Design, synthesis, and biological evaluation of somatostatin-based radiopeptides

Ginj, Mihaela; Schmitt, Jörg S; Chen, Jianhua; Waser, Beatrice; Reubi, Jean-Claude; de Jong, Marion; Schulz, Stefan; Maecke, Helmut R (2006). Design, synthesis, and biological evaluation of somatostatin-based radiopeptides. Chemistry & biology, 13(10), pp. 1081-90. San Francisco, Calif.: Current Biology Ltd. 10.1016/j.chembiol.2006.08.012

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The prototypes for tumor targeting with radiolabeled peptides are derivatives of somatostatin. Usually, they primarily have high affinity for somatostatin receptor subtype 2 (sst2), and they have moderate affinity for sst5. We aimed at developing analogs that recognize different somatostatin receptor subtypes for internal radiotherapy in order to extend the present range of accessible tumors. We synthesized DOTA-octapeptides based on octreotide by replacing Phe3 mainly with unnatural amino acids. The affinity profile was determined by using cell lines transfected with sst1-5. Internalization was determined by using AR42J, HEK-sst3, and HEK-sst5 cell lines, and biodistribution was studied in rat tumor models. Two of the derivatives thus obtained showed an improved binding affinity profile, enhanced internalization into cells expressing sst2 and sst3, respectively, and better tumor:kidney ratios in animals.

Item Type:

Journal Article (Original Article)


04 Faculty of Medicine > Service Sector > Institute of Pathology

UniBE Contributor:

Waser, Beatrice and Reubi-Kattenbusch, Jean-Claude


500 Science > 570 Life sciences; biology
600 Technology > 610 Medicine & health






Current Biology Ltd.




Factscience Import

Date Deposited:

04 Oct 2013 14:48

Last Modified:

17 Oct 2019 10:14

Publisher DOI:


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Web of Science ID:


URI: (FactScience: 3549)

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