The putative somatostatin antagonist,cyclo-(7-aminoheptanoyl-Phe-D-Trp-Lys-Thr[BZL]), may act as potent antiproliferative agonist |
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Authors: | Stirnweis Jörg Boehmer Frank-D Liebmann Claus |
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Institution: | Biological and Pharmaceutical Faculty, Institute of Biochemistry and Biophysics, Friedrich-Schiller-University Jena, Philosophenweg 12, D-07743 Jena, Germany. |
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Abstract: | The cyclic somatostatin (SST) analogue, cyclo-(7-aminoheptanoyl-Phe-D-Trp-Lys-ThrBZL]) (cSSTA), has been widely used as somatostatin antagonist. In the human neuroblastoma cell line SH-SY5Y the cyclopeptide acts as a somatostatin receptor agonist. Similar to SST, cSSTA inhibits cell proliferation, activates the protein tyrosine phosphatase SHP-2, and stimulates the activity of mitogen-activated protein kinase. These results suggest that in SH-SY5Y neuroblastoma cells somatostatin receptors may exist which exhibit altered antagonist binding properties. |
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