Angewandte Chemie,
Год журнала:
2024,
Номер
136(15)
Опубликована: Фев. 7, 2024
We
realized
the
microenvironment-differential
Imaging
of
demethylated
metabolites
methionine
and
regional
regulation
ferroptosis.
The
authors
declare
no
conflict
interest.
data
that
support
findings
this
study
are
available
in
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article.
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typeset.
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(other
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addressed
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Journal of the American Chemical Society,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 12, 2025
Covalent
modification
of
cell
membranes
has
shown
promise
for
tumor
imaging
and
therapy.
However,
existing
membrane
labeling
techniques
face
challenges
such
as
slow
kinetics
poor
selectivity
cancer
cells,
leading
to
off-target
effects
suboptimal
in
vivo
efficacy.
Here,
we
present
an
enzyme-triggered
self-immobilization
strategy,
termed
E-SIM,
which
enables
rapid
selective
with
bioorthogonal
trans-cycloctene
(TCO)
handles
vivo.
E-SIM
utilizes
P-TCO,
alkaline
phosphatase
(ALP)
responsive
quinone
methide
(QM)
precursor
a
TCO
group,
facilitating
the
conjugation
high-density
onto
via
proximity
labeling.
These
groups
then
react
efficiently
tetrazine
(Tz)-bearing
reporters
fast
reaction,
resulting
significant
enrichment
various
sizes
modalities
on
membranes.
We
demonstrate
efficacy
reaction
pretargeted
multimodality
tumors
Notably,
achieve
efficient
installation
Tz-modified
Renilla
luciferase
cells
vivo,
thereby
offering
highly
sensitive
bioluminescence
signals
detecting
guiding
surgical
removal
small
human
HepG2
liver
peritoneal
metastases.
represents
robust
tool
precise
complex
environments,
feasible
multimodal
applications.
Journal of Medicinal Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 2, 2025
Hypoxia
is
a
state
of
low
oxygen
tension
that
found
in
numerous
solid
tumors.
Generally,
nitroreductase
(NTR)
overexpressed
and
directly
correlated
with
the
hypoxic
status
tumors,
supporting
hypothesis
prodrug
could
be
activated
by
intracellular
NTR
lead
to
potential
antitumor
therapy.
Herein,
evodiamine-based
hypoxia-targeting
theranostic
agents
were
developed
enhance
efficacy.
These
are
NTR-mediated
p-nitrobenzyl
reduction,
enabling
simultaneous
fluorophore
activation
for
imaging
therapeutic
agent
(3-fluoro-10-hydroxyl-evodiamine)
release
tumor
treatment.
After
systemic
test,
these
verified
selectively
excellent
fluorescence
properties
potency.
In
particular,
Probe-2
exhibited
vivo
activity
(tumor
growth
inhibition
value
(TGI)
=
76.1%)
HCT116
xenograft
nude
mice
favorable
tumor-targeted
toxicity.
Thus,
this
NTR-responsive
provides
platform
constructing
prodrugs
monitoring
active
substances
controlled
status.
Chemical Science,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 1, 2025
Tetrazine-based
fluorogenic
labels
are
widely
utilized
in
medical
and
biological
studies,
exhibiting
substantial
fluorescence
enhancement
(FE)
following
tetrazine
degradation
through
bio-orthogonal
reactions.
However,
the
underlying
mechanisms
driving
this
response
remain
only
partially
resolved,
particularly
regarding
diminished
FE
efficiency
deep-red
near-infrared
(NIR)
regions.
This
knowledge
gap
has
impeded
efforts
to
optimize
these
for
extended
emission
wavelengths
improved
ratios.
review
offers
a
photophysical
perspective,
discussing
quenching
pathways
(i.e.,
energy
flows
charge
separation)
that
regulate
properties
exhibited
various
types
of
labels.
Moreover,
work
examines
emerging
role
intramolecular
rotations
certain
tetrazine-based
structures
integration
additional
quencher
units.
The
proposed
alternative
channel
potential
surpass
traditional
wavelength
constraints
while
achieving
FE.
By
examining
mechanisms,
aims
advance
understanding
tetrazine-functionalized
provide
guiding
principles
their
future
design
practical
applications.
Chemical Society Reviews,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 1, 2025
In
this
review,
recent
progress
in
tetrazine-based
fluorogenic
probes
for
bioorthogonal
chemistry
is
comprehensively
analyzed,
with
a
focus
on
advancements
probe
design
and
their
imaging
applications
molecular
processes
live
cells.