Accessing Self-Illuminated, Luminescent Lanthanide Probes by Enzymatic Radiophosphorylation.

ABSTRACT: Here, we describe the design and synthesis of Tb³⁺ and Eu³⁺ complexes appended to a kinase-substrate peptide, enabling the incorporation of ³²P, a potent Cerenkov emitter, by enzymatic phosphorylation to form a metallacyclized peptide structure with a dual turn-on effect. The construct was optimized to accommodate one inner-sphere donor, identifying 8-coordinate, tricazamacrocycles as ideal to produce a selective turn-on response by displacement of an inner-sphere water molecule by phosphate. The optimization of the peptide sequence allowed for the maximization of PKCα kinase-induced luminescence enhancement. The resulting peptide gave a selective turn-on response of 15% upon displacement of inner-sphere waters. Sequence elongation or rigidification results

SUBMITTER: Sands GG 

PROVIDER: S-EPMC12754790 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature