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@ARTICLE{Peng:303087,
author = {W. Peng and T. Zhou and L. Hu and V. Vankann and T.
Bohn$^*$ and T. Bopp$^*$ and S. L. Kuan and T. Weil},
title = {{A}utonomous {A}ctivation of a {G}ated {C}hemiluminescent
{P}hotosensitizer {E}nables {T}argeted {P}hotodynamic
{T}herapy in {T}umor {C}ells.},
journal = {Journal of the American Chemical Society},
volume = {147},
number = {31},
issn = {0002-7863},
address = {Washington, DC},
publisher = {ACS Publications},
reportid = {DKFZ-2025-01512},
pages = {27822-27834},
year = {2025},
note = {2025 Aug 6;147(31):27822-27834},
abstract = {Chemiluminescence-based photodynamic therapy (CLPDT) offers
a promising solution to the light penetration limits of
traditional PDT. However, it lacks spatiotemporal control.
Intracellularly activated, self-luminescent PDT agents via a
molecular logic gate switch may address this key limitation.
We report the synthesis of the self-activating,
chemiluminescent photosensitizer (PS) that enables tumor
microenvironment-controlled PDT applications. This system
integrates a dioxetane-based (Diox) chemiluminescent
scaffold with a ruthenium-based (Ru) PS through an oxidation
and pH-sensitive linker to enable an AND-gated activation
mechanism. The Diox@Ru conjugate is selectively activated by
elevated intracellular reactive oxygen species (ROS),
characteristic of aggressive cancer phenotypes arising from
altered cell metabolism. Upon exposure to ROS (in this case,
hydrogen peroxide), the boronic acid ester protecting group
of the dioxetane is cleaved, initiating localized
chemiluminescence that directly excites the Ru(II) PS to
generate cytotoxic singlet oxygen (1O2). Importantly,
Diox@Ru remains inert under physiological conditions
(neutral pH, low ROS) as well as in the acidic, ROS-rich
extracellular tumor milieu (slightly acidic, high ROS). Its
activation is confined to the intracellular space of
glycolytic cancer cells with mildly alkaline, ROS-rich
cytoplasm; and proceeds autonomously, without the need for
external light irradiation. In both two-dimensional (2D)
monolayer cultures and three-dimensional (3D) tumor spheroid
models, Diox@Ru exhibits robust luminescence and efficient
1O2 production, resulting in potent cytotoxic effects. These
findings present a versatile platform for autonomous
activation of self-luminescent PDT agents and highlight the
promise of logic-gated chemiluminescence for spatially
controlled therapy in complex biological settings.},
cin = {FM01},
ddc = {540},
cid = {I:(DE-He78)FM01-20160331},
pnm = {899 - ohne Topic (POF4-899)},
pid = {G:(DE-HGF)POF4-899},
typ = {PUB:(DE-HGF)16},
pubmed = {pmid:40696775},
doi = {10.1021/jacs.5c06761},
url = {https://inrepo02.dkfz.de/record/303087},
}