Skip to main content
SpringerLink
Log in

Endocrine, Gastrointestinal, and Antitumor Activity of Somatostatin Analogues

  • Chapter
Neural and Endocrine Peptides and Receptors

Abstract

Since recent studies with somatostatin were carefully reviewed by Reichlin (1983) and by a variety of authors in the 2nd International Symposium on Somatostatin, which was held in Athens in 1981 but published with updates in 1984 (Raptis et al., 1984), no attempts are made to cover new developments with somatostatin-14 and somatostatin-28. Instead, this chapter focuses on the recent work in the field of somatostatin analogues and the investigations of their endocrine, gastrointestinal, and antitumor activities.

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

Access this chapter

Log in via an institution
Chapter
USD 29.95
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
eBook
USD 39.99
Price excludes VAT (USA)
  • Available as PDF
  • Read on any device
  • Instant download
  • Own it forever
Softcover Book
USD 54.99
Price excludes VAT (USA)
  • Compact, lightweight edition
  • Dispatched in 3 to 5 business days
  • Free shipping worldwide - see info

Tax calculation will be finalised at checkout

Purchases are for personal use only

Institutional subscriptions

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  • Adrian, T. E., Barnes, A. J., Long, R. G., O’Shaughnessy, D. J., Brown, M. R., Rivier, J., Vale, W., Blackburn, A. M., and Bloom, S. R., 1981, The effect of somatostatin analogs on secretion of growth, pancreatic, and gastrointestinal hormones in man, J. Clin. Endocrol. Metab. 53:675–681.

    Article  CAS  Google Scholar 

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

    Article  PubMed  CAS  Google Scholar 

  • Bloom, S. R., Thorner, M. O., Besser, G. M., Hall, R., Gomez-Pan, A., Roy, V. M., Russell, R. C. G., Coy, D. H., Kastin, A. J., and Schally, A. V., 1974, Inhibition of gastrin and gastric-acid secretion by growth-hormone release-inhibiting hormone, Lancet 2:1106.

    Article  PubMed  CAS  Google Scholar 

  • Brown, M. E., Rivier, J. E., and Vale, W. W., 1977, Somatostatin analogs with selected biological activities, Science 196:1467–1468.

    Article  PubMed  CAS  Google Scholar 

  • Brown, M. P., Coy, D. H., Gomez-Pan, A., Hirst, B. H., Hunter, M., Meyers, C., Reed, J. D., Schally, A. V., and Shaw, B., 1978, Structure-activity relationships of eighteen somatostatin analogues on gastric secretion, J. Physiol. (Lond.) 277:1–14.

    CAS  Google Scholar 

  • Cai, R.-Z., Szoke, B., Fu, D., Redding, T. W., Colaluca, J., Torres-Aleman, I., and Schally, A. V., 1986, in: Proceedings of the Ninth American Peptide Symposium June 1985 (V. J. Hruby, K. D. Kopple, and C. M. Deber, eds.), Pierce Chemical Co., Rockford, II, pp. 627–630.

    Google Scholar 

  • Charro, A. L., Cabranes, J. A., Lafuente, A., Diaz-Salgado, C., Cordero, M., Almoguera, E., Comaru-Schally, A. M., Meyers, C. A., Coy, D. H., and Schally, A. V., 1984, Inhibition of growth hormone and glucagon release by Phe-4-somatostatin in patients with acromegaly, Res. Commun. Chem. Pathol. Pharmacol. 45:432–444.

    PubMed  CAS  Google Scholar 

  • Dembinski, A. B., and Johnson, L. R., 1980, Stimulation of pancreatic growth by secretin, caerulein, and pentagastrin, Endocrinology 106:323–328.

    Article  PubMed  CAS  Google Scholar 

  • De Quijada, M. G., Redding, T. W., Coy, D. H., Torres-Aleman, I., and Schally, A. V., 1983, Inhibition of growth of a prolactin-secreting pituitary tumor in rats by analogs of luteinizing hormone-releasing hormone and somatostatin, Proc. Natl. Acad. Sci. U.S.A. 80:3485–3488.

    Article  PubMed  Google Scholar 

  • Dollinger, H. C., Raptis, S., and Pfeiffer, E. F., 1976, Effects of somatostatin on exocrine and endocrine pancreatic function stimulated by intestinal hormones in man, Horm. Metab. Res. 8:74–78.

    Article  PubMed  CAS  Google Scholar 

  • Downward, J., Yarden, Y., Mayes, E., Scrace, G., Totty, N., Stockwell, P., Ullrich, A., Schlessinger, J., and Waterfield, M. D., 1984, Close similarity of epidermal growth factor receptor and v-erb-B oncogene protein sequences, Nature 307:521–527.

    Article  PubMed  CAS  Google Scholar 

  • Gibbs, J., Young, R. C., and Smith, G. P., 1973, Cholecystokinin elicits satiety in rats with open gastric fistulas, Nature 245:323–325.

    Article  PubMed  CAS  Google Scholar 

  • Gonzalez-Barcena, D., Mendoza, F., Medina, R., Coy, D. H., Murphy, W. A., and Schally, A. V., 1984, Effect of Ala-2-D-Trp-8-D-Cys-14-somatostatin on the arginine induced release of insulin, GH and glucagon in normal men, Endocrine Res. 10:39–48.

    CAS  Google Scholar 

  • Gottesman, E. S., Mandarino, L. J., and Gerich, J. E., 1982, Somatostatin, in: Special Topics in Endocrinology and Metabolism, Vol. 4 (M. Cohen, ed.), Alan R. Liss, New York, pp. 177–243.

    Google Scholar 

  • Grant, N., Clark, D., Garsky, V., Juanakais, E., McGregor, W., and Sarantakis, D., 1976, Dissociation of somatostatin effects. Peptides inhibiting the release of growth hormone but not glucagon or insulin in rats, Life Sci. 19:629–632.

    Article  PubMed  CAS  Google Scholar 

  • Hall, R., and Gomez-Pan, A., 1976, The hypothalamic regulatory hormones and their clinical applications, Adv. Clin. Chem. 18:173–212.

    Article  PubMed  CAS  Google Scholar 

  • Heldin, C.-H., and Westermark, B., 1984, Growth factors: Mechanism of action and relation to on-cogenes, Cell 37:9–20.

    Article  PubMed  CAS  Google Scholar 

  • Hierowski, M. T., Liebow, C., du Sapin, K., and Schally, A. V., 1985, Stimulation by somatostatin of dephosphorylation of membrane proteins in pancreatic cancer MIA PaCa-2 cell line, FEBS Lett. 179:252–256.

    Article  PubMed  CAS  Google Scholar 

  • Hirst, B. H., Shaw, B., Meyers, C. A., and Coy, D. H., 1980, Structure-activity studies with somatostatin: The role of tryptophan in position 8, Regul. Peptides 1:97–113.

    Article  CAS  Google Scholar 

  • Hirst, B. H., Arilla, E., Coy, D. H., and Shaw, B., 1984, Cyclic hexa-and pentapeptide somatostatin analogues with reduced gastric inhibitory activity, Peptides 5:857–860.

    Article  PubMed  CAS  Google Scholar 

  • Konturek, S. J., Tasler, J., Krol, R., Dembinski, A., Coy, D. H., and Schally, A. V., 1977, Effect of somatostatin analogs on gastric and pancreatic secretion, Proc. Soc. Exp. Biol. Med. 155:519–522.

    PubMed  CAS  Google Scholar 

  • Konturek, S. J., Cieszkowski, M., Bilski, J., Konturek, J., Bielanski, W., and Schally, A. V., 1985, Effects of cyclic hexapeptide analog of somatostatin on pancreatic secretion in dogs, Proc. Soc. Exp. Biol. Med. 178:68–72.

    PubMed  CAS  Google Scholar 

  • Kraenzlin, M. E., Ch’ng, J. C., Wood, S. M., and Bloom, S. R., 1983, Can inhibition of hormone secretion be associated with endocrine tumour shrinkage? Lancet 2:1501.

    Article  PubMed  CAS  Google Scholar 

  • Kraenzlin, M. E., Ch’ng, J. L. C., Wood, S. M., and Bloom, S. R., 1984, Remission of symptoms and shrinkage of metastasis with long term treatment with somatostatin analogue, Gut 25:A576.

    Google Scholar 

  • Lamberts, S. W. J., Uitterlinden, P., Zuiderwijk, J., Verleun, T., Neufeld, M., and Del Pozo, E., 1984, The effects of a long-acting somatostatin analog on pituitary tumor growth and hormone secretion in rat and man, Excerpta Med. 652:847.

    Google Scholar 

  • Long, R. G., Barnes, A. J., Adrian, T. E., Mallinson, C. N., Brown, M. R., Vale, W., Rivier, J. E., Christopides, N. D., and Bloom, S. R., 1979, Suppression of pancreatic endocrine tumour secretion by long-acting somatostatin analogue, Lancet 2:764–767.

    Article  PubMed  CAS  Google Scholar 

  • Marbach, M., Neufeld, M., and Pless, J., 1984, Clinical applications of somatostatin analogs, in: Proceedings of the Symposium on Somatostatin, Montreal, July 1984 (Y. C. Patel and G. S. Tannenbaum, eds.), Elsevier, Amsterdam, pp. 339–345.

    Google Scholar 

  • Mascardo, R. N., and Sherline, P., 1982, Somatostatin inhibits rapid centrosomal separation and cell proliferation induced by epidermal growth factor, Endocrinology 111:1394–1396.

    Article  PubMed  CAS  Google Scholar 

  • Maton, P. N., O’Dorisio, T. M., Howe, B. A., McArthur, K. E., Howard, J. M., Cherner, J. A., Malarkey, T. B., Collen, M. J., Gardner, J. D., and Jensen, R. T., 1985, Effect of a long-acting somatostatin analogue (SMS 201–995) in a patient with pancreatic cholera, N. Engl. J. Med. 312:17–21.

    Article  PubMed  CAS  Google Scholar 

  • McCumbee, W. D., McCarty, D. S., Jr., and Lebovitz, H. E., 1980, Hormone responsiveness of a transplantable rat chondrosarcoma. II. Evidence for in vivo hormone dependence, Endocrinology 106:1930–1940.

    Article  PubMed  CAS  Google Scholar 

  • Merrifield, R. B., 1967, Solid phase peptide synthesis. III. An improved synthesis of bradykinin, Recent Prog. Horm. Res. 23:451–482.

    PubMed  CAS  Google Scholar 

  • Meyers, C., Arimura, A., Gordin, A., Fernandez-Durango, R., Coy, D. H., Schally, A. V., Drouin, J., Ferland, L., Beaulieu, M., and Labrie, F., 1977, Somatostatin analogs which inhibit glucagon and growth hormone more than insulin release, Biochem. Biophys. Res. Commun. 74:630–636.

    Article  PubMed  CAS  Google Scholar 

  • Meyers, C. A., Coy, D. H., Huang, W. Y., Schally, A. V., and Redding, T. W., 1978, Highly active position eight analogues of somatostatin and separation of peptide diastereomers by partition chro-matography, Biochemistry 17:2326–2331.

    Article  PubMed  CAS  Google Scholar 

  • Mortimer, C. H., Tunbridge, W. M. G., Carr, D., Yeomans, L., Lind, T., Coy, D. H., Bloom, S. R., Kastin, A., Mallinson, C. N., Besser, G. M., Schally, A. V., and Hall, R., 1974, Effects of growth-hormone release-inhibiting hormone on circulating glucagon, insulin, and growth hormone in normal, diabetic, acromegalic, and hypo-pituitary patients, Lancet 1:697–701.

    Article  PubMed  CAS  Google Scholar 

  • Pfeiffer, E. F., and Schusdziarra, V., 1984, What can a clinician extract from the development of somatostatin for therapy? in: 2nd International Symposium on Somatostatin, Athens (Greece) (S. Raptis, J. Rosenthal, and J. E. Gerich, eds.), Attempto Verlag, Tübingen, pp. 222–231.

    Google Scholar 

  • Plewe, G., Beyer, J., Krause, U., Neufeld, M., and Del Pozo, E., 1984, Long-acting and selective suppression of growth hormone secretion by somatostatin analogue SMS 201–995 in acromegaly, Lancet 2:782–784.

    Article  PubMed  CAS  Google Scholar 

  • Raptis, S., Rosenthal, J., and Gerich, J. E., eds., 1984, 2nd International Symposium on Somatostatin, Athens (Greece), Attempto Verlag, Tübingen.

    Google Scholar 

  • Redding, T. W., and Schally, A. V., 1983, Inhibition of growth of the transplantable rat chondrosarcoma by analogs of hypothalamic hormones, Proc. Natl. Acad. Sci. U.S.A. 80:1078–1082.

    Article  PubMed  CAS  Google Scholar 

  • Redding, T. W., and Schally, A. V., 1984, Inhibition of growth of pancreatic carcinomas in animal models by analogs of hypothalamic hormones, Proc. Natl. Acad. Sci. U.S.A. 81:248–252.

    Article  PubMed  CAS  Google Scholar 

  • Redding, T. W., Schally, A. V., Tice, T. R., and Meyers, W. E., 1984, Long-acting delivery systems for peptides: Inhibition of rat prostate tumors by controlled release of [D-Trp-6]luteinizing hormone-releasing hormone from injectable microcapsules, Proc. Natl. Acad. Sci. U.S.A. 81:5845–5848.

    Article  PubMed  CAS  Google Scholar 

  • Reichlin, S., 1983, Somatostatin, N. Engl. J. Med. 309:1495–1501, 1556–1563.

    Article  PubMed  CAS  Google Scholar 

  • Rivier, J., Brown, M., and Vale, W., 1975, D-Trp-8-Somatostatin: An analog of somatostatin more potent than the native molecule, Biochem. Biophys. Res. Commun. 65:746–751.

    Article  PubMed  CAS  Google Scholar 

  • Rivier, J., Brown, M., Rivier, C., Ling, N., and Vale, W., 1977, Hypothalamic hypophysiotropic hormones. Review on the design of synthetic analogs, in: Peptides 1976 (A. Loffet, ed.), l’Université de Bruxelles, Brussels, pp. 427–449.

    Google Scholar 

  • Rose, D. P., Gottardis, M., and Noonan, J. J., 1983, Rat mammary carcinoma regressions during suppression of serum growth hormone and prolactin, Anticancer Res. 3:323–326.

    PubMed  CAS  Google Scholar 

  • Salomon, D. S., Paglia, L. M., and Verbruggen, L., 1979, Hormone-dependent growth of a rat chondrosarcoma in vivo, Cancer Res. 39:4387–4395.

    PubMed  CAS  Google Scholar 

  • Schally, A. V., Coy, D. H., and Meyers, C. A., 1978, Hypothalamic regulatory hormones, Annu. Rev. Biochem. 47:89–128.

    Article  PubMed  CAS  Google Scholar 

  • Schally, A. V., Comaru-Schally, A. M., and Redding, T. W., 1984a, Antitumor effects of analogs of hypothalamic hormones in endocrine-dependent cancers, Proc. Soc. Exp. Biol. Med. 175:259–281.

    PubMed  CAS  Google Scholar 

  • Schally, A. V., Coy, D. H., Murphy, W. A., Redding, T. W., Comaru-Schally, A. M., Hall, R., Rodriguez-Arnao, M. D., Gomez-Pan, A., Gonzalez-Barcena, D., Millar, R. P., and Konturek, S., 1984b, Physiological and clinical studies with somatostatin analogs and pro-somatostatin, in: 2nd International Symposium on Somatostatin, Athens (Greece) (S. Raptis, J. Rosenthal, and J. E. Gerich, eds.), Attempto Verlag, Tübingen, pp. 188–196.

    Google Scholar 

  • Schally, A. V., Redding, T. W., and Comaru-Schally, A. M., 1984c, Potential use of analogs of luteinizing hormone-releasing hormones in the treatment of hormone-sensitive neoplasms, Cancer Treat. Rep. 68:281–289.

    PubMed  CAS  Google Scholar 

  • Snodgrass, P. J., 1977, Section 7, Disorders of the pancreas, in: Harrison’s Principles of Internal Medicine, 8th ed. (G. W. Thorn, R. D. Adams, E. Braunwald, K. J. Isselbacher, and R. G. Petersdorf, eds.), McGraw-Hill, New York, pp. 1643–1645.

    Google Scholar 

  • Szilagyi, G., Irsy, G., Goth, M., Szabolcs, I., Coy, D. H., Comaru-Schally, A. M., and Schally, A. V., 1984, Effect of a somatostatin analogue on trophic hormone levels in acromegalic patients with elevated hGH after adrenomectomy and treatment with bromocriptine, Exp. Clin. Endocrinol. 84:190–196.

    Article  PubMed  CAS  Google Scholar 

  • Torres-Aleman, I., Redding, T. W., and Schally, A. V., 1985, Inhibition of growth of a prolactin and growth hormone-secreting pituitary tumor in rats by D-tryptophan-6 analog of luteinizing hormone-releasing hormone, Proc. Natl. Acad. Sci. U.S.A. 82:1252–1256.

    Article  PubMed  CAS  Google Scholar 

  • Townsend, C. M., Jr., Franklin, R. B., Watson, L. C., Glass, E. J., and Thompson, J. C., 1981, Stimulation of pancreatic cancer growth by caerulein and secretin, Surg. Forum 34:228–229.

    Google Scholar 

  • Usadel, K. H., Leuschner, U., and Uberla, K. K., 1980, Treatment of acute pancreatitis with somatostatin: A multicenter double-blind trial, N. Engl. J. Med. 303:999–1000.

    Article  PubMed  CAS  Google Scholar 

  • Usadel, K. H., Leuschner, U., and Uberla, K. K., 1984, Report on a randomized double-blind European multicenter study on the use of somatostatin in acute pancreatitis (APTS) in: 2nd International Symposium on Somatostatin, Athens (Greece) (S. Raptis, J. Rosenthal, and J. E. Gerich, eds.), Attempto Verlag, Tübingen, pp. 236–243.

    Google Scholar 

  • Veber, D. F., Holly, F. W., Nutt, R. F., Bergstrand, S. J., Brady, St. F., Hirschmann, R., Glitzer, M. S., and Saperstein, R., 1979, Highly active cyclic and bicyclic somatostatin analogs of reduced ring size, Nature 280:512–514.

    Article  PubMed  CAS  Google Scholar 

  • Veber, D. F., Freidinger, R. M., Schwenk-Perlow, D., Paleveda, W. J., Jr., Holly, R. W., Strachan, R. G., Nutt, R. F., Arison, B. H., Homnick, C., Randall, W. C., Glitzer, M. S., Saperstein, R., and Hirschmann, R., 1981, A potent cyclic hexapeptide analogue of somatostatin, Nature 292:55–58.

    Article  PubMed  CAS  Google Scholar 

  • Veber, D. F., Saperstein, R., Nutt, R. F., Freidinger, R. M., Brady, S. F., Curley, P., Perlow, D. S., Paleveda, W. J., Colton, C. D., Zacchei, A. G., Tocco, D. J., Hoff, D. R., Vandlen, R. L., Gerich, J. E., Hall, L., Mandarino, L., Cordes, E. H., Anderson, P. S., and Hirschmann, R., 1984, A super active cyclic hexapeptide analog of somatostatin, Life Sci. 34:1371–1378.

    Article  PubMed  CAS  Google Scholar 

  • Von Werder, K., Losa, M., Müller, O. A., Schweiberer, L., Falhbusch, R., and Del Pozo, E., 1984, Treatment of metastasising GRF-producing tumour with a long-acting somatostatin analogue, Lancet 2:282–283.

    Article  Google Scholar 

  • Wajchenberg, B. L., Cesar, F. P., Lerne, C. E., Borghi, V. C., Souza, I. T. T., Neto, D. G., Germek, O. A., Coy, D. H., Comaru-Schally, A. M., and Schally, A. V., 1983, Dissociated effects of somatostatin analogs on arginine-induced insulin, glucagon and growth hormone release in acromegalic patients, Horm. Metab. Res. 15:471–474.

    Article  PubMed  CAS  Google Scholar 

  • Yamamoto, T., Nishida, T., Miyajima, N., Kawai, S., Ooi, T., and Toyoshima, K., 1983, The erbB gene of avian erythroblastosis virus is a member of the sre gene family, Cell 35:71–78.

    Article  PubMed  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

  1. Veterans Administration Medical Center, Tulane University School of Medicine, New Orleans, Louisiana, 70146, USA

    Andrew V. Schally, Ren-Zhi Cai, I. Torres-Aleman, Tommie W. Redding, Balazs Szoke, Dadin Fu, Marion T. Hierowski & John Colaluca

  2. Medical Academy, Krakow, Poland

    Stanislaw Konturek

Authors
  1. Andrew V. Schally
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Ren-Zhi Cai
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. I. Torres-Aleman
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Tommie W. Redding
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. Balazs Szoke
    View author publications

    You can also search for this author in PubMed Google Scholar

  6. Dadin Fu
    View author publications

    You can also search for this author in PubMed Google Scholar

  7. Marion T. Hierowski
    View author publications

    You can also search for this author in PubMed Google Scholar

  8. John Colaluca
    View author publications

    You can also search for this author in PubMed Google Scholar

  9. Stanislaw Konturek
    View author publications

    You can also search for this author in PubMed Google Scholar

Editor information

Editors and Affiliations

  1. The George Washington University School of Medicine and Health Sciences, Washington, D.C., USA

    Terry W. Moody

Rights and permissions

Reprints and permissions

Copyright information

© 1986 Plenum Press, New York

About this chapter

Cite this chapter

Schally, A.V. et al. (1986). Endocrine, Gastrointestinal, and Antitumor Activity of Somatostatin Analogues. In: Moody, T.W. (eds) Neural and Endocrine Peptides and Receptors. GWUMC Department of Biochemistry Annual Spring Symposia. Springer, Boston, MA. https://doi.org/10.1007/978-1-4684-5152-8_7

Download citation

  • DOI: https://doi.org/10.1007/978-1-4684-5152-8_7

  • Publisher Name: Springer, Boston, MA

  • Print ISBN: 978-1-4684-5154-2

  • Online ISBN: 978-1-4684-5152-8

  • eBook Packages: Springer Book Archive

Publish with us

Policies and ethics

Search

Navigation