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.
Orally
targeting
nanostrategies
of
multiple
nutraceuticals
have
attracted
increasing
attention
in
ulcerative
colitis
(UC)
therapy
for
superior
patient
compliance,
cost-effectiveness,
and
biocompatibility.
However,
the
actual
delivery
bioefficacy
are
extremely
restricted
by
their
poor
solubility,
interior
gastrointestinal
retention,
base
permeability.
Herein,
we
developed
controllable
colon-targeting
nanoparticles
(NPs)
composed
a
quaternary
ammonium
chitosan
(HTCC)
shell
succinic
acid-modified
γ-cyclodextrin
(SACD)
core
precise
UC
treatment.
Egg
white-derived
peptides
(EWDP,
typical
food-derived
peptides)
could
not
only
function
as
potential
cross-linkers
to
induce
differential
coassembly
with
above
biopolymers
but
also
aid
hydrophobic
curcumin
(Cur)
solubility
well
nutrition
enhancers
oral
synergism
therapy.
More
specifically,
NPs
higher
EWDP
efficiency
exhibited
better
pH-sensitive
colloidal
tunability
(e.g.,
smaller
size,
rigidity,
roughness)
robust
(EWDP/Cur)
coloading
capacity
(24.0–33.2%
≫
10%,
pH
2.0–7.0).
Compared
pure
nutraceuticals,
excellent
cellular
absorption
(almost
10
times)
bioavailability
(4.19–5.05
enhancement
via
faster
mucus
permeation
macropinocytosis
transport,
indirectly
regulating
systemic
inflammatory
response.
The
sustainable
sequential
release
targeted
accumulation
profiles
directly
facilitated
interactions
colonic
microenvironment,
verified
intestinal
barrier
recovery
gut
microbiota
restoration.
Moreover,
critical
role
amino
acid
metabolism
reconfirmed
importance
maintaining
homeostasis.
Overall,
this
study
would
provide
facile,
quantitative,
versatile
perspective
into
programmable
design
peptide
EWDP)
coassembled
nanoplatforms
UC.
Advanced Materials,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 10, 2025
Abstract
Cancer
immunotherapy,
which
leverages
immune
system
components
to
treat
malignancies,
has
emerged
as
a
cornerstone
of
contemporary
therapeutic
strategies.
Yet,
critical
concerns
about
the
efficacy
and
safety
cancer
immunotherapies
remain
formidable.
Nanotechnology,
especially
polymeric
nanoparticles
(PNPs),
offers
unparalleled
flexibility
in
manipulation‐from
chemical
composition
physical
properties
precision
control
nanoassemblies.
PNPs
provide
an
optimal
platform
amplify
potency
minimize
systematic
toxicity
broad
spectrum
immunotherapeutic
modalities.
In
this
comprehensive
review,
basics
polymer
chemistry,
state‐of‐the‐art
designs
from
physicochemical
standpoint
for
encompassing
vaccines,
situ
vaccination,
adoptive
T‐cell
therapies,
tumor‐infiltrating
cell‐targeted
antibodies,
cytokine
therapies
are
delineated.
Each
immunotherapy
necessitates
distinctively
tailored
design
strategies
nanoplatforms.
The
extensive
applications
PNPs,
investigation
their
mechanisms
action
enhanced
particularly
focused
on.
profiles
clinical
research
progress
discussed.
Additionally,
forthcoming
developments
emergent
trends
nano‐immunotherapeutics
poised
transform
treatment
paradigms
into
clinics
explored.
Journal of the American Chemical Society,
Год журнала:
2024,
Номер
146(19), С. 13163 - 13175
Опубликована: Май 3, 2024
A
pretargeted
strategy
that
decouples
targeting
vectors
from
radionuclides
has
shown
promise
for
nuclear
imaging
and/or
therapy
in
vivo.
However,
the
current
approach
relies
on
use
of
antibodies
or
nanoparticles
as
vectors,
which
may
be
compromised
by
poor
tissue
penetration
and
limited
accumulation
tumor
tissues.
Herein,
we
present
an
orthogonal
dual-pretargeted
combining
stimuli-triggered
situ
self-assembly
with
fast
inverse
electron
demand
Diels-Alder
(IEDDA)
reaction
strong
biotin-streptavidin
(SA)
interaction
near-infrared
fluorescence
(NIR
FL)
magnetic
resonance
(MR)
tumors.
This
uses
a
small-molecule
probe
(P-Cy-TCO&Bio)
containing
both
biotin
trans-cyclooctene
(TCO)
tumor-targeting
vector.
P-Cy-TCO&Bio
can
efficiently
penetrate
subcutaneous
HeLa
tumors
through
biotin-assisted
targeted
delivery
undergo
to
form
biotinylated
TCO-bearing
(Cy-TCO&Bio
NPs)
cell
membranes.
Cy-TCO&Bio
NPs
exhibited
"off-on"
NIR
FL
retained
tumors,
offering
high
density
TCO
groups
concurrent
capture
Gd-chelate-labeled
tetrazine
(Tz-Gd)
IR780-labeled
SA
(SA-780)
via
IEDDA
SA-biotin
interaction.
Moreover,
offered
multiple-valent
binding
modes
toward
SA,
additionally
regulated
cross-linking
Cy-Gd&Bio
into
microparticles
(Cy-Gd&Bio/SA
MPs).
process
could
significantly
(1)
increase
Angewandte Chemie International Edition,
Год журнала:
2024,
Номер
63(30)
Опубликована: Май 3, 2024
Eosinophils
are
important
immune
effector
cells
that
affect
T
cell-mediated
antitumor
immunity.
However,
the
low
frequency
and
restrained
activity
of
eosinophils
restricted
outcome
cancer
immunotherapies.
We
herein
report
an
eosinophil-activating
semiconducting
polymer
nanoparticle
(SPNe)
to
improve
photodynamic
tumor
immunogenicity,
modulate
eosinophil
chemotaxis,
reinvigorate
T-cell
immunity
for
activated
photo-immunotherapy.
SPNe
comprises
amphiphilic
a
dipeptidyl
peptidase
4
(DPP4)
inhibitor
sitagliptin
via
ACS Applied Materials & Interfaces,
Год журнала:
2024,
Номер
16(15), С. 18400 - 18410
Опубликована: Апрель 5, 2024
Drug-resistant
bacterial
infection
and
biofilm
formation
are
the
key
inhibitors
of
wound
healing,
new
strategies
urgently
needed
to
address
these
issues.
In
this
study,
we
designed
a
pH-responsive
co-assembled
peptide
hydrogel
inhibit
Methicillin-resistant
Staphylococcus
aureus
(MRSA)
promote
healing.
We
synthesized
cationic
short
(Nap-FFKKK)
with
curcumin
at
pH
∼
7.8.
The
loaded
was
continuously
released
in
weak
acid
environment
(pH
5.5).
lysine-rich
inhibited
MRSA
via
electrostatic
interaction
negatively
charged
cell
surface
and,
thus,
provided
reinforcing
antibacterial
effect
curcumin.
vitro
experiments
showed
that
system
considerably
reduced
minimum
inhibitory
concentration
against
by
10-fold
promoted
healing
mouse
model
MRSA-infected
wounds.
This
study
provides
simple
promising
strategy
treat
drug-resistant
infections
Macromolecular Rapid Communications,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 21, 2025
Abstract
Residual
dipolar
coupling
(RDC)
not
only
contributes
to
the
dynamic
analysis
of
proteins
but
also
provides
a
robust
route
for
structure
determination
small
organic
compounds.
An
essential
prerequisite
this
methodology
is
availability
alignment
media.
Herein,
series
novel
peptide‐based
media
are
generated
by
introducing
D‐type
or
halogen‐bearing
amino
acids
RDC
measurements.
Compared
with
self‐assembled
peptide
liquid
crystal
(LC)
medium
containing
D
‐amino
acid,
incorporation
halogen
elements
improved
electronegativity
LCs,
resulting
in
enhanced
strength
toward
analytes.
Meanwhile,
LCs
can
provide
different
orientations
relative
non‐halogenated
media,
allowing
acquirement
independent
sets
RDCs.
The
presented
enrich
existing
ignite
way
creating
multiple
independent,
non‐linearly
related
measurement.
Angewandte Chemie International Edition,
Год журнала:
2024,
Номер
63(28)
Опубликована: Апрель 24, 2024
Abstract
Self‐assembly
in
living
cells
represents
one
versatile
strategy
for
drug
delivery;
however,
it
suffers
from
the
limited
precision
and
efficiency.
Inspired
by
viral
traits,
we
here
report
a
cascade
targeting‐hydrolysis‐transformation
(THT)
assembly
of
glycosylated
peptides
holistically
resembling
infection
efficient
cargo
delivery
combined
tumor
therapy.
We
design
peptide
via
incorporating
β‐galactose‐serine
residue
into
bola‐amphiphilic
sequences.
Co‐assembling
with
two
counterparts
containing
irinotecan
(IRI)
or
ligand
TSFAEYWNLLSP
(PMI)
results
formation
co‐assemblies
SgVEIP
,
which
target
cancer
β‐galactose‐galectin‐1
association
undergo
galactosidase‐induced
morphological
transformation.
While
GSH‐reduction
causes
release
IRI
co‐assemblies,
PMI
moieties
p53
facilitate
cell
death
binding
protein
MDM2.
Cellular
experiments
show
membrane
targeting,
endo‐/lysosome‐mediated
internalization
situ
nanofibers
cytoplasm
.
This
THT
process
enables
secreting
Gal‐1
overexpressing
β‐galactosidase.
In
vivo
studies
illustrate
enhanced
accumulation
retention
thereby
suppressing
growth.
Our
findings
demonstrate
an
mimicking
infection,
thus
providing
new
route
therapy
future.
Biomedicines,
Год журнала:
2024,
Номер
12(1), С. 202 - 202
Опубликована: Янв. 16, 2024
Peptide-functionalized
nanomedicine,
which
addresses
the
challenges
of
specificity
and
efficacy
in
drug
delivery,
is
emerging
as
a
pivotal
approach
for
cancer
therapy.
Globally,
remains
leading
cause
mortality,
conventional
treatments,
such
chemotherapy,
often
lack
precision
adverse
effects.
The
integration
peptides
into
nanomedicine
offers
promising
solution
enhancing
targeting
delivery
therapeutic
agents.
This
review
focuses
on
three
primary
applications
peptides:
cell-targeting
ligands,
building
blocks
self-assembling
nanostructures,
elements
stimuli-responsive
systems.
Nanoparticles
modified
with
improved
cells,
minimized
damage
to
healthy
tissues,
optimized
delivery.
versatility
self-assembled
peptide
structures
makes
them
an
innovative
vehicle
by
leveraging
their
biocompatibility
diverse
nanoarchitectures.
In
particular,
mechanism
cell
death
induced
novel
addition,
systems
enable
precise
release
response
specific
conditions
tumor
microenvironment.
use
not
only
augments
safety
treatments
but
also
suggests
new
research
directions.
this
review,
we
introduce
functionalization
methods
using
or
peptide-modified
nanoparticles
overcome
treatment
cancers,
including
breast
cancer,
lung
colon
prostate
pancreatic
liver
skin
glioma,
osteosarcoma,
cervical
cancer.
ABSTRACT
Because
of
their
wide
variety
biological
effects,
bioactive
peptides
(BAPs)
have
recently
attracted
a
lot
attention.
BAPs
been
observed
to
be
safe,
thanks
widely
acknowledged
safety
status
by
the
United
States
Food
and
Drug
Administration
(USFDA).
This
has
led
widespread
use
in
various
industries,
such
as
food
nutrition,
pharmaceuticals,
therapeutics.
A
considerable
amount
research
devoted
developing
cutting‐edge
nanomaterials
derived
from
BAPs,
which
utilized
range
industries.
In
realm
scientific
research,
remarkable
ability
self‐assemble
harnessed
develop
nanoassemblies.
These
nanoassemblies
hold
immense
potential
for
advancement
biomaterials
future.
Research
interest
continues
focus
on
study
detection
using
artificial
intelligence
(AI).
Over
past
few
years,
there
surge
utilizing
bio‐inspired
strategies
explore
new
possibilities
development
advanced
energy
devices
storage
solutions.
However,
these
require
extensive
review
offers
broad
perspective
applications
nanotechnology
well
pharmaceuticals
Moreover,
silico
analysis
coupled
with
‐omics
techniques,
discussed.
bargain,
next‐generation
approaches
BAP
comprising
BAP‐based
devices,
AI,
catalogued.
There
is
emphasis
more
eco‐friendly
energy‐storage
technologies
that
draw
inspiration
nature
BAPs.