Abstract
Tumor
progression
depends
on
angiogenesis,
which
is
stimulated
by
growth
factors
like
VEGF,
targeting
VEGFR
kinase
with
small
molecules
an
effective
anti‐angiogenic
therapeutic
approach.
The
rational
modification
of
sunitinib
(VEGFR‐2
inhibitor)
to
spirocyclopropyloxindoline
carboxamides
have
been
performed
and
their
in
vitro
cytotoxic
profiling
was
evaluated.
molecular
modelling
studies
enabled
the
screening
designed
analogues
identifying
possible
interactions
within
type
III
allosteric
inhibitor
binding
site
VEGFR‐2.
biological
synthesized
compounds
15
a
–
y
,
revealed
ability
compound
w
inhibit
cell
MCF‐7
line
IC
50
value
3.87±0.19
μM
alongside
inhibition
VEGFR‐2
at
concentration
4.34±0.13
observed.
Also,
validated
through
HUVEC
tube
formation
assay.
qualitative
assessment
apoptosis
induction
cells
evaluated
staining
such
as
AO/EB
DAPI
staining,
whereas
quantification
cycle
analysis
were
FACS
analysis.
metastatic
cancer
migration
scratch
wound
healing
current
study
strives
sequentially
optimize
structural
attributes
3‐alkenyl
oxindole
core
surpass
existing
challenges
well‐known
inhibitors.
findings
observed
from
this
highlights
that
be
prominent
lead
towards
development
clinical
drug
candidates.
Nursing,
Год журнала:
2024,
Номер
54(10), С. 50 - 53
Опубликована: Сен. 20, 2024
Abstract:
Age-related
macular
degeneration
(AMD)
is
the
leading
cause
of
visual
impairment
in
patients
age
50
and
older,
with
an
estimated
200
million
people
affected
worldwide
a
projected
288
by
2040.
This
article
provides
overview
epidemiology,
risk
factors,
pathophysiology,
clinical
manifestations,
diagnosis,
management,
nursing
considerations
for
AMD
to
equip
nurses
knowledge
play
crucial
role
early
detection
this
disease.
Frontiers in Pharmacology,
Год журнала:
2024,
Номер
15
Опубликована: Ноя. 12, 2024
The
tumor
microenvironment
(TME)
plays
a
crucial
role
in
cancer
development
and
metastasis.
This
review
summarizes
the
current
research
on
how
TME
promotes
metastasis
through
molecular
pathways,
focusing
key
components,
such
as
cancer-associated
fibroblasts,
immune
cells,
endothelial
cytokines,
extracellular
matrix.
Significant
findings
have
highlighted
that
alterations
cellular
communication
within
enable
cells
to
evade
surveillance,
survive,
invade
other
tissues.
highlights
roles
of
TGF-β
VEGF
signaling
promoting
angiogenesis
matrix
remodeling,
which
facilitate
Additionally,
we
explored
metabolic
reprogramming
stromal
influenced
by
nutrient
availability
TME,
drives
progression.
study
also
evaluated
therapeutic
strategies
targeting
these
interactions
disrupt
By
providing
multidisciplinary
perspective,
this
suggests
understanding
basis
can
lead
more
effective
therapies
identify
potential
avenues
for
future
research.
Future
should
prioritize
unraveling
complex
environment,
could
novel
personalized
treatments.
Moreover,
advancements
technologies
single-cell
analysis,
spatial
transcriptomics,
epigenetic
profiling
offer
promising
identifying
new
targets
improving
efficacy
immunotherapies,
particularly
context
Abstract
Tumor
progression
depends
on
angiogenesis,
which
is
stimulated
by
growth
factors
like
VEGF,
targeting
VEGFR
kinase
with
small
molecules
an
effective
anti‐angiogenic
therapeutic
approach.
The
rational
modification
of
sunitinib
(VEGFR‐2
inhibitor)
to
spirocyclopropyloxindoline
carboxamides
have
been
performed
and
their
in
vitro
cytotoxic
profiling
was
evaluated.
molecular
modelling
studies
enabled
the
screening
designed
analogues
identifying
possible
interactions
within
type
III
allosteric
inhibitor
binding
site
VEGFR‐2.
biological
synthesized
compounds
15
a
–
y
,
revealed
ability
compound
w
inhibit
cell
MCF‐7
line
IC
50
value
3.87±0.19
μM
alongside
inhibition
VEGFR‐2
at
concentration
4.34±0.13
observed.
Also,
validated
through
HUVEC
tube
formation
assay.
qualitative
assessment
apoptosis
induction
cells
evaluated
staining
such
as
AO/EB
DAPI
staining,
whereas
quantification
cycle
analysis
were
FACS
analysis.
metastatic
cancer
migration
scratch
wound
healing
current
study
strives
sequentially
optimize
structural
attributes
3‐alkenyl
oxindole
core
surpass
existing
challenges
well‐known
inhibitors.
findings
observed
from
this
highlights
that
be
prominent
lead
towards
development
clinical
drug
candidates.