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Somatostatin

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References

  • Bauer W, Briner U, Doepfner W, Haller R, Huguenin R, Marbach P, Petcher TJ, Pless J (1982) SMS 201-995: a very potent and selective octapeptide analogue of somatostatin with prolonged action. Life Sci 31:1133–1140

    Article  CAS  PubMed  Google Scholar 

  • 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

    Article  CAS  PubMed  Google Scholar 

  • Buchan AM, Lin CY, Choi J, Barber DL (2002) Somatostatin, acting at receptor subtype 1, inhibits Rho activity, the assembly of actin stress fibers, and cell migration. J Biol Chem 277:28431–28438

    Article  CAS  PubMed  Google Scholar 

  • Callaghan B, Furness JB (2014) Novel and conventional receptors for ghrelin, desacyl-ghrelin, and pharmacologically related compounds. Pharmacol Rev 66:984–1001

    Article  CAS  PubMed  Google Scholar 

  • Cervia D, Casini G, Bagnoli P (2008) Physiology and pathology of somatostatin in the mammalian retina: a current view. Mol Cell Endocrinol 286:112–122

    Article  CAS  PubMed  Google Scholar 

  • Colao A, Petersenn S, Newell-Price J, Findling JW, Gu F, Maldonado M, Schoenherr U, Mills D, Salgado LR, Biller BM (2012) Pasireotide B2305 Study Group. A 12-month phase 3 study of pasireotide in Cushing’s disease. N Engl J Med 366:914–924

    Article  CAS  PubMed  Google Scholar 

  • Conlon JM, Tostivint H, Vaudry H (1997) Somatostatin- and urotensin II-related peptides: molecular diversity and evolutionary perspectives. Regul Pept 69:95–103

    Article  CAS  PubMed  Google Scholar 

  • Córdoba-Chacón J, Gahete MD, Durán-Prado M, Luque RM, Castaño JP (2011) Truncated somatostatin receptors as new players in somatostatin-cortistatin pathophysiology. Ann N Y Acad Sci 1220:6–15

    Article  PubMed  CAS  Google Scholar 

  • Cuevas-Ramos D, Carmichael JD, Cooper O, Bonert VS, Gertych A, Mamelak AN, Melmed S (2015) A structural and functional acromegaly classification. J Clin Endocrinol Metab 100:122–131

    Article  CAS  PubMed  Google Scholar 

  • de Lecea L, Criado JR, Prospero-Garcia O, Gautvik KM, Schweitzer P, Danielson PE, Dunlop CLM, Siggins GR, Henriksen SJ, Sutcliffe JG (1996) A cortical neuropeptide with neuronal depressant and sleep-modulating properties. Nature 381:242–245

    Article  PubMed  Google Scholar 

  • Durán-Prado M, Gahete MD, Martínez-Fuentes AJ, Luque RM, Quintero A, Webb SM, Benito-López P, Leal A, Schulz S, Gracia-Navarro F et al (2009) Identification and characterization of two novel truncated but functional isoforms of the somatostatin receptor subtype 5 differentially present in pituitary tumors. J Clin Endocrinol Metab 94:2634–2643

    Article  PubMed  CAS  Google Scholar 

  • Ensinck JW, Baskin DG, Vahl TP, Vogel RE, Laschansky EC, Francis BH, Hoffman RC, Krakover JD, Stamm MR, Low MJ et al (2002) Thrittene, homologous with somatostatin-28((1-13)), is a novel peptide in mammalian gut and circulation. Endocrinology 143:2599–2609

    Article  CAS  PubMed  Google Scholar 

  • Ensinck JW, Laschansky EC, Vogel RE, D’Alessio DA (2003) Effect of ingested nutrients on the release of thrittene into the human circulation. J Clin Endocrinol Metab 88:4798–4804

    Article  CAS  PubMed  Google Scholar 

  • Gadelha MR, Bronstein MD, Brue T, Coculescu M, Fleseriu M, Guitelman M, Pronin V, Raverot G, Shimon I, Lievre KK et al (2014) Pasireotide C2402 Study Group. Pasireotide versus continued treatment with octreotide or lanreotide in patients with inadequately controlled acromegaly (PAOLA): a randomised, phase 3 trial. Lancet Diabetes Endocrinol 2:875–884

    Article  CAS  PubMed  Google Scholar 

  • Gatto F, Feelders RA, Franck SE, van Koetsveld PM, Dogan F, Kros JM, Neggers SJCMM, van der Lely A-J, Lamberts SWJ, Ferone D et al (2017) In vitro head-to-head comparison between octreotide and pasireotide in GH-secreting pituitary adenomas. J Clin Endocrinol Metab 102:2009–2018

    Article  PubMed  Google Scholar 

  • Giustina A, Mazziotti G, Torri V, Spinello M, Floriani I, Melmed S (2012) Metaanalysis on the effects of octreotide on tumor mass in acromegaly. PLoS One 7:e36411

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Gunther T, Tulipano G, Dournaud P, Bousquet C, Csaba Z, Kreienkamp HJ, Lupp A, Korbonits M, Castano JP, Wester HJ, Culler M, Melmed S, Schulz S (2018) International union of basic and clinical pharmacology. CV. Somatostatin receptors: structure, function, ligands, and new nomenclature. Pharmacol Rev 70:763–835

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  • Heiman ML, Murphy WA, Coy DH (1987) Differential binding of somatostatin agonists to somatostatin receptors in brain and adenohypophysis. Neuroendocrinology 45:429–436

    Article  CAS  PubMed  Google Scholar 

  • Johansson O, Hökfelt T, Elde RP (1984) Immunohistochemical distribution of somatostatin-like immunoreactivity in the central nervous system of the adult rat. Neuroscience 13:265–339

    Article  CAS  PubMed  Google Scholar 

  • Kreienkamp H-J, Roth A, Richter D (1998) Rat somatostatin receptor subtype 4 can be made sensitive to agonist-induced internalization by mutation of a single threonine (residue 331). DNA Cell Biol 17:869–878

    Article  CAS  PubMed  Google Scholar 

  • Krenning EP, Bakker WH, Breeman WA, Koper JW, Kooij PP, Ausema L, Lameris JS, Reubi JC, Lamberts SWJ (1989) Localisation of endocrine-related tumours with radioiodinated analogue of somatostatin. Lancet 1:242–244

    Article  CAS  PubMed  Google Scholar 

  • Lehmann A, Kliewer A, Schütz D, Nagel F, Stumm R, Schulz S (2014) Carboxylterminal multi-site phosphorylation regulates internalization and desensitization of the human sst2 somatostatin receptor. Mol Cell Endocrinol 387:44–51

    Article  CAS  PubMed  Google Scholar 

  • Lehmann A, Kliewer A, Günther T, Nagel F, Schulz S (2016) Identification of phosphorylation sites regulating sst3 somatostatin receptor trafficking. Mol Endocrinol 30:645–659

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Lesche S, Lehmann D, Nagel F, Schmid HA, Schulz S (2009) Differential effects of octreotide and pasireotide on somatostatin receptor internalization and trafficking in vitro. J Clin Endocrinol Metab 94:654–661

    Article  CAS  PubMed  Google Scholar 

  • Liu Y, Lu D, Zhang Y, Li S, Liu X, Lin H (2010) The evolution of somatostatin in vertebrates. Gene 463:21–28

    Article  CAS  PubMed  Google Scholar 

  • Müller EE, Locatelli V, Cocchi D (1999) Neuroendocrine control of growth hormone secretion. Physiol Rev 79:511–607

    Article  PubMed  Google Scholar 

  • Oakley RH, Laporte SA, Holt JA, Caron MG, Barak LS (2000) Differential affinities of visual arrestin, beta arrestin1, and beta arrestin2 for G protein-coupled receptors delineate two major classes of receptors. J Biol Chem 275:17201–17210

    Article  CAS  PubMed  Google Scholar 

  • Olias G, Viollet C, Kusserow H, Epelbaum J, Meyerhof W (2004) Regulation and function of somatostatin receptors. J Neurochem 89:1057–1091

    Article  CAS  PubMed  Google Scholar 

  • Patel YC (1999) Somatostatin and its receptor family. Front Neuroendocrinol 20:157–198

    Article  CAS  PubMed  Google Scholar 

  • Peineau S, Potier B, Petit F, Dournaud P, Epelbaum J, Gardette R (2003) AMPAsst2 somatostatin receptor interaction in rat hypothalamus requires activation of NMDA and/or metabotropic glutamate receptors and depends on intracellular calcium. J Physiol 546:101–117

    Article  CAS  PubMed  Google Scholar 

  • Petrich A, Mann A, Kliewer A, Nagel F, Strigli A, Märtens JC, Pöll F, Schulz S (2013) Phosphorylation of threonine 333 regulates trafficking of the human sst5 somatostatin receptor. Mol Endocrinol 27:671–682

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Peverelli E, Mantovani G, Calebiro D, Doni A, Bondioni S, Lania A, Beck-Peccoz P, Spada A (2008) The third intracellular loop of the human somatostatin receptor 5 is crucial for arrestin binding and receptor internalization after somatostatin stimulation. Mol Endocrinol 22:676–688

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Pfeiffer M, Koch T, Schröder H, Klutzny M, Kirscht S, Kreienkamp H-J, Höllt V, Schulz S (2001) Homo- and heterodimerization of somatostatin receptor subtypes: inactivation of sst(3) receptor function by heterodimerization with sst(2A). J Biol Chem 276:14027–14036

    Article  CAS  PubMed  Google Scholar 

  • Pfeiffer M, Koch T, Schröder H, Laugsch M, Höllt V, Schulz S (2002) Heterodimerization of somatostatin and opioid receptors cross-modulates phosphorylation, internalization, and desensitization. J Biol Chem 277:19762–19772

    Article  CAS  PubMed  Google Scholar 

  • Rai U, Thrimawithana TR, Valery C, Young SA (2015) Therapeutic uses of somatostatin and its analogues: current view and potential applications. Pharmacol Ther 152:98–110

    Article  CAS  PubMed  Google Scholar 

  • Rocheville M, Lange DC, Kumar U, Patel SC, Patel RC, Patel YC (2000a) Receptors for dopamine and somatostatin: formation of hetero-oligomers with enhanced functional activity. Science 288:154–157

    Article  CAS  PubMed  Google Scholar 

  • Rocheville M, Lange DC, Kumar U, Sasi R, Patel RC, Patel YC (2000b) Subtypes of the somatostatin receptor assemble as functional homo- and heterodimers. J Biol Chem 275:7862–7869

    Article  CAS  PubMed  Google Scholar 

  • Roth A, Kreienkamp H-J, Meyerhof W, Richter D (1997) Phosphorylation of four amino acid residues in the carboxyl terminus of the rat somatostatin receptor subtype 3 is crucial for its desensitization and internalization. J Biol Chem 272:23769–23774

    Article  CAS  PubMed  Google Scholar 

  • Samson WK, Zhang JV, Avsian-Kretchmer O, Cui K, Yosten GLC, Klein C, Lyu R-M, Wang YX, Chen XQ, Yang J et al (2008) Neuronostatin encoded by the somatostatin gene regulates neuronal, cardiovascular, and metabolic functions. J Biol Chem 283:31949–31959

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Schreff M, Schulz S, Händel M, Keilhoff G, Braun H, Pereira G, Klutzny M, Schmidt H, Wolf G, Höllt V (2000) Distribution, targeting, and internalization of the sst4 somatostatin receptor in rat brain. J Neurosci 20:3785–3797

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Schulz S, Lehmann A, Kliewer A, Nagel F (2014) Fine-tuning somatostatin receptor signalling by agonist-selective phosphorylation and dephosphorylation: IUPHAR review 5. Br J Pharmacol 171:1591–1599

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Siehler S, Nunn C, Hannon J, Feuerbach D, Hoyer D (2008) Pharmacological profile of somatostatin and cortistatin receptors. Mol Cell Endocrinol 286:26–34

    Article  CAS  PubMed  Google Scholar 

  • Smalley KSM, Koenig JA, Feniuk W, Humphrey PPA (2001) Ligand internalization and recycling by human recombinant somatostatin type 4 (h sst(4)) receptors expressed in CHO-K1 cells. Br J Pharmacol 132:1102–1110

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Spier AD, de Lecea L (2000) Cortistatin: a member of the somatostatin neuropeptide family with distinct physiological functions. Brain Res Brain Res Rev 33:228–241

    Article  CAS  PubMed  Google Scholar 

  • Stengel A, Karasawa H, Taché Y (2015) The role of brain somatostatin receptor 2 in the regulation of feeding and drinking behavior. Horm Behav 73:15–22

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Stroh T, Jackson AC, Sarret P, Dal Farra C, Vincent JP, Kreienkamp HJ, Mazella J, Beaudet A (2000) Intracellular dynamics of sst5 receptors in transfected COS-7 cells: maintenance of cell surface receptors during ligand-induced endocytosis. Endocrinology 141:354–365

    Article  CAS  PubMed  Google Scholar 

  • Tulipano G, Schulz S (2007) Novel insights in somatostatin receptor physiology. Eur J Endocrinol 156(Suppl 1):S3–S11

    Article  CAS  PubMed  Google Scholar 

  • Tulipano G, Stumm R, Pfeiffer M, Kreienkamp H-J, Höllt V, Schulz S (2004) Differential b-arrestin trafficking and endosomal sorting of somatostatin receptor subtypes. J Biol Chem 279:21374–21382

    Article  CAS  PubMed  Google Scholar 

  • Urban-Ciecko J, Barth AL (2016) Somatostatin-expressing neurons in cortical networks. Nat Rev Neurosci 17:401–409

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Viollet C, Lepousez G, Loudes C, Videau C, Simon A, Epelbaum J (2008) Somatostatinergic systems in brain: networks and functions. Mol Cell Endocrinol 286:75–87

    Article  CAS  PubMed  Google Scholar 

  • Vockel M, Breitenbach U, Kreienkamp H-J, Brandner JM (2010) Somatostatin regulates tight junction function and composition in human keratinocytes. Exp Dermatol 19:888–894

    Article  CAS  PubMed  Google Scholar 

  • Vockel M, Pollok S, Breitenbach U, Ridderbusch I, Kreienkamp H-J, Brandner JM (2011) Somatostatin inhibits cell migration and reduces cell counts of human keratinocytes and delays epidermal wound healing in an ex vivo wound model. PLoS One 6:e19740

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Yosten GLC, Elrick MM, Salvatori A, Stein LM, Kolar GR, Ren J, Corbett JA, Samson WK (2015) Understanding peptide biology: the discovery and characterization of the novel hormone, neuronostatin. Peptides 72:192–195

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  • Zhao P, Canals M, Murphy JE, Klingler D, Eriksson EM, Pelayo JC, Hardt M, Bunnett NW, Poole DP (2013) Agonist-biased trafficking of somatostatin receptor 2A in enteric neurons. J Biol Chem 288:25689–25700

    Article  CAS  PubMed  PubMed Central  Google Scholar 

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Authors and Affiliations

  1. Unit of Pharmacology, Department of Molecular and Translational Medicine, University of Brescia, Brescia, Italy

    Giovanni Tulipano

  2. Institut für Pharmakologie & Toxikologie, Universitätsklinikum Jena, Friedrich-Schiller-Universität Jena, Jena, Germany

    Stefan Schulz

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  1. Giovanni Tulipano
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  2. Stefan Schulz
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Correspondence to Stefan Schulz .

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Editors and Affiliations

  1. Max-Planck-Institut Herz/Lungenforschg., Bad Nauheim, Hessen, Germany

    Stefan Offermanns

  2. Presidential Office, Friedrich-Schiller University Jena, Jena, Thüringen, Germany

    Walter Rosenthal

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Tulipano, G., Schulz, S. (2021). Somatostatin. In: Offermanns, S., Rosenthal, W. (eds) Encyclopedia of Molecular Pharmacology. Springer, Cham. https://doi.org/10.1007/978-3-030-21573-6_137-1

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  • DOI: https://doi.org/10.1007/978-3-030-21573-6_137-1

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