Evaluation of Actinium-225 Labeled Minigastrin Analogue [²²⁵Ac]Ac-DOTA-PP-F11N for Targeted Alpha Particle Therapy.

ABSTRACT: The overexpression of cholecystokinin B receptor (CCKBR) in human cancers led to the development of radiolabeled minigastrin analogues for targeted radionuclide therapy, which aims to deliver cytotoxic radiation specifically to cancer cells. Alpha emitters (e.g., actinium-225) possess high potency in cancer cell-killing and hold promise for the treatment of malignant tumors. In these preclinical studies, we developed and evaluated CCKBR-targeted alpha particle therapy. The cellular uptake and cytotoxic effect of actinium-225 labeled and HPLC-purified minigastrin analogue [²²⁵Ac]Ac-PP-F11N were characterized in the human squamous cancer A431 cells transfected with CCKBR. Nude mice bearing A431/CCKBR tumors were used for biodistribution and therapy studies followed by histological

SUBMITTER: Qin Y 

PROVIDER: S-EPMC7696055 | biostudies-literature | 2020 Nov

REPOSITORIES: biostudies-literature