This is a preview of subscription content, log in via an institution to check access.
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
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., 1979, The effect of somatostatin analogs on secretion of growth, pancreatic, and gastrointestinal hormones in man, J. Clin. Endocrinol. Metab. 53:675–681.
Anthony, L., Johnson, D., Hande, K., Shaff, M., Winn, S., Krozely, M., and Gates, J., 1993, Somatostatin analogueue phase I trials in neuroendocrine neoplasms, Acta Oncol. 32:217–223.
Arnold, R., Neuhaus, C., Benning, R., Schwerk, W. B., Trautmann, M. E., Joseph, K., and Bruns, C., 1993, Somatostatin analogue sandostatin and inhibition of tumor growth in patients with metastatic endocrine gastroenteropancreatic tumors, World J. Surg. 17:511–519.
Arnold, R., Trautmann, M. E., Creutzfeldt, W., Benning, R., Benning, M., Neuhaus, C., Juergensen, R., Stein, K., Schaefer, H., Bruns, C., and Dennler, H. J., 1996, Somatostatin analogueue octreotide and inhibition of tumour growth in metastatic endocrine gastroenteropancreatic tumours, Gut 38:430–438.
Bakker, W. H., Alberts, R., Bruns, C., Breeman, W. A. P., Hofland, L. J., Marbach, P., Pless, J., Pralet, D., Stolz, B., Koper, J. W., Lamberts, S. W. J., Visser, T. J., and Krenning, E. P., 1991, In-DTPA-DPhe1-octreotide a potential radiopharmaceutical for imaging of somatostatin receptor-positive tumors: Synthesis, radiolabelling and in vitro validation, Life Sci. 49:1583–1591.
Barrie, R., Woltering, E. A., Hajarizadeh, H., Mueller, C., Ure, T., and Fletcher, W. S., 1993, Inhibition of angiogenesis by somatostatin and somatostatin-like compounds is structurally dependent, J. Surg. Res. 55:446–450.
Bauer, W., Briner, U., Doepfner, W., Haller, R., Huguenin, R., Marbach, P., Petcher, T. J., and Pless, J., 1982a, SMS 201–995: A very potent and selective octapeptide analogue of somatostatin with prolonged action, Life Sci. 31:1133–1140.
Bauer, W., Briner, U., Doepfner, W., Haller, R., Huguenin, R., Marbach, P., Petcher, T. J., and Pless, J., 1982b, Structure-activity relationships of highly potent and specific octapeptide analogues of somatostatin, in: Proceedings of the European Peptide Symposium, Prague (K. Blaha and P. Malon, eds.), pp. 583–588, de Gruyter, Berlin.
Bergmann, U., Yokoyama, M., Berger, H. G., and Korc, M., 1996, Insulin-like growth factor-II is expressed in human islet cells and is mitogenic in pancreatic cancer cells, Proc. Am. Assoc. Cancer Res. 37:1504A.
Bloom, S. R. (ed.), 1990, Somatostatin analogueues-peptide therapy in action: Gastro-enteropancreatic tumors, Digestion 45(Suppl. 1):1–43.
Bodmer, D., Kissel, T., and Traechslin, E., 1992, Factors influencing the release of peptides and proteins from biodegradable parenteral depot systems, J. Control. Rel. 21:129–138.
Bodmer, D., Gengenbacher, T., and Esparza, I., 1994, Stabilization of pharmacologically active compounds in sustained release compositions, European Patent EP 0 626 170A2.
Brazeau, P., Vale, W., Burgus, R., Ling, N., Butcher, M., Rivier, J., and Guillemin, R., 1973, Hypothalamic polypeptide that inhibits the secretion of immunoreactive pituitary growth hormone, Science 179:77–79.
Bruns, C., Stolz, B., Albert, R., Marbach, P., and Pless, J., 1993, OctreoScan® 111 for imaging of a somatostatin receptor-positive islet cell tumor in rat, Harm. Metab. Res. 27(Suppl.):5–11.
Bruns, C., Weckbecker, G., Raulf, F., Kaupmann, K., Schoeffter, P., Hoyer, D., and Lübbert, H., 1994, Molecular pharmacology of somatostatin-receptor subtypes, Ann. N. Y. Acad. Sci. 733:138–146.
Bruns, C., Weckbecker, G., Raulf, F., Lübbert, H., and Hoyer, D., 1995, Characterization of somatostatin receptor subtypes, Ciba Found. Symp. 190:89–101.
Bruns, C., Raulf, F., Hoyer, D., Schloos, J., Lübbert, H., and Weckbecker, G., 1996, Binding properties of somatostatin receptor subtypes, Metabolism 45(Suppl. 1):7–20.
Buechler, M., Sulkowski, U., Pederzoli, P., Arnold, R., Dinse, P., Mietlowski, W., and Israel, R., 1994, A phase II study of octreotide (SMS) in advanced pancreatic cancer, Proc. Am. Soc. Clin. Oncol. 13:A642.
Buscail, L., Delesque, N., Estève, J.-P., Saint Laurent, N., Prats, H., Clerc, P., Robberecht, P., Bell, G. I., Liebow, C., Schally, A. V., Vaysse, N., and Susini, C., 1994, Stimulation of tyrosine phosphatase and inhibition of cell proliferation by somatostatin analogueues: Mediation by human somatostatin receptor subtypes SSTR1 and SSTR2, Proc. Natl. Acad. Sci. USA 91:2315–2319.
Colletti, R. B., Roberts, J. D., Devlin, J. T., and Copeland, K. C., 1989, Effect of tamoxifen on plasma insulin-like growth factor I in patients with breast cancer, Cancer Res. 49:1882–1884.
Danesi, R., and Del Tacca, M., 1996, Effects of octreotide on angiogenesis, in: Octreotide: From Basic Science to Clinical Medicine (C. Scarpignato, ed.), pp. 234–245, Karger, Basel.
De Vries, E. G., Kema, I. P., Slooff, M. J., Verschueren, R. C., Kleibeuker, J. H., Mulder, N. H., Sleijfer, D. T., and Willemse, P. H., 1993, Recent developments in diagnosis and treatment of metastatic carcinoid tumours, Scand. J. Gastroenterol. Suppl. 200:87–93.
Di Bartolomeo, M., Bajetta, E., Buzzoni, R., Mariani, L., Carnaghi, C., Somma, L., Zilembo, N., and di Leo, A., 1996, Clinical efficacy of octreotide in the treatment of metastatic neuroendocrine tumors, Cancer 77:402–408.
Ebert, M., Friess, H., Beger, H. G., and Buchler, M. W., 1994, Role of octreotide in the treatment of pancreatic cancer, Digestion 55(Suppl. 1):48–51.
Farthing, M. J. G. (ed.), 1990, Somatostatin analogueues-peptide therapy in action: Perspectives in gastroenterology, Digestion 45(Suppl. l):45–87.
Flueckiger, E., Richardson, B., Donatsch, P., and Enz, A., 1983, Neuroendocrine aspects of the aging rat, in: Aging Brain and Ergot Alkaloids (A. Agnoli, ed.), pp. 61–71, Raven Press, New York.
Grass, P., Marbach, P., Bruns, C., and Lancranjan, I., 1996, Sandostatin LAR (microencapsulated octreotide acetate) in acromegaly: Pharmacokinetic and pharmacodynamic relationships, Metabolism 45(Suppl. 2):27–30.
Grasso, P., 1976, Review of tests for carcinogenicity and their significance to man, Clin. Toxicol. 9:745–760.
Guillemin, R., 1992, Somatostatin: The early days, Metabolism 41(Suppl.2):2–4.
Harris, A. G., Kokoris, S. P., and Ezzat, S., 1995, Continuous versus intermittent subcutaneous infusion of octreotide in the treatment of acromegaly, J. Clin. Pharmacol. 35:59–71.
Huynh, H. T., and Pollak, M. N., 1994, Enhancement of tamoxifen-induced suppression of insulin-like growth factor I gene expression and serum level by somatostatin analogue, Biochem. Biophys. Res. Commun. 203:253–259.
Johnson, L. R., 1981, Effects of gastrointestinal hormones on pancreatic growth, Cancer 47:1640–1645.
Kaal, A., Frystyk, J., Skjaerbaek, C., Nielsen, S., Jorgensen, J. O. L., Bruns, C., Marbach, P., Lancranjan, I., Weeke, J., and Orskov, H., 1995, Effects of intramuscular microsphere-encapsulated octreotide on serum growth hormone, insulin-like growth factors (IGFs), free IGFs, and IGF-binding proteins in acromegalic patients, Metabolism 44(Suppl. 1):6–14.
Kaupmann, K., Bruns, C., Raulf, F., Weber, H. P., Mattes, H., and Lübbert, 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., and Lübbert, H., 1992, Expression cloning of a rat brain somatostatin receptor cDNA, Proc. Natl. Acad. Sci. USA 89:4618–4622.
Krejs, G. J. (ed.), 1987, Gastrointestinal endocrine tumors: Diagnosis and management; role of somatostatin analogue SMS 201–995, Am. J. Med. 83(5B):1–99.
Krenning, E. P., Bakker, W. H., Breeman, W. A. P., Koper, J. W., Kooij, P. P. M., Ausema, L., Lameris, J. S., Reubi, J. C., and Lamberts, S. W. J., 1989, Localization of endocrine related tumors with radioiodinated analogueue of somatostatin, Lancet 1:242–245.
Krenning, E. P., Kwekkeboom, D. J., Bakker, W. H., Breeman, W. A. P., Kooij, P. P. M., Oei, H. Y., Van Hagen, P. M., Postema, P. T. E., De Jong, M., Reubi, J. C., Visser, T. J., Reijs, A. E. M., Hofland, L. J., Koper, J. W., and Lamberts, S. W. J., 1993, Somatostatin receptor scintigraphy with [111In-DTPA-D-Phe1] and [123I-Tyr3]-octreotide. The Rotterdam experience with more than 1000 patients, Eur. J. Nucl. Med. 20:283–292.
Krenning, E. P., Kwekkeboom, D. J., Pauwels, S., Kvols, L. K., and Reubi, J. C., 1995, Somatostatin receptor scintigraphy, in: Nuclear Medicine Annual (L. M. Freeman, ed.), pp. 1–50, Raven Press, New York.
Lamberts, S. W. J., Krenning, E. P., and Reubi, J. C., 1991, The role of somatostatin and its analogues in the diagnosis and treatment of tumors, Endocr. Rev. 12:450–482.
Lancranjan, I., Bruns, C. H., Grass, P., Jaquet, P., Jervell, J., Kendall-Taylor, P., Lamberts, S. W. J., Marbach, P., Orskov, H., Pagani, G., Sheppard, M., and Simionescu, L., 1996, Sandostatin LAR: A promising therapeutic tool in the management of acromegalic patients, Metabolism 45(Suppl. 1):67–71.
Lemaire, M., Azria, M., Dannecker, R., Marbach, P., Schweitzer, A., and Maurer, G., 1989, Disposition of Sandostatin, a new synthetic somatostatin analogueue, in rats, Drug Metab. Dispos. 17:699–705.
Marbach, P., Goetz, U., Veteau, J. P., and Wagner, H., 1978, RIA analysis by means of non-linearized response functions, in: Radioimmunoassay and Related Procedures in Medicine, pp. 383–397, IAEA, Vienna.
Marbach, P., Neufeld, M., and Pless, J., 1985, Clinical applications of somatostatin analogues, Adv. Exp. Med. Biol. 188:339–353.
Marbach, P., Andres, H., Azria, M., Bauer, W., Briner, U., Buchheit, K. H., Doepfner, W., Lemaire, M., Petcher, T. J., Pless, J., and Reubi, J. C., 1988, Chemical structure, pharmacodynamic profile and pharmacokinetics of SMS 201-995 (Sandostatin), in: Sandostatin in the Treatment of Acromegaly (S. W. J. Lamberts, ed.), pp. 53–60, Springer-Verlag, Berlin.
Marbach, P., Briner, U., Lemaire, M., Schweitzer, A., and Terasaki, T., 1992, From somatostatin to Sandostatin: Pharmacodynamics and pharmacokinetics, Metabolism 41(Suppl. 2): 1–10.
Martin, J. L., Chesselet, M. F., Raynor, K., Gonzales, C., and Reisine, T., 1991, Differential distribution of somatostatin receptor subtypes in rat brain revealed by newly developed somatostatin ana-logues, Neuroscience 41:581–593.
Mergler, M., Hellstern, H., Wirth, W., Langer, W., Gysi, P., and Prikoszowich, W., 1991, A new acid-labile linker for the solid-phase synthesis of peptides with C-terminal threoninol, Poster presented at the Twelfth American Peptide Symposium, Boston.
Myai, Y., Shiu, R. P. C., Bhaumick, B., and Bala, M., 1984, Receptor binding and growth-promoting activity of insulin-like growth factors in human breast cancer cells (T-47D) in culture, Cancer Res. 44:5486–5490.
O’Dorisio, T. M. (ed.), 1986, Neuroendocrine disorders of the gastroenteropancreatic system; clinical applications of the somatostatin analogue SMS 201-995, Am. J. Med. 81(6B): 1–101.
Panetta, R., Greenwood, M. T., Warszynska, A., Demchyshyn, L. L., Day, R., Niznik, H. B., Srikant, C. B., and 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.
Patel, Y. C., Greenwood, M. T., Panetta, R., Demchyshyn, L., Niznik, H., and Srikant, C. B., 1995, The somatostatin receptor family, Life Sci. 5:1249–1265.
Peyrat, J. P., Bonneterre, J., Vennin, P. H., Jammes, H., Beuscart, R., Hecquet, B., Djiane, J., Lefebvre, J., and Demaille, A., 1990, Insulin-like growth factor 1 receptors (IGF1-R) and IGF1 in human breast tumors, J. Steroid Biochem. Mol. Biol. 37:823–827.
Pohl, E., Heine, A., Sheldrick, G., Dauter, Z., Wilson, K., Kallen, J., Huber, W., and Pfaeffli, P., 1995, Structure of octreotide, Acta Crystallogr. D51:48–59.
Pollak, M. N., Ingle, J. N., Susman, V. J., Kugler, J. W., Nickerson, T., and Deroo, B., 1996, Enhancement of tamoxifen-induced suppression of serum IGF-1 levels in metastatic breast cancer patients by coadministration of somatostatin analogueue octreotide, Proc. Am. Assoc. Cancer Res. 37:1167A.
Pratt, W. B., Ruddon, R. W., Ensminger, W. D., and Maybaum, J., 1994, The Anticancer Drugs, 2nd ed., Oxford University Press, London.
Raulf, F., Pérez, J., Hoyer, D., and Brims, C., 1994, Differential expression of five somatostatin receptor subtypes, SSTR1-5, in the CNS and peripheral tissue, Digestion 55(Suppl. 3):46–53.
Reichlin, S., 1983, Somatostatin, N. Engl. J. Med. 309:1495–1501.
Reisine, T., and Bell, G. I., 1995, Molecular biology of somatostatin receptors, Endocr. Rev. 16:427–442.
Reubi, J. C., 1984, Evidence for two somatostatin-14 receptor subtypes in rat brain cortex, Neurosci. Lett. 49:259–263.
Reubi, J. C., Krenning, E., Lamberts, S. W. J., and Kvols, L., 1992, In vitro detection of somatostatin receptors in human tumors, Metabolism 41:104–110.
Reubi, J. C., Horisberger, U., and Laissue, J., 1994, High density of somatostatin receptors in veins surounding human cancer tissue: Role in tumor-host interaction? Int. J. Cancer 56:681–688.
Rivier, J., Brown, M., and Vale, W., 1975, d-Trp8-somatostatin: An analogue of somatostatin more potent than the native molecule, Biochem. Biophys. Res. Commun. 65:746–751.
Rohrer, L., Raulf, F., Bruns, C., Buettner, R., Hofstaedter, F., and Schüle, R., 1993, Cloning and chaacterization of a fourth human somatostatin receptor, Proc. Natl. Acad. Sci. USA 90:4196–4200.
Schirmer, W. J., O’Dorisio, T. M., Sc hirmer, T. P., Mojzisik, C. M., Hinkle, G. H., and Martin, E. W., 1993, Intraoperative localization of neuroendocrine tumors with 125I-Tyr3-octreotide and a hand held gamma detecting probe, Surgery 114:745–752.
Serri, O., Brazeau, P., Kachra, Z., and Posner, B., 1992, Octreotide inhibits insulin-like growth factor-I hepatic gene expression in the hypophysectomized rat: Evidence for a direct and indirect mechanism of action, Endocrinology 130:1816–1821.
Somlo, G., Vogel, C., Flamm Honig, S., Linnartz, R., and Israel, R., 1993, A phase I study of octreotide (SMS) in patients with advanced breast cancer, Proc. Am. Soc. Clin. Oncol. 12:A172.
Srikant, C. B., and Shen, S. H., 1996, Octapeptide somatostatin analogue SMS 201-995 induces translocation of intracellular PTP1C to membranes in MCF-7 human breast adenocarcinoma cells, Endocrinology 137:3461–3468.
Theiss, J. C., 1982, Utility of injection site tumorigenicity in assessing the carcinogenicity risk of chemicals to man, Regul. Toxicol. Pharmacol. 2:213–222.
Vale, W., Rivier, J., Ling, N., and Brown, M., 1978, Biological and immunologic activities and application of SRIF analogues, Metabolism 27(Suppl. 1):1391–1401.
Veber, D., Holly, F. W., Paleweda, W. J., Nutt, R. F., Bergstrand, S. J., Torchiana, M., Glitzer, M. S., Saperstein, R., and Hirschmann, R., 1978, Conformationally restricted bicyclic analogues of somatostatin, Proc. Natl. Acad. Sci. USA 75:2636–2640.
Veber, D., Saperstein, R., Nutt, R. F., Freidinger, R. M., Brady, S. F., Curley, P., Perlow, D. S., Paleweda, W. J., Dylion Colton, C., Zacchei, A. G., Tocco, D. J., Hoff, D. R., Vandlen, R. L., Gerich, J. E., Hall, L., Mandarine, L., Cordes, E. H., Anderson, P. S., and Hirschmann, R., 1984, A super active cyclic hexapeptide analogue of somatostatin, Life Sci. 34:1371–1378.
Weckbecker, G., 1991, Biochemical pharmacology and analysis of fluoropyrimidines alone and in combination with modulators, Pharmacol. Ther. 50:367–424.
Weckbecker, G., Liu, R., Tolcsvai, L., and Bruns, C., 1992a, Antiproliferative effects of the somatostatin analogueue octreotide (SMS 201-995) on ZR-75-1 human breast cancer cells in vivo and in vitro, Cancer Res. 52:4973–978.
Weckbecker, G., Tolcsvai, L., Liu, R., and Bruns, C., 1992b, Preclinical studies on the anticancer activity of the somatostatin analogueue octreotide, SMS 201-995, Metabolism 41:99–103.
Weckbecker, G., Raulf, F., Stolz, B., and Bruns, C., 1993, Somatostatin analogues for diagnosis and treatment of cancer, Pharmacol. Ther. 60:245–264.
Weckbecker, G., Tolcsvai, L., Stolz, B., Pollak, M., and Bruns, C., 1994, Somatostatin analogue octreotide enhances the antineoplastic effects of tamoxifen and ovariectomy on 7,12-dimethylbenz(a)anthracene-induced rat mammary carcinomas, Cancer Res. 54:6334–6337.
Weckbecker, G., Raulf, F., Tolcsvai, L., and Bruns, C., 1996, Potentiation of the antiproliferative effects of anticancer drugs by octreotide in vitro and in vivo, Digestion 57:22–28.
Yamada, Y., Post, S. R., Wang, K., Tager, H. S., Bell, G. I., and 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. USA 89:251–255.
Yamada, Y., Reisine, T., Law, S. F., Ihara, Y., Kubota, A., Kagimoto, S., Seino, M., Seino, Y., Bell, G. I., and 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.
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 2002 Kluwer Academic Publishers
About this chapter
Cite this chapter
Marbach, P. et al. (2002). Discovery and Development of Somatostatin Agonists. In: Borchardt, R.T., Freidinger, R.M., Sawyer, T.K., Smith, P.L. (eds) Integration of Pharmaceutical Discovery and Development. Pharmaceutical Biotechnology, vol 11. Springer, Boston, MA. https://doi.org/10.1007/0-306-47384-4_9
Download citation
DOI: https://doi.org/10.1007/0-306-47384-4_9
Publisher Name: Springer, Boston, MA
Print ISBN: 978-0-306-45743-2
Online ISBN: 978-0-306-47384-5
eBook Packages: Springer Book Archive