Chemical Reviews,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Feb. 25, 2025
Cell-surface
receptors
are
vital
for
controlling
numerous
cellular
processes
with
their
dysregulation
being
linked
to
disease
states.
Therefore,
it
is
necessary
develop
tools
study
and
the
signaling
pathways
they
control.
This
Review
broadly
describes
molecular
approaches
that
enable
1)
visualization
of
determine
localization
distribution;
2)
sensing
receptor
activation
permanent
readouts
as
well
in
real
time;
3)
perturbing
activity
mimicking
receptor-controlled
learn
more
about
these
processes.
Together,
have
provided
valuable
insight
into
fundamental
biology
helped
characterize
therapeutics
target
receptors.
The Journal of Organic Chemistry,
Journal Year:
2024,
Volume and Issue:
89(10), P. 6740 - 6748
Published: May 2, 2024
BODIPY
photocages
are
photoreactive
chromophores
that
release
covalently
linked
cargo
upon
absorption
of
visible
light.
Here,
we
used
computations
the
T1
photoheterolysis
barrier
to
ascertain
whether
a
computational
approach
could
assist
in
priori
structure
design
by
identifying
new
structures
with
higher
quantum
yields
photorelease.
The
electronic
structure–photoreactivity
relationships
were
elucidated
for
boron-substituted
and
core-functionalized
2-substituted
as
well
aryl
substitutions
at
meso-methyl
position.
Although
there
is
clear
trend
derivatives,
donor-substituted
derivatives
featuring
both
lower
computed
barriers
experimental
yields,
no
yield
activation
found
meso-methyl-substituted
or
derivatives.
lack
correlation
between
latter
two
substitution
cases
attributed
substituents
having
larger
effects
on
rates
competing
channels
(internal
conversion
competitive
photoreactions)
than
rate
channel.
Thus,
although
some
photoreaction
can
aid
ignored
impacts
how
changing
affects
photophysical/photochemical
limit
effectiveness
this
single-parameter
approach.
Journal of Medicinal Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Feb. 17, 2025
Resiquimod,
an
imidazoquinoline
scaffold,
exhibits
potent
immunotherapeutic
activity
but
is
associated
with
off-target
effects,
limiting
its
clinical
utility.
To
address
this
limitation,
we
developed
a
novel
BODIPY-caged
resiquimod
that
responsive
to
red
light,
combining
photocaging
and
photodynamic
therapy
functionalities.
Molecular
docking
studies
guided
identification
of
the
optimal
caging
site
for
resiquimod,
effectively
masking
immune
activity.
remained
inactive
under
dark
conditions,
resiquimod's
immunostimulatory
effects.
However,
light
irradiation
precisely
uncaged
inducing
robust
activation,
even
in
presence
N-acetyl
cysteine
as
antioxidant.
Notably,
attachment
BODIPY
reduced
toxicity
typically
photosensitizer.
In
3D
spheroid
models
HeLa
A549
cells,
demonstrated
spatiotemporal
control
over
cytotoxicity,
significantly
enhancing
cell
death
only
upon
irradiation.
This
dual-function
therapeutic
approach
highlights
"win–win"
strategy:
precise,
red-light-mediated
activation
efficacy
collateral
toxicity.
RSC Medicinal Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Jan. 1, 2025
This
review
covers
the
history
of
light
therapy,
emergence
photopharmacology,
its
methods,
and
challenges.
Current
advancements
show
promise
for
treating
diseases
like
cancer
with
precision
minimal
side
effects.