Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Nov. 20, 2024
Tumor
necrosis
factor
receptor-associated
protein
1
(TRAP1)
is
a
molecular
chaperone
implicated
in
pro-tumorigenic
pathways
by
regulating
the
folding
of
substrate
proteins
(clients)
within
cancer
cells.
Recent
research
has
pinpointed
potentially
druggable
allosteric
site
client
binding
(CBS)
TRAP1,
suggesting
this
might
offer
more
effective
strategy
for
developing
potent
and
selective
TRAP1
inhibitors.
However,
absence
reliable
assay
systems
hindered
quantitative
evaluation
In
study,
we
have
developed
fluorescent
probe,
Rho6TPP,
designed
to
target
CBS.
Utilizing
fluorescence
polarization-based
high-throughput
screening
assays,
Rho6TPP
exhibits
excellent
signal-to-noise
ratio
(>20),
Z
(>0.6),
Z′
(>0.6).
Additionally,
it
facilitates
comparative
analysis
existing
small
molecules
discovery
novel
binders.
MitoTam,
mitochondria-targeted
tamoxifen,
emerges
as
CBS-targeting
inhibitor.
Our
findings
highlight
potential
crucial
tool
advancing
development
Molecules,
Journal Year:
2025,
Volume and Issue:
30(2), P. 396 - 396
Published: Jan. 18, 2025
Ratiometric
lanthanide
coordination
polymers
(Ln-CPs)
are
advanced
materials
that
combine
the
unique
optical
properties
of
ions
(e.g.,
Eu3+,
Tb3+,
Ce3+)
with
structural
flexibility
and
tunability
polymers.
These
widely
used
in
biological
chemical
sensing,
environmental
monitoring,
medical
diagnostics
due
to
their
narrow-band
emission,
long
fluorescence
lifetimes,
excellent
resistance
photobleaching.
This
review
focuses
on
composition,
sensing
mechanisms,
applications
ratiometric
Ln-CPs.
The
mechanism
relies
two
distinct
emission
bands,
which
provides
a
self-calibrating,
reliable,
precise
method
for
detection.
relative
intensity
ratio
between
these
bands
varies
concentration
target
analyte,
enabling
real-time
monitoring
minimizing
interference.
approach
is
particularly
suitable
detecting
trace
analytes
use
complex
environments
where
factors
like
background
noise,
temperature
fluctuations,
light
variations
may
affect
results.
Finally,
we
outline
future
research
directions
improving
design
synthesis
Ln-CPs,
such
as
incorporating
long-lifetime
reference
luminescent
molecules,
exploring
near-infrared
systems,
developing
up-conversion
or
two-photon
materials.
Progress
areas
could
significantly
broaden
scope
Ln-CP
applications,
especially
biosensing,
other
fields.
International Journal of Molecular Sciences,
Journal Year:
2024,
Volume and Issue:
25(6), P. 3521 - 3521
Published: March 20, 2024
The
phrase
“Let
food
be
thy
medicine…”
means
that
can
a
form
of
medicine
and
food;
in
other
words,
the
diet
we
eat
have
significant
impact
on
our
health
well-being.
Today,
this
is
gaining
prominence
as
more
scientific
evidence
suggests
one’s
help
prevent
treat
disease.
A
rich
fruits,
vegetables,
whole
grains,
lean
protein
reduce
risk
heart
disease,
cancer,
diabetes,
problems
and,
hand,
processed
foods,
added
sugars,
saturated
fats
increase
same
diseases.
Electrophilic
compounds
health,
they
are
molecules
covalently
modify
cysteine
residues
present
thiol-rich
Keap1
protein.
These
bind
to
activate
NRF2,
which
promotes
its
translocation
nucleus
binding
DNA
ARE
region,
triggering
antioxidant
response
protecting
against
oxidative
stress.
include
polyphenols
flavonoids
nucleophilic
but
converted
electrophilic
quinones
by
metabolic
enzymes
such
polyphenol
oxidases
(PPOs)
sulfur
foods
Brassica
genus
(broccoli,
cauliflower,
cabbage,
Brussel
sprouts,
etc.)
garlic.
This
review
summarizes
current
knowledge
subject.
Biomolecules,
Journal Year:
2024,
Volume and Issue:
14(7), P. 746 - 746
Published: June 24, 2024
Leukemias
are
cancers
of
the
blood-forming
system,
representing
a
significant
challenge
in
medical
science.
The
development
leukemia
cells
involves
substantial
disturbances
within
cellular
machinery,
offering
hope
search
for
effective
selective
treatments
that
could
improve
5-year
survival
rate.
Consequently,
pathophysiological
processes
focus
critical
research.
Enzymes
such
as
cystathionine
beta-synthase
and
sulfurtransferases
like
thiosulfate
sulfurtransferase,
3-mercaptopyruvate
gamma-lyase
play
vital
role
sulfur
metabolism.
These
enzymes
essential
to
maintaining
homeostasis,
providing
robust
antioxidant
defenses,
supporting
cell
division.
Numerous
studies
have
demonstrated
cancerous
can
alter
expression
activity
these
enzymes,
uncovering
potential
vulnerabilities
or
molecular
targets
cancer
therapy.
Recent
laboratory
research
has
indicated
certain
lines
may
exhibit
changes
patterns
enzymes.
Analysis
scientific
literature
online
datasets
confirmed
variations
enzyme
function
specific
leukemic
compared
normal
leukocytes.
This
comprehensive
review
collects
analyzes
available
information
on
lines,
valuable
insights
identifying
new
pathways
this
field.
Biomedicines,
Journal Year:
2024,
Volume and Issue:
12(9), P. 1951 - 1951
Published: Aug. 26, 2024
Atherosclerosis
is
a
chronic
inflammatory
condition
marked
by
endothelial
dysfunction,
lipid
accumulation,
cell
infiltration,
and
extracellular
matrix
(ECM)
remodeling
within
arterial
walls,
leading
to
plaque
formation
potential
cardiovascular
events.
Key
players
in
ECM
inflammation
are
metalloproteinases
(MMPs)
CD147/EMMPRIN,
surface
glycoprotein
expressed
on
cells,
vascular
smooth
muscle
cells
(VSMCs),
immune
that
regulates
MMP
activity.
Hydrogen
sulfide
(H₂S),
gaseous
signaling
molecule,
has
emerged
as
significant
modulator
of
these
processes
including
oxidative
stress
mitigation,
reduction,
remodeling.
This
systematic
review
investigates
the
mechanistic
pathways
through
which
H₂S
influences
MMPs
CD147/EMMPRIN
assesses
its
impact
atherosclerosis
progression.
A
comprehensive
literature
search
was
conducted
across
PubMed,
Scopus,
Web
Science
databases,
focusing
studies
examining
modulation
contexts.
Findings
indicate
modulates
expression
activity
transcriptional
regulation
post-translational
modifications,
S-sulfhydration.
By
mitigating
stress,
reduces
activation,
contributing
stability
also
downregulates
via
pathways,
diminishing
responses
cellular
proliferation
plaques.
The
dual
regulatory
role
inhibiting
downregulating
CD147
suggests
therapeutic
agent
stabilizing
atherosclerotic
plaques
inflammation.
Further
research
warranted
elucidate
precise
molecular
mechanisms
explore
H₂S-based
therapies
for
clinical
application
atherosclerosis.
Advanced Functional Materials,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Jan. 7, 2025
Abstract
Atherosclerosis
(AS)
stands
as
a
primary
cause
of
vascular
diseases
worldwide,
with
its
occurrence
and
progression
being
attributed
to
the
interplay
multiple
risk
factors.
Therefore,
it
is
imperative
develop
comprehensive
strategy
aimed
at
effectively
mitigating
reversing
AS.
Herein,
hydrogen
sulfide
(H
2
S)
donor
incorporated
into
thermal‐sensitive
polymer
possessing
an
upper
critical
solution
temperature
(UCST),
which
not
only
serves
novel
macromolecular
H
S
but
also
forms
targeted
nanocarrier
for
delivering
near
infrared
II
photothermal
agent,
achieving
gas‐photothermal
therapy
against
AS
notable
advantages.
For
one
aspect,
multifunctional
UCST
nanomedicine
could
target
atherosclerotic
plaque
perform
photoacoustic
imaging‐guided
S‐photothermal
reduce
ratio
en‐face
aortic
lesion
areas
from
17.2%
6.5%
alleviate
inflammatory
microenvironment.
another
inevitable
hepatic
accumulation
would
activate
5'‐adenosine
monophosphate
(AMP)‐activated
protein
kinase/mammalian
rapamycin
signaling
pathway,
thereby
enhancing
lipid
metabolism
reducing
plasma
triglyceride
levels.
This
transformation
waste
valuable
asset
further
aids
in
inhibiting
Consequently,
here
mediate
effective
attenuate
Pharmaceuticals,
Journal Year:
2025,
Volume and Issue:
18(3), P. 344 - 344
Published: Feb. 27, 2025
Age-related
oxidative
stress
is
a
critical
factor
in
vascular
dysfunction,
contributing
to
hypertension
and
atherosclerosis.
Smooth
muscle
cells
endothelial
are
particularly
susceptible
damage,
which
exacerbates
aging
through
cellular
senescence,
chronic
inflammation,
arterial
stiffness.
Gasotransmitters—hydrogen
sulfide
(H2S),
nitric
oxide
(NO),
carbon
monoxide
(CO)—are
emerging
as
promising
therapeutic
agents
for
counteracting
these
processes.
This
review
synthesizes
findings
from
recent
studies
focusing
on
the
mechanisms
by
H2S,
NO,
CO
influence
smooth
cell
function.
Therapeutic
strategies
involving
exogenous
gasotransmitter
delivery
systems
combination
therapies
were
analyzed.
H2S
enhances
mitochondrial
bioenergetics,
scavenges
ROS,
activates
antioxidant
pathways.
NO
improves
function,
promotes
vasodilation,
inhibits
platelet
aggregation.
exhibits
cytoprotective
anti-inflammatory
effects
modulating
heme
oxygenase
activity
ROS
production.
In
preclinical
studies,
gasotransmitter-releasing
molecules
(e.g.,
NaHS,
SNAP,
CORMs)
targeted
show
significant
promise.
Synergistic
with
lifestyle
modifications
further
enhance
their
potential.
conclusion,
gasotransmitters
hold
promise
combat
age-related
cells.
Their
multifaceted
innovative
approaches
make
them
potential
candidates
treating
dysfunction
promoting
healthy
aging.
Further
research
needed
translate
into
clinical
applications.
Scientific Reports,
Journal Year:
2025,
Volume and Issue:
15(1)
Published: March 3, 2025
Kawasaki
disease
(KD)
is
a
severe
pediatric
vasculitis
leading
to
coronary
artery
complications.
Hydrogen
sulfide
(H2S),
recognized
endogenous
gasotransmitter
with
anti-inflammatory
properties,
offers
potential
as
novel
treatment
for
KD
through
its
cardiovascular
benefits.
However,
the
specific
effects
and
underlying
mechanisms
remain
unclear.
The
objective
of
present
study
investigate
therapeutic
exogenous
H2S
in
using
network
pharmacology
experimental
validation.
By
online
database
searches,
total
405
pharmacological
targets
H2S,
826
KD-related
targets,
107
were
identified.
Through
PPI
analysis
Cytoscape
screening,
9
hub
genes
filtered,
namely
TNF,
IL6,
JUN,
AKT1,
IL1B,
TP53,
NFKB1,
MAPK1,
RELA.
KEGG
pathway
enrichment
indicated
that
TLR4/MyD88/NF-κB
signaling
may
play
crucial
role
on
KD.
Additionally,
vivo
experiments
confirmed
sodium
hydrosulfide
(NaHS),
an
donor,
markedly
improved
body
weight,
reduced
inflammatory
pathology
arteries,
downregulated
levels
cytokines
TNF-α,
IL-1β,
IL-6.
Furthermore,
WB
NaHS
inhibited
expression
TLR4,
MyD88,
NF-κB,
p-NF-κB.
In
brief,
it
first
reveal
attenuates
response
via
pathway,
highlighting
approach
These
findings
lay
foundation
further
development
H2S-based
therapies
management.