Bis(Disulfide)-Bridged Somatostatin-14 Analogs and Their [¹¹¹In]In-Radioligands: Synthesis and Preclinical Profile.

ABSTRACT: The overexpression of one or more somatostatin receptors (SST_1-5R) in human tumors has provided an opportunity for diagnosis and therapy with somatostatin-like radionuclide carriers. The application of "pansomatostatin" analogs is expected to broaden the clinical indications and upgrade the diagnostic/therapeutic efficacy of currently applied SST₂R-prefering radioligands. In pursuit of this goal, we now introduce two bicyclic somatostatin-14 (SS14) analogs, AT5S (DOTA-Ala¹-Gly²-c[Cys³-Lys⁴-Asn⁵-c[Cys⁶-Phe⁷-DTrp⁸-Lys⁹-Thr¹⁰-Cys¹¹]-Thr¹²-Ser¹³-Cys¹⁴]) and AT6S (DOTA-Ala¹-Gly²-c[Cys³-Lys

SUBMITTER: Tatsi A 

PROVIDER: S-EPMC10856354 | biostudies-literature | 2024 Feb

REPOSITORIES: biostudies-literature