Novel Auger-Electron-Emitting ¹⁹¹Pt-Labeled Pyrrole-Imidazole Polyamide Targeting MYCN Increases Cytotoxicity and Cytosolic dsDNA Granules in MYCN-Amplified Neuroblastoma.

ABSTRACT: Auger electrons can cause nanoscale physiochemical damage to specific DNA sites that play a key role in cancer cell survival. Radio-Pt is a promising Auger-electron source for damaging DNA efficiently because of its ability to bind to DNA. Considering that the cancer genome is maintained under abnormal gene amplification and expression, here, we developed a novel ¹⁹¹Pt-labeled agent based on pyrrole-imidazole polyamide (PIP), targeting the oncogene MYCN amplified in human neuroblastoma, and investigated its targeting ability and damaging effects. A conjugate of MYCN-targeting PIP and Cys-(Arg)₃-coumarin was labeled with ¹⁹¹Pt via Cys (¹⁹¹Pt-MYCN-PIP) with a radiochemical purity of >99%. The binding potential of ¹⁹¹Pt-MYCN-PIP was evalu

SUBMITTER: Obata H 

PROVIDER: S-EPMC10675227 | biostudies-literature | 2023 Oct

REPOSITORIES: biostudies-literature