⁶⁸Ga, ⁴⁴Sc and ¹⁷⁷Lu-labeled AAZTA⁵-PSMA-617: synthesis, radiolabeling, stability and cell binding compared to DOTA-PSMA-617 analogues.

ABSTRACT:

Background

The AAZTA chelator and in particular its bifunctional derivative AAZTA⁵ was recently investigated to demonstrate unique capabilities to complex diagnostic and therapeutic trivalent radiometals under mild conditions. This study presents a comparison of ⁶⁸Ga, ⁴⁴Sc and ¹⁷⁷Lu-labeled AAZTA⁵-PSMA-617 with DOTA-PSMA-617 analogues. We evaluated the radiolabeling characteristics, in vitro stability of the radiolabeled compounds and evaluated their binding affinity and internalization behavior on LNCaP tumor cells in direct comparison to the radiolabeled DOTA-conjugated PSMA-617 analogs.

Results

AAZTA⁵ was synthesized in a five-step synthesis and coupled to the PSMA-617 backbone on solid phase. Radiochemical

SUBMITTER: Sinnes JP 

PROVIDER: S-EPMC7691401 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature