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.
Biomacromolecules,
Год журнала:
2024,
Номер
25(5), С. 3087 - 3097
Опубликована: Апрель 8, 2024
Heparan
sulfate
proteoglycans
(HSPGs)
play
a
crucial
role
in
regulating
cancer
growth
and
migration
by
mediating
interactions
with
factors.
In
this
study,
we
developed
self-assembling
peptide
(
Angewandte Chemie,
Год журнала:
2024,
Номер
136(30)
Опубликована: Май 3, 2024
Abstract
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
1
O
2
‐cleavable
thioketal
linker.
Upon
localized
NIR
photoirradiation,
generates
elicit
immunogenic
cell
death
tumors
induce
specific
activation
sitagliptin.
The
subsequent
inhibition
DPP4
increases
intratumoral
CCL11
levels
promote
chemotaxis
activation.
SPNe‐mediated
photo‐immunotherapy
synergized
with
checkpoint
blockade
greatly
promotes
infiltration
both
cells,
effectively
inhibiting
growth
metastasis.
Thus,
this
study
presents
generic
polymeric
nanoplatform
precision
immunotherapy.
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.
