H₂BZmacropa-NCS: A Bifunctional Chelator for Actinium-225 Targeted Alpha Therapy.

ABSTRACT: Actinium-225 (²²⁵Ac) is one of the most promising radionuclides for targeted alpha therapy (TAT). With a half-life of 9.92 days and a decay chain that emits four high-energy α particles, ²²⁵Ac is well-suited for TAT when conjugated to macromolecular targeting vectors that exhibit extended in vivo circulation times. The implementation of ²²⁵Ac in these targeted constructs, however, requires a suitable chelator that can bind and retain this radionuclide in vivo. Previous work has demonstrated the suitability of a diaza-18-crown-6 macrocyclic chelator H₂macropa for this application. Building upon these prior efforts, in this study, two rigid variants of H₂macropa, which contain either one (H₂BZmacropa) or two (H₂BZ

SUBMITTER: Kadassery KJ 

PROVIDER: S-EPMC9362842 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature