Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.

@article{Cescato2008DesignAI,
  title={Design and in vitro characterization of highly sst2-selective somatostatin antagonists suitable for radiotargeting.},
  author={Renzo Cescato and Judith Erchegyi and Beatrice Waser and V{\'e}ronique Piccand and Helmut R. Maecke and Jean E F Rivier and Jean Claude Reubi},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 13},
  pages={4030-7}
}
Radiolabeled sst 2 and sst 3 antagonists are better candidates for tumor targeting than agonists with comparable binding characteristics (Ginj, M.; Zhang, H.; Waser, B.; Cescato, R.; Wild, D.; Erchegyi, J.; Rivier, J.; Mäcke, H. R.; Reubi, J. C. Proc. Natl. Acad. Sci. U.S.A. 2006, 103, 16436-16441.). Because most of the neuroendocrine tumors express sst 2, we used the known antagonists acetyl- pNO 2Phe (2)- c[ dCys (3)-Tyr (7)- dTrp (8)-Lys (9)-Thr (10)-Cys (14)]- dTyr (15)-NH 2 ( 1) (Bass, R… CONTINUE READING

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