Retinoic
acid
receptor-related
orphan
receptor
γ
(RORγ)
is
a
circadian
regulator
and
has
emerged
as
experimental
therapeutic
target
in
inflammation
immunity.
The
cyclic
temporal
role
of
RORγ
rhythms
makes
temporally-resolved
pharmacological
control
this
particularly
intriguing.
To
achieve
next-generation
tools
to
study
biology,
we
designed
ligands
featuring
central
azobenzene
photoswitch,
that
act
light-dependent
inverse
agonists.
Structural
optimization
enabled
efficient
photocontrol
over
inhibition,
with
remarkable
potency
on
excellent
selectivity
related
receptors.
These
high-specificity
photopharmaceuticals
can
serve
high-precision
the
dynamic
modulation
signaling
pathways
inflammatory
disorders.
Chemistry - A European Journal,
Journal Year:
2023,
Volume and Issue:
29(26)
Published: Feb. 15, 2023
Hemipiperazines
are
a
recently
discovered
class
of
peptide-derived
molecular
photoswitches
with
high
biocompatibility
and
therapeutic
potential.
Here,
for
the
first
time
we
describe
photochromism
heterocyclic
hemipiperazines.
They
demonstrate
long
thermal
lifetimes,
enlarged
band
separation
between
photoisomers.
Efficient
photoisomerization
occurs
under
aqueous
conditions,
although
need
organic
co-solvent.
Bidirectional
switching
visible
light
is
observed
an
extended
aromatic
system.
Organic & Biomolecular Chemistry,
Journal Year:
2023,
Volume and Issue:
21(24), P. 4993 - 4998
Published: Jan. 1, 2023
Incorporation
of
azobenzenes
into
macrocycles
is
an
intriguing
approach
for
fine
tuning
the
photophysical
properties
these
photoswitches
and
tailoring
them
to
specific
applications.
A
versatile
synthesis
macrocyclic
has
been
developed
that
allows
facile
modification
photoswitches.
One
example
shows
high
chemical
stability,
long
half-life
its
Z-isomers,
quantitative
Z
→
E
conversion
under
white
light,
excellent
separation
excitation
bands
address
either
or
Z-state
selectively.
The
near
light
a
unique
feature
with
important
impact
on
applications,
in
which
configuration
ambient
needs
be
close
100%.
New Journal of Chemistry,
Journal Year:
2023,
Volume and Issue:
47(25), P. 11882 - 11889
Published: Jan. 1, 2023
A
combination
of
experiment
and
theory
rationalize
the
unexpected
loss
photoisomerization
upon
azo
dye
protonation
at
a
site
that
does
not
interact
with
bond!
ChemMedChem,
Journal Year:
2023,
Volume and Issue:
18(11)
Published: March 10, 2023
Abstract
Activation
of
the
oxysterol‐sensing
transcription
factor
liver
X
receptor
(LXR)
has
been
studied
as
a
therapeutic
strategy
in
metabolic
diseases
and
cancer
but
is
compromised
by
side
effects
LXR
agonists.
Local
activation
treatment
may
offer
an
opportunity
to
overcome
this
issue
suggesting
potential
uses
photopharmacology.
We
report
computer‐aided
development
photoswitchable
agonists
based
on
T0901317
scaffold,
which
known
agonist.
Azologization
structure‐guided
structure‐activity
relationship
evaluation
enabled
design
agonist,
activated
with
low
micromolar
potency
its
light‐induced
(
Z
)‐state
was
inactive
E
)‐isomer.
This
tool
sensitized
human
lung
cells
chemotherapeutic
light‐dependent
manner
supporting
locally
adjuvant
treatment.
Angewandte Chemie International Edition,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Sept. 9, 2024
Abstract
Retinoic
acid
receptor‐related
orphan
receptor
γ
(RORγ)
is
a
nuclear
hormone
with
multiple
biological
functions
in
circadian
clock
regulation,
inflammation,
and
immunity.
Its
cyclic
temporal
role
rhythms,
cell‐specific
activity
the
immune
system,
make
it
an
intriguing
target
for
spatially
temporally
localised
pharmacology.
To
create
tools
that
can
study
RORγ
biology
appropriate
spatiotemporal
resolution,
we
designed
light‐dependent
inverse
agonists
by
building
azobenzene
photoswitches
into
ligand
consensus
structures.
Optimizations
gave
photoswitchable
inhibitors
combining
large
degree
of
potency
photocontrol,
remarkable
on‐target
potency,
excellent
selectivity
over
related
off‐target
receptors.
This
still
rare
combination
performance
features
distinguishes
them
as
high
quality
photopharmaceutical
probes,
which
now
serve
precision
to
spatial
dynamic
intricacies
action
signaling
inflammatory
disorders.
Journal of the American Chemical Society,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Dec. 16, 2024
Incorporating
photoisomerizable
moieties
within
drugs
offers
the
possibility
of
rapid
and
reversible
light-dependent
switching
between
active
inactive
configurations.
Here,
we
developed
a
photoswitchable
adenosine
A3
receptor
(A3R)
agonist
that
confers
optical
control
on
this
G
protein-coupled
through
noninvasive
topical
skin
irradiation
in
an
animal
model
psoriasis.
This
was
achieved
by
covalently
bonding
adenosine-5′-methyluronamide
moiety
to
diazocine
photochrome,
whose
singular
photoswitching
properties
facilitated
repeated
interconversion
thermally
stable,
biologically
Z
form
photoinduced,
pharmacologically
E
configuration.
As
result,
our
allowed
precise
modulation
A3R
function
both
vitro
vivo,
which
led
clear
light-controlled
pharmacotherapeutic
effect
mouse
lesions.
breakthrough
not
only
demonstrates
potential
photoswitches
for
vivo
photopharmacology
but
also
paves
way
development
new
strategies
skin-related
diseases
require
localized
temporally
controlled
drug
action.
Chemistry - A European Journal,
Journal Year:
2023,
Volume and Issue:
29(40)
Published: May 8, 2023
Abstract
Multiple
triggered‐release
strategies
are
widely
utilized
to
control
the
release
of
caged
target
molecules.
Among
them,
photocages
with
conditional
triggers
provide
extra
layers
in
photorelease.
In
this
work,
a
series
pH‐responsive
was
designed
that
could
be
triggered
under
irradiation
and
specific
intracellular
pH
values.
pH‐sensitive
phenolic
groups
were
conjugated
o
‐nitrobenzyl
(
oNB
)
form
azo‐phenolic
NPX
tunable
p
K
a.
These
azo‐phenol‐based
showed
differentiable
photoreleasing
profiles
at
5.0,
7.2
9.0.
By
attaching
fluorogenic
cargos,
it
shown
one
photocages,
NPdiCl
,
used
differentiate
between
acidic
5.0
neutral
cells
artificial
conditions.
Finally,
identified
as
promising
photocage
for
cargo
inside
tumor
cells.
Macromolecular Rapid Communications,
Journal Year:
2023,
Volume and Issue:
44(18)
Published: May 26, 2023
Modulating
on-demand
polymerization
is
a
challenge
in
synthetic
macromolecules.
Herein,
tailoring
controllability
and
dispersity
during
single-electron
transfer
mediated
living
radical
(SET-LRP)
of
methyl
methacrylate
(MMA)
achieved.
Hexaarylbiimidazole
(HABI)
employed
as
photoswitchable
catalyst,
allowing
reversible
control
catalytic
activity
between
an
active
inactive
state.
In
the
presence
HABI
with
light
on
(active
state),
SET-LRP
MMA
follows
first-order
kinetics,
resulting
polymers
narrow
molecular
weight
distribution.
contrast,
responds
to
reverts
their
original
uncontrolled
state
off
(inactive
state).
Therefore,
repeatable
resetting
can
be
easily
performed.
The
key
photomodulating
use
efficient
switch
tailor
breadths
dispersity.
Besides,
mechanism
HABI-mediated
switchable
ability
proposed.
Journal of Materials Chemistry C,
Journal Year:
2023,
Volume and Issue:
11(47), P. 16571 - 16577
Published: Jan. 1, 2023
Responsive
conductive
gels
have
gained
attention
owing
to
potential
applications
in
flexible
displays,
implantable
medical
devices,
touch
panels,
wearable
electronic
skin,
sensors,
soft
robotics,
and
related
areas
.
