, R.E. III, Xiang, K.S., Seino, M., Seino, S., Le Beau, M.M. & Bell, G.I. (1993b). Human somatostatin receptor genes: Localization to human chromosomes 14, 17, and 22 and identification of simple tandem repeat polymorphisms. Genomics 15, 449–452.
Yang, L., Berk, S.C., Rohrer, S.P. Mosley, R.T., Guo, L., Underwood, D.J., Arison, B.H., Birzin, E.T., Hayes, E.C., Mitra, S.W., Parmar, R.M., Cheng, K., Wu, T.J., Butler, B.S., Poor, F., Pasternak, A., Pan, Y., Silva, M., Freidinger, R.M., Smith, R.G., Chapman, K., Schaeffer, J.M. & Patchett, A.A. (1998). Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2. Proc. Natl. Acad. Sci. U.S.A. 95, 10836–10841.
Yasuda, K., Rens-Domiano, S., Breder, C.D., Law, S.F., Saper, C.B., Reisine, T. & Bell, G.I. (1992). Cloning of a novel somatostatin receptor, SSTR3, coupled to adenylyl cyclase. J. Biol. Chem. 267, 20422–20428.
Zaki, M., Harrington, L., McCuen, R., Coy, D.H., Arimura, A. & Schubert, M.L. (1996). Somatostatin receptor subtype 2 mediates inhibition of gastrin and histamine secretion from human, dog, and rat antrum. Gastroenterology 111, 919–924.
Zheng, H., Bailey, A., Jiang, M.H., Honda, K., Chen, H.Y., Trumbauer, M.E., Van der Ploeg, L.H., Schaeffer, J.M., Leng, G. & Smith, R.G. (1997). Somatostatin receptor subtype 2 knockout mice are refractory to growth hormone-negative feedback on arcuate neurons. Mol. Endocrinol. 11, 1709–1717.
Zumpe, E.T., Tilakaratne, N., Fraser, N.J., Christopoulos, G., Foord, S.M. & Sexton, P.M. (2000). Multiple Ramp Domains Are Required for Generation of Amylin Receptor Phenotype from the Calcitonin Receptor Gene Product. Biochem. Biophys. Res. Commun. 267, 368–372.
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2004 Springer Science + Business Media, Inc.
About this chapter
Cite this chapter
Hannon, J.P., Bruns, C., Weckbecker, G., Hoyer, D. (2004). Somatostatin Receptor Gene Family - Subtype Selectivity for Ligand Binding. In: Srikant, C.B. (eds) Somatostatin. Endocrine Updates, vol 24. Springer, Boston, MA. https://doi.org/10.1007/1-4020-8033-6_6
Download citation
DOI: https://doi.org/10.1007/1-4020-8033-6_6
Publisher Name: Springer, Boston, MA
Print ISBN: 978-1-4020-7799-9
Online ISBN: 978-1-4020-8033-3
eBook Packages: Springer Book Archive