Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
67(5), P. 3244 - 3273
Published: Feb. 29, 2024
Camptothecin
(CPT)
is
a
potent
anti-cancer
agent
targeting
topoisomerase
I
(TOP1).
However,
CPT
has
poor
pharmacokinetic
properties,
causes
toxicities,
and
leads
to
drug
resistance,
which
limit
its
clinical
use.
In
this
paper,
review
the
current
state
of
research.
We
first
briefly
explain
CPT's
TOP1
inhibition
mechanism
key
hurdles
in
development.
Then
we
examine
strategies
overcome
limitations
through
structural
modifications
advanced
delivery
systems.
Though
alone
seem
insufficient
fully
enhance
therapeutic
potential,
structure-activity
relationship
analysis
provides
insights
guide
optimization
analogs.
comparison,
systems
integrating
controlled
release,
imaging
capabilities,
combination
therapies
via
stimulus-responsive
linkers
moieties
show
great
promise
for
improving
pharmacological
profile.
Looking
forward,
multifaceted
approaches
combining
selective
derivatives
with
systems,
informed
by
emerging
biological
insights,
hold
unleashing
potential.
Aggregate,
Journal Year:
2023,
Volume and Issue:
5(2)
Published: Oct. 3, 2023
Abstract
The
induction
of
tumor
carbonyl
stress
is
reported
to
efficiently
revert
immune
suppression
in
the
microenvironment
and
enhance
cancer
immunotherapy.
However,
low
oxygen
concentration
due
inherent
hypoxia
limits
its
catalytic
effect.
Herein,
an
injectable
thermosensitive
hydrogel
system
(named
APH)
developed
for
co‐loading
near‐infrared
(NIR)
aggregation‐induced
emission
(AIE)
nanoparticles
plasma
amine
oxidase
(PAO)
boosting
enhancing
antitumor
immunity.
Upon
808
nm
NIR
laser
irradiation,
AIE
trigger
a
mild‐temperature
(around
45°C)
photothermal
effect
site,
which
significantly
relieves
promotes
released
PAO
inhibit
growth
Myeloid‐derived
suppressor
cells.
Remarkably,
synergistic
therapeutic
APH
verified
through
significant
inhibitory
on
distant
tumor,
enhanced
memory,
effective
postoperative
recurrence,
rechallenge,
metastasis.
Overall,
combined
AIE‐mediated
therapy
by
upon
irradiation
can
activate
immunotherapy,
making
it
promising
treatment
approach
treatment.
Aggregate,
Journal Year:
2024,
Volume and Issue:
5(4)
Published: Feb. 29, 2024
Abstract
Solar‐driven
interfacial
evaporation
is
a
promising
technology
for
desalination.
The
photothermal
conversion
materials
are
at
the
core
and
play
key
role
in
this
field.
Design
of
based
on
organic
dyes
desalination
still
challenge
due
to
lack
efficient
guiding
strategy.
Herein,
new
D
(donor)‐A
(acceptor)
type
conjugated
tetraphenylpyrazine
(TPP)
luminophore
(namely
TPP‐2IND)
was
prepared
as
molecule.
It
exhibited
broad
absorption
spectrum
strong
π
–
stacking
solid
state,
resulting
sunlight
harvesting
boosting
nonradiative
decay.
TPP‐2IND
powder
high
efficiency
upon
660
nm
laser
irradiation
(0.9
W
cm
−2
),
surface
temperature
can
reach
200°C.
Then,
an
heating
system
established
successfully.
water
rate
solar‐driven
were
evaluated
up
1.04
kg
m
h
−1
65.8%
under
1
sunlight,
respectively.
Thus,
novel
shows
potential
stimulates
development
advanced
materials.
Aggregate,
Journal Year:
2024,
Volume and Issue:
5(3)
Published: Jan. 22, 2024
Abstract
The
induction
of
regulated
cell
death
(RCD)
through
photo/ultrasound
sensitization
therapeutic
agents
has
gained
significant
attention
as
a
vital
approach
to
combat
drug
resistance
in
tumors.
Aggregation‐induced
emission
(AIE)
generate
reactive
oxygen
species
activation,
which
can
synergize
with
RCD
inducers
or
directly
induce
RCD,
ultimately
resulting
the
tumor
cells.
presented
comprehensive
review
delves
into
recent
advancements
AIE
designed
trigger
inducers,
encompassing
apoptosis,
necroptosis,
pyroptosis,
immunogenic
death,
autophagy,
ferroptosis,
and
cuproptosis.
Additionally,
intricate
regulatory
mechanisms
activatory‐AIE
therapeutics
influence
distinct
pathways
are
examined.
A
forward‐looking
perspective
on
future
developments
pertinent
challenges
within
this
exciting
realm
is
presented,
anticipating
continued
evolution
activatable
transformative
enhance
therapy.
Journal of Medicinal Chemistry,
Journal Year:
2024,
Volume and Issue:
67(5), P. 3244 - 3273
Published: Feb. 29, 2024
Camptothecin
(CPT)
is
a
potent
anti-cancer
agent
targeting
topoisomerase
I
(TOP1).
However,
CPT
has
poor
pharmacokinetic
properties,
causes
toxicities,
and
leads
to
drug
resistance,
which
limit
its
clinical
use.
In
this
paper,
review
the
current
state
of
research.
We
first
briefly
explain
CPT's
TOP1
inhibition
mechanism
key
hurdles
in
development.
Then
we
examine
strategies
overcome
limitations
through
structural
modifications
advanced
delivery
systems.
Though
alone
seem
insufficient
fully
enhance
therapeutic
potential,
structure-activity
relationship
analysis
provides
insights
guide
optimization
analogs.
comparison,
systems
integrating
controlled
release,
imaging
capabilities,
combination
therapies
via
stimulus-responsive
linkers
moieties
show
great
promise
for
improving
pharmacological
profile.
Looking
forward,
multifaceted
approaches
combining
selective
derivatives
with
systems,
informed
by
emerging
biological
insights,
hold
unleashing
potential.
