ACS Infectious Diseases,
Год журнала:
2024,
Номер
10(11), С. 3915 - 3927
Опубликована: Окт. 11, 2024
Bioinspired
from
cationic
antimicrobial
peptides,
sequence-defined
triazolium-grafted
peptoid
oligomers
(6-
to
12-mer)
were
designed
adopt
an
amphipathic
helical
polyproline
I-type
structure.
Their
evaluation
on
a
panel
of
bacterial
strains
(Escherichia
coli,
Pseudomonas
aeruginosa,
Staphylococcus
aureus,
and
Enterococcus
faecalis),
pathogenic
fungi
(Candida
albicans,
Cryptococcus
neoformans,
Aspergillus
fumigatus),
human
cells
(hRBC,
BEAS-2B,
Caco-2,
HaCaT,
HepG2)
enabled
the
identification
two
heptamers
with
improved
activity
selectively
fight
aureus
pathogens.
Modulation
parameters
such
as
nature
triazolium
hydrophobic/lipophilic
side
chains,
charge
content,
sequence
length
drastically
potentiates
selectivity.
Besides,
ability
block
proinflammatory
effect
induced
by
lipopolysaccharide
or
lipoteichoic
acid
was
also
explored.
Finally,
biophysical
studies
circular
dichroism
fluorescence
spectroscopies
strongly
supported
that
bactericidal
these
primarily
due
selective
disruption
membrane.
Frontiers in Immunology,
Год журнала:
2024,
Номер
15
Опубликована: Июнь 24, 2024
Protein-protein
interactions
(PPIs)
play
critical
roles
in
a
wide
range
of
biological
processes
including
the
dysregulation
cellular
pathways
leading
to
loss
cell
function,
which
turn
leads
diseases.
The
dysfunction
several
signaling
is
linked
insurgence
pathological
such
as
inflammation,
cancer
development
and
neurodegeneration.
Thus,
there
an
urgent
need
for
novel
chemical
modulators
dysregulated
PPIs
drive
progress
targeted
therapies.
Several
have
been
by
bioactive
compounds,
and,
often,
properly
cover
interacting
protein
regions
improve
activities
modulators,
particular
focus
concerns
employment
macrocycles
proteomimetics.
Indeed,
their
physicochemical
properties,
they
occupy
intermediate
space
between
small
organic
molecules
macromolecular
proteins
are
prominent
drug
discovery
process.
Peptide
can
modulate
fundamental
mechanisms
here
we
will
on
peptidomimetics
active
Janus
kinase/signal
transducers
activators
transcription
(JAK-STAT)
pathways.
Expert Opinion on Drug Discovery,
Год журнала:
2024,
Номер
19(6), С. 699 - 723
Опубликована: Май 16, 2024
Introduction
Peptide
foldamers
play
a
critical
role
in
pharmaceutical
research
and
biomedical
applications.
This
review
highlights
recent
(post-2020)
advancements
novel
foldamers,
synthetic
techniques,
their
applications
research.
Chemical Communications,
Год журнала:
2024,
Номер
unknown
Опубликована: Янв. 1, 2024
1-2
Sentences
highlighting
the
novelty
of
work
In
this
review,
we
provide
a
very
first
comprehensive
exposition
artificial
potassium
transporters
derived
from
aromatic
foldamers
mostly
over
past
ten
years.
Abstract
We
report
the
development
of
a
redox‐responsive
system
that
induces
reversible
conformational
changes
in
peptides
through
design
seven‐membered
cyclic
α,α‐disubstituted
α‐amino
acid
with
disulfide
bond,
5‐amino‐1,2‐dithiepane‐5‐carboxylic
(Dtp).
Upon
reduction,
bond
Dtp
was
cleaved
to
form
thiols,
converting
into
(2‐mercaptoethyl)homocysteine
(Mhc),
and
this
process
reversed
by
oxidation.
Dtp‐containing
predominantly
adopted
3
10
‐helical
conformation
solution,
whereas
Mhc‐containing
exhibited
mixture
helical
other
conformations.
This
mechanism
allows
for
precise
control
over
peptide
secondary
structures,
making
it
promising
approach
designing
functional
capable
acting
molecular
switches
response
intracellular
reductive
environments.
Comptes Rendus Chimie,
Год журнала:
2025,
Номер
28(G1), С. 1 - 10
Опубликована: Фев. 19, 2025
This
account
summarizes
our
work
on
the
synthesis
of
fluorinated
peptidomimetics
integrating
N-CF2R
triazole
functions.
Emphasis
is
placed
development
foldamers
possessing
preferential
conformations.
We
have
shown
that
these
are
potential
modulators
amyloid
protein
aggregation.
Ce
compte
rendu
résume
nos
travaux
de
synthèse
peptidomimétiques
fluorés
intégrant
la
fonction
N-CF2R.
L'accent
est
mis
sur
le
développement
foldamères
possédant
des
conformations
préférentielles.
Nous
avons
montré
que
ces
sont
modulateurs
l'agrégation
protéines
amyloïdes.
Chemistry - A European Journal,
Год журнала:
2025,
Номер
unknown
Опубликована: Март 11, 2025
Abstract
Structural
analysis
of
a
co‐crystal
helically‐folded
peptide‐foldamer
hybrid
in
complex
with
hDM2
E3
ubiquitin
ligase,
revealed
unique
orientation
for
the
C
‐terminal
proline
pyrrolidine
ring
pointing
backwards
sequence,
and
suggested
new
opportunities
macrocyclization.
In
particular,
we
found
that
prolyl
residue
could
be
replaced
by
its
(2
S
,4
)‐4‐mercaptoprolyl
analogue
optimal
bisthioether
crosslinking
cysteine
installed
at
position
4
sequence.
The
resulting
i
,
+7
stapled
is
high‐affinity
binder
to
hDM2,
cell
permeable
restores
p53
signalling
pathway
p53wt
cancer
cells.
structure
was
determined
1.84
Å,
fully
validating
original
design
further
highlighting
potential
cis
‐4‐mercaptoproline
context
peptide
foldamer
stapling.
