AUTHOR=Pratesi Alessandro , Ginanneschi Mauro , Lumini Marco , Papini Anna M. , Novellino Ettore , Brancaccio Diego , Carotenuto Alfonso 

TITLE=DOTA-Derivatives of Octreotide Dicarba-Analogs with High Affinity for Somatostatin sst2,5 Receptors

JOURNAL=Frontiers in Chemistry

VOLUME=5

YEAR=2017

URL=https://www.frontiersin.org/journals/chemistry/articles/10.3389/fchem.2017.00008

DOI=10.3389/fchem.2017.00008

ISSN=2296-2646

ABSTRACT=<p><italic>In vivo</italic> somatostatin receptor scintigraphy is a valuable method for the visualization of human endocrine tumors and their metastases. In fact, peptide ligands of somatostatin receptors (sst's) conjugated with chelating agents are in clinical use. We have recently developed octreotide dicarba-analogs, which show interesting binding profiles at sst's. In this context, it was mandatory to explore the possibility that our analogs could maintain their activity also upon conjugation with DOTA. In this paper, we report and discuss the synthesis, binding affinity and conformational preferences of three DOTA-conjugated dicarba-analogs of octreotide. Interestingly, two conjugated analogs exhibited nanomolar affinities on sst<sub>2</sub> and sst<sub>5</sub> somatostatin receptor subtypes.</p>