Current Molecular Pharmacology,
Год журнала:
2022,
Номер
16(3), С. 254 - 279
Опубликована: Сен. 3, 2022
Alzheimer's
disease
(AD),
the
primary
cause
of
dementia,
escalating
worldwide,
has
no
proper
diagnosis
or
effective
treatment.
Neuronal
cell
death
and
impairment
cognitive
abilities,
possibly
triggered
by
several
brain
mechanisms,
are
most
significant
characteristic
this
disorder.A
multitude
pharmacological
targets
have
been
identified
for
potential
drug
design
against
AD.
Although
many
advances
in
treatment
strategies
made
to
correct
various
abnormalities,
these
often
exhibit
limited
clinical
significance
because
aggressively
progresses
into
different
regions
brain,
causing
severe
deterioration.These
biomarkers
can
be
game-changers
early
detection
timely
monitoring
such
disorders.This
review
covers
clinically
AD
precise
risk
factors
stages
disease,
site
action
novel
drugs,
approaches
management.
Angewandte Chemie International Edition,
Год журнала:
2023,
Номер
62(15)
Опубликована: Фев. 14, 2023
Photoswitchable
materials
have
attracted
considerable
attention
in
various
fields.
Developing
excellent
solid-state
dual-mode
photoswitches
is
an
important
but
challenging
task.
Herein,
we
propose
a
new
strategy
to
construct
excited-state
intramolecular
proton
transfer
(ESIPT)
inspired
photoswitch
(DiAH-pht)
that
possesses
aggregation-induced
emission
(AIE)
features
and
displays
fast
molecular
isomerization
process
characterized
by
behavior
the
solid
state.
Mechanistic
studies
indicate
introduction
of
bulky
group
can
create
folded
conformation
provides
adequate
volume
facilitate
photoisomerization
enhanced
ESIPT
effect
boost
process.
The
feasibility
our
was
further
demonstrated
activated
performance
Schiff
base
derivatives.
Furthermore,
DiAH-pht
shows
good
fields
information
encryption
high-density
data
storage.
Analytical Chemistry,
Год журнала:
2023,
Номер
95(21), С. 8340 - 8347
Опубликована: Май 16, 2023
Biomarkers
detection
in
blood
with
high
accuracy
is
crucial
for
the
diagnosis
and
treatment
of
many
diseases.
In
this
study,
proof-of-concept
fabrication
a
dual-mode
sensor
based
on
single
probe
(Re-BChE)
using
dual-signaling
electrochemical
ratiometric
strategy
"turn-on"
fluorescent
method
presented.
The
Re-BChE
was
synthesized
step
demonstrated
dual
mode
response
toward
butyrylcholinesterase
(BChE),
promising
biomarker
Alzheimer's
disease
(AD).
Due
to
specific
hydrolysis
reaction,
turn-on
current
BChE
at
−0.28
V,
followed
by
turn-off
−0.18
while
fluorescence
spectrum
an
emission
wavelength
600
nm.
developed
sensitivity
concentrations
low
limit
0.08
μg
mL–1
0.05
mL–1,
respectively.
Importantly,
presents
following
advantages:
(1)
readout
can
correct
impact
systematic
or
background
error,
thereby
achieving
more
accurate
results;
(2)
responses
originate
from
two
distinct
mechanisms
relatively
independent
signal
transduction,
which
there
no
interference
between
signaling
routes.
Additionally,
compared
reported
single-signal
assays
BChE,
both
redox
potential
signals
were
detected
absence
biological
within
negative
window.
Furthermore,
it
discovered
that
outcomes
direct
quantifications
level
serum
agreement
those
obtained
use
commercially
available
assay
kits
sensing.
This
has
serve
as
useful
point-of-care
tool
early
AD.
Journal of Medicinal Chemistry,
Год журнала:
2023,
Номер
66(9), С. 6414 - 6435
Опубликована: Апрель 26, 2023
We
present
the
synthesis
and
characterization
of
merged
human
butyrylcholinesterase
(hBChE)
inhibitor/cannabinoid
receptor
2
(hCB2R)
ligands
for
treatment
neurodegeneration.
In
total,
15
benzimidazole
carbamates
were
synthesized
tested
their
inhibition
cholinesterases,
also
with
regard
to
pseudoirreversible
binding
mode
affinity
toward
both
cannabinoid
receptors
in
radioligand
studies.
After
evaluation
a
calcium
mobilization
assay
as
well
β-arrestin
(βarr2)
recruitment
assay,
two
compounds
balanced
activities
on
targets
immunomodulatory
effect
microglia
activation
regarding
pharmacokinetic
properties
blood–brain
barrier
penetration.
Compound
15d,
containing
dimethyl
carbamate
motif,
was
further
evaluated
vivo,
showing
prevention
Aβ25–35-induced
learning
impairments
pharmacological
mouse
model
Alzheimer's
disease
short-
long-term
memory
responses.
Additional
combination
studies
proved
synergic
BChE
CB2R
vivo.
Drugs and Drug Candidates,
Год журнала:
2025,
Номер
4(1), С. 2 - 2
Опубликована: Янв. 9, 2025
The
Group
for
the
Promotion
of
Pharmaceutical
Chemistry
in
Academia
(GP2A)
held
its
32nd
annual
conference
August
2024
at
University
Coimbra,
Portugal.
There
were
8
keynote
presentations,
12
early
career
researcher
oral
and
34
poster
presentations.
Four
awards
delivered,
two
best
communications
Medicinal Research Reviews,
Год журнала:
2025,
Номер
unknown
Опубликована: Март 23, 2025
ABSTRACT
Cholinergic
transmission
plays
a
critical
role
in
both
the
central
and
peripheral
nervous
systems,
affecting
processes
such
as
learning,
memory,
inflammation.
Conventional
cholinergic
drugs
generally
suffer
from
poor
selectivity
temporal
precision,
leading
to
undesired
effects
limited
therapeutic
efficacy.
Photopharmacology
aims
overcome
limitations
of
traditional
using
photocleavable
or
photoswitchable
ligands
spatiotemporal
patterns
illumination.
Spanning
muscarinic
nicotinic
modulators
cholinesterase
inhibitors,
this
review
explores
development
application
light‐activated
compounds
tools
for
unraveling
signaling
physiological
pathological
contexts,
while
also
paving
way
innovative
phototherapeutic
approaches.
Medicinal Research Reviews,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 5, 2025
ABSTRACT
Photopharmacology
is
an
innovative
approach
that
uses
light
to
activate
drugs.
This
method
offers
the
potential
for
highly
localized
and
precise
drug
activation,
making
it
particularly
promising
treatment
of
neurological
disorders.
Despite
enticing
prospects
photopharmacology,
its
application
treat
human
central
nervous
system
(CNS)
diseases
remains
be
demonstrated.
In
this
review,
we
provide
overview
prominent
strategies
design
activation
photopharmaceutical
agents
in
field
neuroscience.
Photocaged
photoswitchable
drugs
bioactive
molecules
are
discussed,
instructive
list
examples
provided
highlight
compound
strategies.
Special
emphasis
placed
on
photoactivatable
compounds
modulation
glutamatergic,
GABAergic,
dopaminergic,
serotonergic
neurotransmission
conditions,
as
well
various
photoresponsive
with
improved
pain
management.
Compounds
holding
promise
clinical
translation
discussed
in‐depth
their
future
applications
assessed.
Neurophotopharmaceuticals
have
yet
achieve
breakthrough
clinic,
both
delivery
not
reached
full
maturity.
However,
by
describing
current
state
art
providing
illustrative
case
studies,
offer
a
perspective
opportunities
neurophotopharmacology
focused
addressing
CNS
