Research Square (Research Square),
Journal Year:
2023,
Volume and Issue:
unknown
Published: July 17, 2023
Abstract
The
5-hydroxytryptamine
receptor
(5-HTR)
family
involves
seven
classes
of
receptors.
5-HT
7
R
is
the
newest
member
this
and
contributes
to
different
physiological
pathological
processes.
As
a
pathology,
Glioblastoma
multiform
(GBM)
overexpresses
R;
hence,
study
aims
develop
radiolabeled
aryl
piperazine
derivatives
as
imaging
agents.
To
that
end,
compounds
6
1-(3-nitropyridin-2-yl)piperazine
were
with
fac
-[
99m
Tc(CO)
3
(H
2
O)
]
+
(
Tc(CO)3-[
])
obtained
high
radiochemical
purity
(RCP>94%).
possess
affinity
toward
U-87
MG
cell
line.
calculated
K
i
for
them
was
26.85±0.78
nM
36.67±0.89
nM.
biodistribution
in
normal
mice
indicates
brain
uptake
highest
at
30
min
post-injection
(0.8±0.25
0.64±0.18
%ID/g,
respectively).
data
U87-MG
xenograft
model
revealed
these
radiotracers
could
accumulate
tumor
site,
observed
60
(3.38±0.65
3.27±0.5
injection
pimozide
can
block
tumor’s
radiotracer
uptake,
indicating
binding
R.
also
confirms
data.
acquired
images
clearly
show
tumor-to-muscle
ratio
3.33
3.88,
respectively.
International Journal of Molecular Sciences,
Journal Year:
2023,
Volume and Issue:
24(4), P. 3521 - 3521
Published: Feb. 9, 2023
Glioblastoma
multiforme
(GBM)
is
the
most
common,
malignant,
poorly
promising
primary
brain
tumor.
GBM
characterized
by
an
infiltrating
growth
nature,
abundant
vascularization,
and
a
rapid
aggressive
clinical
course.
For
many
years,
standard
treatment
of
gliomas
has
invariably
been
surgical
supported
radio-
chemotherapy.
Due
to
location
significant
resistance
conventional
therapies,
prognosis
glioblastoma
patients
very
poor
cure
rate
low.
The
search
for
new
therapy
targets
effective
therapeutic
tools
cancer
current
challenge
medicine
science.
microRNAs
(miRNAs)
play
key
role
in
cellular
processes,
such
as
growth,
differentiation,
cell
division,
apoptosis,
signaling.
Their
discovery
was
breakthrough
diagnosis
diseases.
Understanding
structure
miRNAs
may
contribute
understanding
mechanisms
regulation
dependent
on
miRNA
pathogenesis
diseases
underlying
these
short
non-coding
RNAs,
including
glial
tumors.
This
paper
provides
detailed
review
latest
reports
relationship
between
changes
expression
individual
formation
development
gliomas.
use
this
also
discussed.
Computers in Biology and Medicine,
Journal Year:
2023,
Volume and Issue:
165, P. 107402 - 107402
Published: Aug. 28, 2023
Lung
adenocarcinoma
(LUAD)
is
the
most
prevalent
subtype
of
non-small
cell
lung
cancer.
Additionally,
disulfidptosis,
a
newly
discovered
type
death,
has
been
found
to
be
closely
associated
with
onset
and
progression
tumors.
The
study
first
identified
genes
related
disulfidptosis
through
correlation
analysis.
These
were
then
screened
using
univariate
cox
regression
LASSO
regression,
prognostic
model
was
constructed
multivariate
regression.
A
nomogram
also
created
predict
prognosis
LUAD.
validated
in
three
independent
data
sets:
GSE72094,
GSE31210,
GSE37745.
Next,
patients
grouped
based
on
their
median
risk
score,
differentially
expressed
between
two
groups
analyzed.
Enrichment
analysis,
immune
infiltration
drug
sensitivity
evaluation
conducted.
In
this
study,
we
examined
21
developed
gene
signature
that
poorer
Our
datasets
showed
AUC
values
greater
than
0.5
at
1,
3,
5
years.
analysis
revealed
disulfidptosis-related
had
multifaceted
impact
LUAD,
particularly
relation
tumor
development,
proliferation,
metastasis.
Patients
high-risk
group
exhibited
higher
purity
lower
stromal
ESTIMATE
Immune
score.
This
analyzed
its
disease
association
microenvironment.
findings
research
provide
valuable
insights
into
understanding
could
potentially
lead
development
new
treatment
strategies.
Journal of Experimental & Clinical Cancer Research,
Journal Year:
2024,
Volume and Issue:
43(1)
Published: Jan. 22, 2024
Abstract
Background
Extensive
local
invasion
of
glioblastoma
(GBM)
cells
within
the
central
nervous
system
(CNS)
is
one
factor
that
severely
limits
current
treatments.
The
aim
this
study
was
to
uncover
genes
involved
in
process,
which
could
also
serve
as
therapeutic
targets.
For
isolation
invasive
GBM
from
non-invasive
cells,
we
used
a
three-dimensional
organotypic
co-culture
where
glioma
stem
cell
(GSC)
spheres
were
confronted
with
brain
organoids
(BOs).
Using
ultra-low
input
RNA
sequencing
(ui-RNA
Seq),
an
gene
signature
obtained
exploited
context.
Methods
GFP-labeled
tumor
sorted
and
regions
co-cultures.
Ui-RNA
analysis
performed
find
cluster
up-regulated
compartment.
This
further
analyzed
using
Connectivity
MAP
(CMap)
database.
led
identification
SKF83566,
antagonist
D1
dopamine
receptor
(DRD1),
candidate
molecule.
Knockdown
overexpression
experiments
molecular
pathways
responsible
for
effects
SKF83566.
Finally,
SKF83566
validated
orthotopic
xenograft
models
vivo.
Results
seq
three
GSC
(P3,
BG5
BG7)
yielded
set
27
differentially
expressed
between
cells.
CMap
analysis,
identified
selective
inhibitor
targeting
both
DRD1
DRD5.
In
vitro
studies
demonstrated
inhibited
proliferation,
sphere
formation,
invasion.
SKF83566-treated
P3,
BG5,
BG7,
control
populations
total
32
genes,
predicted
be
regulated
by
c-Myc.
Of
these,
UHRF1
emerged
most
downregulated
following
treatment,
ChIP
revealed
c-Myc
binds
its
promoter
region.
or
stable
knockdown,
growth
(BG5)
derived
xenografts
nude
mice.
Conclusions
contributes
progression
regulating
entry
into
nucleus
affects
transcription
gene.
inhibits
transmembrane
protein
DRD1,
such
represents
small
molecule
GBMs.
Cancers,
Journal Year:
2022,
Volume and Issue:
14(20), P. 5041 - 5041
Published: Oct. 14, 2022
In
addition
to
being
the
most
common
primary
brain
tumor,
gliomas
are
also
among
difficult
diagnose
and
treat.
At
present,
“gold
standard”
in
glioma
treatment
entails
surgical
resection
of
largest
possible
portion
followed
by
temozolomide
therapy
radiation.
However,
this
approach
does
not
always
yield
desired
results.
Additionally,
ability
cross
blood-brain
barrier
remains
a
major
challenge
for
new
potential
drugs.
Thus,
researchers
continue
search
targeted
therapies
that
can
be
individualized
based
on
specific
characteristics
each
case.
Metabolic
lipidomic
research
may
represent
two
best
ways
achieve
goal,
as
they
enable
detailed
insights
into
changes
profile
small
molecules
biological
system/specimen.
This
article
reviews
approaches
analysis
alterations
biochemical
pathways,
it
provides
an
overview
clinical
results
support
personalized
future.
International Journal of Molecular Sciences,
Journal Year:
2023,
Volume and Issue:
24(11), P. 9393 - 9393
Published: May 28, 2023
Solute
carriers
(SLCs)
are
essential
for
brain
physiology
and
homeostasis
due
to
their
role
in
transporting
necessary
substances
across
cell
membranes.
There
is
an
increasing
need
further
unravel
pathophysiological
implications
since
they
have
been
proposed
play
a
pivotal
tumor
development,
progression,
the
formation
of
microenvironment
(TME)
through
upregulation
downregulation
various
amino
acid
transporters.
Due
implication
malignancy
SLCs
currently
positioned
at
center
novel
pharmacological
targeting
strategies
drug
development.
In
this
review,
we
discuss
key
structural
functional
characteristics
main
SLC
family
members
involved
glioma
pathogenesis,
along
with
potential
options
provide
new
opportunities
CNS
design
more
effective
management.
ACS Omega,
Journal Year:
2025,
Volume and Issue:
10(7), P. 6446 - 6469
Published: Feb. 11, 2025
Recent
investigations
have
shown
serotonin's
stimulatory
effect
on
several
types
of
cancers
and
carcinoid
tumors.
Nowadays
there
has
been
a
significant
increase
in
interest
5-HT7
5-HT5A
receptors
the
context
cancer
treatment.
The
possible
role
5-HT6R
pathogenesis
progression
glioma
remains
an
interesting
relatively
unexplored
issue.
We
developed
new
group
long-chain
2-aminoquinazoline
sulfonamides
as
multifunctional
serotonin
receptor
ligands,
focused
5-HT6R.
chosen
was
further
evaluated
for
antiproliferative
effects
1321N1
astrocytoma
cells,
along
with
U87MG,
U-251,
LN-229
glioblastoma
cell
lines.
Certain
compounds
were
subjected
to
vitro
absorption,
distribution,
metabolism,
excretion,
toxicity
(ADMET)
testing,
assessing
factors
such
lipophilicity,
plasma
protein
binding,
phospholipid
affinity,
potential
drug–drug
interactions
(DDI),
membrane
permeability
(PAMPA),
metabolic
stability,
hepatotoxicity.
Additionally,
vivo
testing
performed
using
Danio
rerio
model.
includes
selective
antagonist
PP
15,
dual
ligand
5-HT1AR/5-HT6R
13,
5-HT5AR/5-HT6R
10.
use
ligands
associated
high
anticancer
activity
both
against
selected
lines
other
(IC50
<
25
μM).
International Immunopharmacology,
Journal Year:
2025,
Volume and Issue:
150, P. 114228 - 114228
Published: Feb. 12, 2025
Glioma-associated
mesenchymal
stem
cells
(GA-MSCs)
are
one
of
the
key
factors
limiting
effectiveness
glioblastoma
(GBM)
treatment
and
contributing
to
poor
patient
prognosis,
making
them
a
potential
therapeutic
target
for
GBM.
In-depth
research
into
complex
crosstalk
between
GA-MSCs
GBM
not
only
aids
in
understanding
mechanisms
progression
but
also
provides
valuable
insights
developing
new
drugs.
We
conducted
comprehensive
bioinformatics
analysis
aimed
at
identifying
shared
dysregulated
genes
GA-MSCs.
Through
hub
gene
enrichment
immune
infiltration
analyses,
we
explored
molecular
pathways
landscape.
Additionally,
Cox
regression
was
employed
identify
influencing
overall
survival
The
expression
patterns
functional
roles
were
validated
across
various
cancer
types
datasets.
Finally,
dynamic
simulations
used
assess
binding
affinity
drugs
targets,
further
supporting
their
as
candidates.
identified
32
candidate
primarily
involved
1-kappa-B
kinase/NF-kappa-B
MAPK
signaling
pathways,
both
which
played
critical
tumor
survival,
proliferation,
invasion.
Notable
included
DUSP1,
FYN,
FLNC,
FN1,
G3BP1,
MYO1B,
WLS,
each
uniquely
progression.
Among
them,
FLNC
highlighted
regulatory
factor
Molecular
dynamics
revealed
its
target,
particularly
demonstrating
high
with
staurosporine.
proportion
dendritic
contributed
formation
microenvironment.
This
study
co-expression
metabolic
GBM,
providing
Targeting
staurosporine
presents
promising
strategy
Aditionally,
targeting
may
offer
approach
treating
malignant
brain
tumors.
Acta Neuropathologica Communications,
Journal Year:
2025,
Volume and Issue:
13(1)
Published: April 30, 2025
Gliomas
and
brain
metastases
are
notorious
for
their
dismal
prognosis
low
survival
rates,
a
challenge
exacerbated
by
our
incomplete
grasp
of
the
complex
dynamics
that
govern
cancers.
Recently,
groundbreaking
paradigm
shift
has
emerged,
highlighting
crucial
role
synaptic
communication
between
neurons
tumor
cells
in
reshaping
neuronal
signaling
to
favor
growth.
This
review
delves
into
pivotal
interplay
mechanisms,
focusing
on
excitatory
glutamatergic
inhibitory
GABAergic
pathways.
Glutamatergic
synapses
utilize
glutamate
propagate
signals,
while
employ
gamma-aminobutyric
acid
(GABA)
inhibit
firing.
can
be
broadly
classified
ionotropic
(NMDAR,
AMPAR
kainite
receptors)
metabotropic
subtypes.
The
harmonious
orchestration
these
types
is
essential
normal
function,
dysregulation
implicated
neurodegenerative
disorders
such
as
Alzheimer's
disease
epilepsy.
Emerging
evidence
reveals
glioma
metastatic
exploit
pathways
neurotransmitters
enhance
proliferation
survival.
In
this
review,
we
will
first
explore
intricate
mechanisms
underlying
signaling.
Next,
summarize
recent
advancements
understanding
how
cancer
hijack
advantage.
Finally,
propose
novel
therapeutic
strategies
aimed
at
disrupting
aberrant
neuron-tumor
communication,
offering
potential
treatment
combating
otherwise
incurable