Molecules,
Год журнала:
2017,
Номер
22(9), С. 1430 - 1430
Опубликована: Авг. 29, 2017
The
rapid
emergence
of
multidrug-resistant
pathogens
has
evolved
into
a
global
health
problem
as
current
treatment
options
are
failing
for
infections
caused
by
pan-resistant
bacteria.
Hence,
novel
antibiotics
in
high
demand,
and
this
reason
antimicrobial
peptides
(AMPs)
have
attracted
considerable
interest,
since
they
often
show
broad-spectrum
activity,
fast
killing
cell
selectivity.
However,
the
therapeutic
potential
natural
AMPs
is
limited
their
short
plasma
half-life.
Antimicrobial
peptidomimetics
mimic
structure
biological
activity
AMPs,
but
display
extended
stability
presence
matrices.
In
present
review,
focus
on
developments
reported
last
decade
with
respect
to
design,
synthesis,
cytotoxic
side
effects
well
applications
anti-infective
agents.
Specifically,
only
modular
residues
connected
via
amide
linkages
will
be
discussed.
These
comprise
classes
α-peptoids
(N-alkylated
glycine
oligomers),
β-peptoids
β-alanine
β3-peptides,
α/β3-peptides,
α-peptide/β-peptoid
hybrids,
α/γ
N-acylated
N-aminoethylpeptides
(AApeptides),
oligoacyllysines
(OAKs).
Such
particular
interest
due
potent
versatile
convenient
optimization
assembly
standard
solid-phase
procedures.
Chemical Society Reviews,
Год журнала:
2021,
Номер
50(8), С. 4932 - 4973
Опубликована: Янв. 1, 2021
Antimicrobial
resistance
(AMR)
is
one
of
the
greatest
threats
to
human
health
that,
by
2050,
will
lead
more
deaths
from
bacterial
infections
than
cancer.
New
antimicrobial
agents,
both
broad-spectrum
and
selective,
that
do
not
induce
AMR
are
urgently
required.
peptides
(AMPs)
a
novel
class
alternatives
possess
potent
activity
against
wide
range
Gram-negative
positive
bacteria
with
little
or
no
capacity
AMR.
This
has
stimulated
substantial
chemical
development
peptide-based
antibiotics
possessing
improved
therapeutic
index.
review
summarises
recent
synthetic
efforts
their
impact
on
analogue
design
as
well
various
applications
in
AMP
development.
It
includes
modifications
have
been
reported
enhance
including
lipidation,
glycosylation
multimerization
through
broad
application
bio-orthogonal
chemistry,
perspectives
direction
future
research.
The
subject
area
primarily
next-generation
agents
rational
modification
AMPs.
further
serves
guide
toward
most
promising
directions
this
field
stimulate
scientific
attention,
new,
effective
selective
solutions
for
several
biomedical
challenges
which
peptidomimetics
being
applied.
Frontiers in Immunology,
Год журнала:
2021,
Номер
11
Опубликована: Янв. 11, 2021
Diet-induced
metabolic
endotoxemia
is
an
important
factor
in
the
development
of
many
chronic
diseases
animals
and
man.
The
gut
epithelium
efficient
barrier
that
prevents
absorption
liposaccharide
(LPS).
Structural
changes
to
intestinal
response
dietary
alterations
allow
LPS
enter
bloodstream,
resulting
increase
plasma
levels
(termed
endotoxemia).
activates
Toll-like
receptor-4
(TLR4)
leading
production
numerous
pro-inflammatory
cytokines
and,
hence,
low-grade
systemic
inflammation.
Thus,
can
lead
several
inflammatory
conditions.
Obesity,
diabetes,
non-alcoholic
fatty
liver
disease
(NAFLD)
also
cause
permeability
potential
pharmacological
interventions
could
be
used
reduce
inflammation
associated
with
endotoxemia.
Microbial Drug Resistance,
Год журнала:
2018,
Номер
24(6), С. 747 - 767
Опубликована: Июнь 29, 2018
In
recent
years,
because
of
increased
resistance
to
conventional
antimicrobials,
many
researchers
have
started
study
the
synthesis
new
antibiotics
control
disease-causing
effects
infectious
pathogens.
Antimicrobial
peptides
(AMPs)
are
among
newest
antibiotics;
these
integral
compounds
in
all
kinds
organisms
and
play
a
significant
role
microbial
ecology,
critically
contribute
innate
immunity
by
destroying
invading
microorganisms.
Moreover,
AMPs
may
encourage
cells
produce
chemokines,
stimulate
angiogenesis,
accelerate
wound
healing,
influence
programmed
cell
death
multicellular
organisms.
Bacteria
differ
their
inherent
susceptibility
mechanisms
when
responding
antimicrobial
AMPs.
Generally,
development
AMP
is
driven
direct
competition
between
bacterial
species,
host
pathogen
interactions.
Several
studies
shown
diverse
AMPs,
for
example,
some
bacteria
proteases
trapping
proteins;
modify
surface
charge,
change
membrane
fluidity,
activate
efflux
pumps;
species
make
use
biofilms
exopolymers,
develop
sensing
systems
selective
gene
expression.
A
closer
understanding
help
developing
novel
therapeutic
approaches
treatment
infections
caused
pathogenic
that
successful
extensive
Based
on
observations,
this
review
discusses
properties
targeting
mechanisms,
against
Abstract
Overuse
of
conventional
antibiotics
as
well
the
slow
pace
new
antibiotic
drug
development
leads
to
antimicrobial
resistance
(AMR).
Because
infections
with
multi‐drug
resistant
(MDR)
pathogens
have
become
a
public
health
issue,
need
for
novel
class
is
urgent.
Recently,
peptides
(AMPs)
emerged
promising
platform
fight
against
MDR
bacteria
ensuring
broad‐spectrum
activity
and
relatively
low
emergence.
Currently,
number
AMPs
are
undergoing
clinical
preclinical
trials
various
infectious
diseases.
This
review
lists
36
(27
9
preclinical)
brief
information
about
their
origin,
structure,
mechanism,
status.
From
examples
under
investigation,
we
categorized
several
improvement
strategies
highlighted
directions
future
design
AMPs.
Frontiers in Chemistry,
Год журнала:
2019,
Номер
7
Опубликована: Фев. 4, 2019
Current
research
has
demonstrated
that
small
cationic
amphipathic
peptides
have
strong
potential
not
only
as
antimicrobials,
but
also
antibiofilm
agents,
immune
modulators,
and
anti-inflammatories.
Although
traditionally
termed
antimicrobial
(AMPs)
these
additional
roles
prompted
a
shift
in
terminology
to
use
the
broader
term
host
defense
(HDPs)
capture
multi-functional
nature
of
molecules.
In
this
review,
we
critically
examined
role
AMPs
HDPs
infectious
diseases
inflammation.
It
is
generally
accepted
are
multi-faceted
mediators
wide
range
biological
processes,
with
individual
activities
dependent
on
their
polypeptide
sequence.
context,
explore
concept
chemical
space
it
applies
hypothesize
various
functions
class
molecule
exist
independent
overlapping
activity
landscapes.
Finally,
outline
several
emerging
highlight
how
an
improved
understanding
processes
can
potentially
be
leveraged
more
fully
realize
therapeutic
promise
HDPs.
Frontiers in Microbiology,
Год журнала:
2021,
Номер
12
Опубликована: Фев. 22, 2021
Antimicrobial
peptides
(AMPs)
or
host
defense
protect
the
against
various
pathogens
such
as
yeast,
fungi,
viruses
and
bacteria.
AMPs
also
display
immunomodulatory
properties
ranging
from
modulation
of
inflammatory
responses
to
promotion
wound
healing.
More
interestingly,
cause
cell
disruption
through
non-specific
interactions
with
membrane
surface
pathogens.
This
is
most
likely
responsible
for
low
limited
emergence
bacterial
resistance
many
AMPs.
Despite
increasing
number
antibiotic-resistant
bacteria
potency
novel
combat
pathogens,
only
a
few
are
in
clinical
use.
Therefore,
current
review
describes
(i)
potential
alternatives
antibiotics,
(ii)
challenges
toward
implementation
(iii)
strategies
improve
success
rate
trials,
emphasizing
lessons
we
could
learn
these
trials.
Nature Communications,
Год журнала:
2019,
Номер
10(1)
Опубликована: Окт. 4, 2019
Abstract
Antimicrobial
peptides
(AMPs)
are
promising
antimicrobials,
however,
the
potential
of
bacterial
resistance
is
a
major
concern.
Here
we
systematically
study
evolution
to
14
chemically
diverse
AMPs
and
12
antibiotics
in
Escherichia
coli
.
Our
work
indicates
that
against
certain
AMPs,
such
as
tachyplesin
II
cecropin
P1,
limited.
Resistance
level
provided
by
point
mutations
gene
amplification
very
low
antibiotic-resistant
bacteria
display
no
cross-resistance
these
AMPs.
Moreover,
genomic
fragments
derived
from
wide
range
soil
confer
detectable
when
introduced
into
native
host
on
plasmids.
We
have
found
simple
physicochemical
features
dictate
propensity
evolve
could
serve
source
for
development
new
AMP-based
therapeutics
less
prone
resistance,
feature
necessary
avoid
any
possible
interference
with
our
innate
immune
system.
