Frontiers in Pharmacology,
Journal Year:
2025,
Volume and Issue:
16
Published: Feb. 18, 2025
Brigatinib
is
approved
in
multiple
countries
for
the
treatment
of
patients
with
anaplastic
lymphoma
kinase
(ALK)-positive
non-small
cell
lung
cancer
(NSCLC).
Despite
its
superior
efficacy,
dermal
toxicities
caused
by
brigatinib
cannot
be
overlooked.
However,
underlying
mechanism
remains
unknown.
The
effects
on
proliferation
ability
human
immortalized
keratinocyte
(HaCaT)
cells
were
evaluated
using
Cell
Counting
Kit-8
(CCK-8)
proliferation,
colony
formation,
and
5-ethynyl-2'-deoxyuridine
(EdU)
incorporation
assays.
apoptosis
detected
Annexin
FITC/PI
Acridine
Orange
(AO)
staining
cycle
was
assessed
flow
cytometry.
An
analysis
transcriptome
RNA
sequencing
procedures
(RNA-seq)
performed
to
reveal
key
regulatory
genes.
Gene
Ontology
(GO)
Kyoto
Encyclopedia
Genes
Genomes
(KEGG)
used
find
out
biological
function
related
signal
pathways.
expressions
amphiregulin,
epiregulin
transforming
growth
factor
alpha
(TGFA)
protein
levels
Phosphoinositide
3-kinase
(PI3K)/protein
B
(AKT)
Cleaved-Caspase
three
measured
quantitative
reverse
transcription
polymerase
chain
reaction
(qRT-PCR)
western
blot
assay.
inhibits
an
IC50
value
2.9
μmol/L
significantly
increases
rates.
Transcriptome
indicates
that
could
downregulate
expression
TGFA.
In
addition,
we
demonstrated
reduced
epiregulin,
TGFA,
PI3K,
AKT
phosphorylated
(p-AKT).
This
study
confirms
inhibition
HaCaT
progression
highlights
potential
PI3K/AKT
pathway
as
a
therapeutic
target
brigatinib-induced
toxicities.
Cancers,
Journal Year:
2023,
Volume and Issue:
15(13), P. 3474 - 3474
Published: July 3, 2023
Non-small
cell
lung
cancer
(NSCLC)
is
a
significant
public
health
concern
with
high
mortality
rates.
Recent
advancements
in
genomic
data,
bioinformatics
tools,
and
the
utilization
of
biomarkers
have
improved
possibilities
for
early
diagnosis,
effective
treatment,
follow-up
NSCLC.
Biomarkers
play
crucial
role
precision
medicine
by
providing
measurable
indicators
disease
characteristics,
enabling
tailored
treatment
strategies.
The
integration
big
data
artificial
intelligence
(AI)
further
enhances
potential
personalized
through
advanced
biomarker
analysis.
However,
challenges
remain
impact
new
on
efficacy
due
to
limited
evidence.
Data
analysis,
interpretation,
adoption
approaches
clinical
practice
pose
additional
emphasize
technologies
such
as
analysis
(AI),
which
enhance
Despite
these
obstacles,
into
has
shown
promising
results
NSCLC,
improving
patient
outcomes
targeted
therapies.
Continued
research
discovery,
utilization,
evidence
generation
are
necessary
overcome
medicine.
Addressing
obstacles
will
contribute
continued
improvement
non-small
cancer.
ACS Nano,
Journal Year:
2024,
Volume and Issue:
18(17), P. 11025 - 11041
Published: April 16, 2024
ALK-positive
NSCLC
patients
demonstrate
initial
responses
to
ALK
tyrosine
kinase
inhibitor
(TKI)
treatments,
but
eventually
develop
resistance,
causing
rapid
tumor
relapse
and
poor
survival
rates.
Growing
evidence
suggests
that
the
combination
of
drug
immune
therapies
greatly
improves
patient
survival;
however,
due
low
immunogenicity
tumors,
do
not
respond
currently
available
immunotherapies.
Tumor-associated
macrophages
(TAMs)
play
a
crucial
role
in
facilitating
lung
cancer
growth
by
suppressing
tumoricidal
activation
absorbing
chemotherapeutics.
However,
they
can
also
be
programmed
toward
pro-inflammatory
suppressive
phenotype,
which
represents
highly
active
area
therapy
development.
Iron
loading
TAMs
achieve
such
reprogramming
correlating
with
an
improved
prognosis
patients.
We
previously
showed
superparamagnetic
iron
oxide
nanoparticles
containing
core-cross-linked
polymer
micelles
(SPION-CCPMs)
target
stimulate
activation.
Here,
we
show
SPION-CCPMs
secrete
reactive
nitrogen
species
cytokines
exert
activity.
further
reshape
immunosuppressive
International Journal of Molecular Sciences,
Journal Year:
2024,
Volume and Issue:
25(13), P. 7264 - 7264
Published: July 1, 2024
Cancer
is
one
of
the
leading
causes
morbidity
and
death
worldwide,
making
it
a
serious
global
health
concern.
Chemotherapy,
radiotherapy,
surgical
treatment
are
most
used
conventional
therapeutic
approaches,
although
they
show
several
side
effects
that
limit
their
effectiveness.
For
these
reasons,
discovery
new
effective
alternative
therapies
still
represents
an
enormous
challenge
for
tumour
diseases.
Recently,
anticancer
peptides
(ACPs)
have
gained
attention
cancer
diagnosis
treatment.
ACPs
small
bioactive
molecules
which
selectively
induce
cell
through
variety
mechanisms
such
as
apoptosis,
membrane
disruption,
DNA
damage,
immunomodulation,
well
inhibition
angiogenesis,
survival,
proliferation
pathways.
can
also
be
employed
targeted
delivery
drugs
into
cells.
With
over
1000
clinical
trials
using
ACPs,
potential
application
in
therapy
seems
promising.
Peptides
utilized
conjunction
with
imaging
agents
molecular
methods,
MRI,
PET,
CT,
NIR,
improving
detection
classification
cancer,
monitoring
response.
In
this
review
we
will
provide
overview
biological
activity
some
natural
synthetic
common
malignant
tumours
affecting
people
around
world.
Frontiers in Pharmacology,
Journal Year:
2023,
Volume and Issue:
14
Published: March 24, 2023
Lung
cancer
is
one
of
the
common
malignant
cancers
worldwide.
Immune
checkpoint
inhibitor
(ICI)
therapy
has
improved
survival
lung
patients.
However,
ICI
leads
to
adaptive
immune
resistance
and
displays
PD-1/PD-L1
blockade
in
cancer,
leading
less
response
Tumor
microenvironment
(TME)
an
integral
tumor
microenvironment,
which
involved
immunotherapy
resistance.
Nanomedicine
been
used
enhance
cancer.
In
this
review
article,
we
described
association
between
TME
We
also
highlighted
importance
Moreover,
discussed
how
nanoparticles
are
regulation
improve
efficacy
immunotherapy,
including
SGT-53,
AZD1080,
Nanomodulator
NRF2,
Cisplatin
nanoparticles,
Au@PG,
DPAICP@ME,
SPIO
NP@M-P,
NBTXR3
ARAC
Nano-DOX,
MS
NPs,
Nab-paclitaxel,
GNPs-hPD-L1
siRNA.
Furthermore,
concluded
that
targeting
by
could
be
helpful
overcome
Frontiers in Oncology,
Journal Year:
2023,
Volume and Issue:
13
Published: Sept. 25, 2023
Breast
and
lung
cancer
are
two
of
the
most
lethal
forms
cancer,
responsible
for
a
disproportionately
high
number
deaths
worldwide.
Both
doctors
patients
express
alarm
about
rising
incidence
disease
globally.
Although
targeted
treatment
has
achieved
enormous
advancements,
it
is
not
without
its
drawbacks.
Numerous
medicines
chemotherapeutic
drugs
have
been
authorized
by
FDA;
nevertheless,
they
can
be
quite
costly
often
fall
short
completely
curing
condition.
Therefore,
this
investigation
conducted
to
identify
potential
medication
against
breast
through
structural
modification
genistein.
Genistein
active
compound
in
Glycyrrhiza
glabra
(licorice),
exhibits
solid
anticancer
efficiency
various
cancers,
including
brain
cancer.
Hence,
design
analogs
with
interchange
five
functional
groups-COOH,
NH2
OCH3,
Benzene,
NH-CH2-CH2-OH-have
employed
enhance
affinities
compared
primary
Additionally,
advanced
computational
studies
such
as
PASS
prediction,
molecular
docking,
ADMET,
dynamics
simulation
were
conducted.
Firstly,
prediction
spectrum
was
analyzed,
revealing
that
designed
genistein
exhibit
improved
antineoplastic
activity.
In
data,
selected
targets.
Subsequently,
other
investigations
gradually
The
mentioned
compounds
shown
acceptable
results
silico
ADME,
AMES
toxicity,
hepatotoxicity
estimations,
which
fundamental
their
oral
medication.
It
noteworthy
initial
binding
affinity
only
-8.7
kcal/mol
protein
(PDB
ID:
3HB5).
However,
after
group,
when
calculating
affinities,
becomes
apparent
increase
gradually,
reaching
maximum
-11.0
-10.0
kcal/mol.
Similarly,
-8.0
2P85),
but
addition
affinity,
reached
-9.5
Finally,
study
models
over
100
ns
examine
stability
docked
complexes.
indicate
complexes
remain
highly
stable
throughout
100-ns
runs,
displaying
strong
correlations
ligands
within
site
protein.
important
further
investigate
proceed
clinical
or
wet
lab
experiments
determine
practical
value
proposed
compounds.
