Tetrahedron Letters,
Год журнала:
2024,
Номер
142, С. 155108 - 155108
Опубликована: Май 12, 2024
Peptides
are
finding
broad
applications
in
drug
discovery
as
Active
Pharmaceutical
Ingredients
(APIs)
and
delivery
systems,
also
the
field
of
new
materials.
In
this
context,
increasing
relevance
these
molecules
has
fueled
development
more
efficient
synthetic
strategies
at
both
research
industrial
scales.
The
generation
peptides
market
contains
hindered
amino
acids,
examples
include
antidiabetic
antiobesity
drugs
semaglutide
tirzepatide,
which
contain
α,α-dimethylglycine
(Aib),
trofinetide,
α-methylproline.
Given
that
peptide
synthesis
involves
proper
combination
protecting
groups
coupling
reagents,
it
is
important
to
develop
for
acid-containing
peptides.
first
communication,
we
report
ethylthio-1H-tetrazole
(ETT),
a
reagent
widely
used
oligonucleotide
but
unknown
synthesis,
well
suited
be
with
N.N'-diisopropylcarbodiimide
(DIC)
preparation
ETT
acidic
than
1-hydroxybenzotriazole
(HOBt)
ethyl
2-hydroxyimino-2-cyanoacetate
(OxymaPure),
and,
such,
active
species
formed
will
have
an
excellent
leaving
group,
thereby
facilitating
reaction.
To
demonstrate
concept,
synthesized
analogs
Leu-enkephalin
amide,
where
two
consecutive
Gly
acids
were
substituted
by
Aib,
NMeGly,
NMeAla.
syntheses
carried
out
superior
those
done
OxymaPure,
HOBt,
1-hydroxy-7-azabenzotriazole.
(HOAt).
However,
terms
racemization,
showed
poorer
performance
other
additives,
especially
case
His(Trt).
conclusion,
emerges
contributor
toolbox
reagents
additives
amide
formation.
Abstract
Negative
therapeutic
feedback
of
inflammation
would
extensively
attenuate
the
antitumor
effect
photodynamic
therapy
(PDT).
In
this
work,
tumor
homing
chimeric
peptide
rhomboids
(designated
as
NP‐Mel)
are
fabricated
to
improve
performance
by
inhibiting
PDT‐upregulated
cyclooxygenase‐2
(COX‐2).
The
hydrophobic
photosensitizer
protoporphyrin
IX
(PpIX)
and
palmitic
acid
conjugated
onto
neuropilin
receptors
(NRPs)
targeting
motif
(CGNKRTR)
obtain
(Palmitic‐K(PpIX)CGNKRTR),
which
can
encapsulate
COX‐2
inhibitor
meloxicam.
well
dispersed
NP‐Mel
not
only
improves
drug
stability
reactive
oxygen
species
(ROS)
production
ability,
but
also
increase
breast
cancer
targeted
delivery
intensify
PDT
effect.
vitro
in
vivo
studies
verify
that
will
decrease
secretion
prostaglandin
E2
(PGE2)
after
treatment,
inducing
downregulation
IL‐6
TNF‐α
expressions
suppress
induced
inflammation.
Ultimately,
an
improved
is
achieved
without
obvious
systemic
toxicity,
might
inspire
development
sophisticated
nanomedicine
consideration
resistance.
ACS Applied Bio Materials,
Год журнала:
2025,
Номер
unknown
Опубликована: Фев. 5, 2025
Despite
its
therapeutic
potential,
photodynamic
therapy
faces
several
key
limitations
in
clinical
applications,
including
poor
drug
delivery
and
insufficient
tumor
selectivity.
We
engineered
RFYFYR-Ce6-RFYFYR
(R-Ce6-R),
a
twin-tail
peptide–photosensitizer
conjugate
that
self-assembles
into
nanostructures
for
improved
cancer
treatment.
By
incorporating
arginine-rich
peptide
sequences,
this
design
not
only
enhances
cellular
internalization
but
also
promotes
peroxynitrite
(ONOO–)
formation,
amplifying
the
effect.
Our
studies
revealed
R-Ce6-R
achieves
33-fold
higher
potency
than
unmodified
Ce6,
with
an
IC50
of
0.18
μM.
The
demonstrated
selective
accumulation
tissue,
robust
ROS
generation,
complete
regression
animal
models
while
maintaining
favorable
safety
profile.
These
results
establish
as
innovative
approach
advancing
Chemical Science,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 1, 2025
This
review
provides
an
overview
of
activatable
peptide–AIEgen
conjugates
for
tumor
imaging,
with
emphasis
on
the
most
recent
breakthroughs
in
past
three
years
(from
2022
to
late
2024)
Abstract
Antimicrobial
resistance
caused
by
overuse
of
antibiotics
has
promoted
the
demand
for
effective
antibacterial
materials.
However,
development
existing
strategies
mostly
focuses
on
direct
sterilization,
which
may
lead
to
flora
imbalance
and
drug
resistance.
Here,
a
series
peptide‐based
aggregation‐induced
emssion
nanomaterials
(PBANs)
with
multiple
structural
domains
were
designed
mimicking
self‐assembly
human
α‐defensin
6.
Specifically,
PBANs
self‐assemble
form
nanoparticles
in
physiological
environments
situ
transform
into
nanofibers
bacterial
surfaces
through
receptor‐ligand
interactions
infected
microenvironments,
resulting
enhanced
fluorescence
signal
activation
functions,
while
labeling
entrapping
bacteria.
Different
from
traditional
that
directly
kill
pathogenic
microorganisms,
can
inhibit
motility
invasion
host
system
physical
barriers
affecting
energy
metabolism
pathways.
In
addition,
further
recruit
macrophages
infection
site
engulf
entrapped
bacteria,
thereby
synergistically
reducing
efficiency.
mouse
piglet
systemic
models,
showed
favorable
therapeutic
efficacy,
significantly
load
levels
inflammation
factors.
Overall,
this
study
provides
perspectives
developing
biomimetic
stimuli‐responsive
combat
infections.
