%0 Journal Article
%A Sinnes, Jean-Philippe
%A Bauder-Wüst, Ulrike
%A Schäfer, Martin
%A Moon, Euy Sung
%A Kopka, Klaus
%A Rösch, Frank
%T 68Ga, 44Sc and 177Lu-labeled AAZTA5-PSMA-617: synthesis, radiolabeling, stability and cell binding compared to DOTA-PSMA-617 analogues.
%J EJNMMI radiopharmacy and chemistry
%V 5
%N 1
%@ 2365-421X
%C [Heidelberg]
%I SpringerOpen
%M DKFZ-2020-02582
%P 28
%D 2020
%X 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.AAZTA5 was synthesized in a five-step synthesis and coupled to the PSMA-617 backbone on solid phase. Radiochemical evaluation of AAZTA5-PSMA-617 with 68Ga, 44Sc and 177Lu achieved quantitative radiolabeling of > 99
%F PUB:(DE-HGF)16
%9 Journal Article
%$ pmid:33242189
%R 10.1186/s41181-020-00107-8
%U https://inrepo02.dkfz.de/record/166043