⁶⁸Ga/¹⁶¹Tb-CP2 as a Paired Radiopharmaceutical Targeting KDM4A and the Preliminary Verification in NCI-H2228 Xenografts Model.

ABSTRACT: Objective: To address the unmet clinical need for Lysine (K)-specific demethylase 4A (KDM4A)-targeted therapies in nonsmall cell lung cancer (NSCLC), we developed a novel theranostic pair, ⁶⁸Ga/¹⁶¹Tb-CP2, leveraging the epigenetic regulator KDM4A and terbium-161's high linear energy transfer (LET) Auger electrons for precision therapy. Methods: The radiopharmaceutical was synthesized via a one-step chelation protocol. Radiochemical purity and stability were validated by radio-HPLC and radio-TLC. In vitro studies evaluated the nuclear targeting ability of ¹⁶¹Tb-CP2 by cellular uptake and cellular internalization, and quantified tumor cell proliferation by carboxyfluorescein diacetate, succinimidyl ester immunofluorescence and flow cytome

SUBMITTER: Zhang Y 

PROVIDER: S-EPMC12242621 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature