Controlled Dual Activation of Rhenium(I) Photosensitizers and Profluorophores/Prodrugs via a Dissociative Bioorthogonal Tetrazine-Isonitrile Reaction.

ABSTRACT: Strategies for prodrug activation have been developed to enhance treatment efficacy, with bioorthogonal dissociation reactions emerging as a promising approach due to their remarkable specificity. In this work, we designed three rhenium(I) polypyridine complexes featuring a tetrazylmethyl (TzMe) group capable of bioorthogonal activation by 3-isocyanopropyl (ICPr) or 3-isocyanopropyl-1-carbamoyl (ICPrc) derivatives. This design serves as a dual-release platform, which liberates rhenium(I) 3-hydroxypyridine complexes and functional payloads from rhenium(I) TzMe complexes and ICPr/ICPrc-caged compounds, respectively. Upon incubation with an ICPrc derivative, the TzMe complexes exhibited strong emission in acidic buffers, attributed to the predominant existence of the resulting rhenium(I) 3-hy

SUBMITTER: Mak EC 

PROVIDER: S-EPMC12684313 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature