A Photoactivatable AIEgen for Selective Imaging and Killing of Estrogen Receptor-Positive Cells

The development of fluorescent probes based on the skeletal
structure
of small-molecule targeted anticancer drugs is promising for biomedical
applications because these probes generally show trackable fluorescence
and connatural bioactivity inherited from the parental anticancer
drugs. By mimicking a classic estrogen receptor (ER) antagonist, namely,
tamoxifen, we herein design and synthesize a photoactivatable luminogen
with aggregation-induced emission and medicinal benefits. The probe
is weakly emissive when it is selectively internalized by estrogen
receptor-positive cells. Under photoirradiation, its emission can
be turned on to report the intracellular distribution. The cell viability
assay suggests that the probe only exhibits cytotoxicity to ER-positive
cells but negligible cytotoxicity to ER-negative cells. This study
thus provides new access to targeted theranostic systems with photoactivity.