Frontiers in Molecular Neuroscience,
Journal Year:
2023,
Volume and Issue:
16
Published: Nov. 30, 2023
The
prevalence
of
allergic
conjunctivitis
in
itchy
eyes
has
increased
constantly
worldwide
owing
to
environmental
pollution.
Currently,
anti-allergic
and
antihistaminic
eye
drops
are
used;
however,
there
many
unknown
aspects
about
the
neural
circuits
that
transmit
eyes.
We
focused
on
gastrin-releasing
peptide
(GRP)
GRP
receptor
(GRPR),
which
reportedly
involved
itch
transmission
spinal
somatosensory
system,
determine
whether
system
is
neurotransmission
trigeminal
sensory
system.
First,
instillation
mediators,
such
as
histamine
(His)
non-histaminergic
mediator
chloroquine
(CQ),
exhibited
concentration-dependent
high
levels
scratching
behavior,
with
a
significant
sex
differences
observed
case
His.
Histological
analysis
revealed
His
CQ
significantly
activity
GRPR-expressing
neurons
caudal
part
nucleus
medulla
oblongata
GRPR
transgenic
mice.
administered
antagonist
or
bombesin-saporin
ablate
neurons,
followed
by
instillation,
decrease
CQ-induced
eye-scratching
behavior
toxin
experiments.
Intracisternal
administration
neuromedin
C
(NMC),
agonist,
resulted
dose-dependent
excessive
facial
despite
absence
an
stimulus
face.
To
our
knowledge,
this
first
study
demonstrate
were
transmitted
centrally
via
NMC
evoked
itching.
Current Cancer Drug Targets,
Journal Year:
2024,
Volume and Issue:
24(12), P. 1275 - 1285
Published: Feb. 15, 2024
Background:
Bombesin
(BBN)
is
a
short
peptide
with
high
affinity
for
receptors
that
are
expressed
on
the
surface
of
various
types
cancer
cells.
However,
full
length
BBN
molecule
has
low
in
vivo
stability.
Objective:
In
our
study,
we
propose
use
toxins,
derived
from
animal
and
plant
as
scaffold
molecules
to
enhance
bioavailability
stability
bombesin.
These
peptides
possess
unique
structure
known
an
inhibitory
cystine
knot.
Methods:
We
synthesized
structures
which
bombesin
was
incorporated
into
domains
arthropod
toxins
using
solid-phase
synthesis.
The
under
different
conditions
assessed
through
high-performance
liquid
chromatography,
binding
cell
cultures
expressing
receptor
analyzed.
Additionally,
toxicity
evaluated
fluorescence
microscopy.
Results:
data
obtained
demonstrated
placing
between
first
second
cysteine
residues
arachnid
results
increased
vitro
bioavailability,
well
cytotoxicity.
Conclusion:
Arachnid
knot
can
be
considered
increasing
therapeutic
peptides.
Forum Dermatologicum,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Sept. 3, 2024
Itch
is
an
unpleasant
sensation
on
the
skin
that
causes
desire
to
scratch.
Its
aetiology
can
be
defined
by
various
categories
such
as
cause,
period
of
occurrence,
location,
and
presence
or
absence
disease
in
a
given
area.
This
burdensome
symptom
experience
even
compared
chronic
pain
terms
quality-of-life-impairment
particularly
common
among
older
people.
article
discusses
neural
pathways
cause
itch,
important
but
clinically
challenging
role
histamine,
some
mechanisms
involved
itch-scratch
cycle,
quite
novel
discoveries
regarding
contributions
gastrin-releasing
peptide
(GRP)/
receptor
(GRPR)
axis,
transient
potential
(TRP)
channels,
Janus
kinase.
Pruritus
may
associated
with
types
diseases
affecting
maternal-foetal
relationship,
skin,
cholestasis,
renal
system
mental
health.
Some
new
therapeutic
options
include
drugs
affect
opioid
receptors,
neurokinin
1
(NK-1R)
antagonists,
kinase
inhibitors,
biologics
made
combining
antibodies
against
different
interleukins
itch
sensation.
Nevertheless,
finding
effective
form
therapy
for
patients
underlying
conditions
remains
challenge
subject
ongoing
clinical
research.
bioRxiv (Cold Spring Harbor Laboratory),
Journal Year:
2024,
Volume and Issue:
unknown
Published: Sept. 15, 2024
Abstract
G
protein-coupled
receptors
(GPCRs)
play
pivotal
roles
in
cellular
signaling
and
represent
prominent
drug
targets.
Structural
elucidation
of
GPCRs
is
crucial
for
discovery
efforts.
However,
structural
studies
remain
challenging,
particularly
inactive
state
structures,
which
often
require
extensive
protein
engineering.
Here,
we
present
a
de
novo
design
strategy
termed
“click
fusion”
generating
fusion
proteins
to
facilitate
GPCR
studies.
Our
method
involves
the
rational
structurally
stable
domains
rigidly
linked
GPCRs.
The
resulting
enhances
thermostability
target
aids
determining
structures
via
cryo-electron
microscopy
(cryo-EM).
We
further
demonstrate
that
designed
can
be
transferred
among
similar
with
minor
adjustments
linker
region.
study
introduces
promising
approach
facilitating
advancing
Frontiers in Molecular Neuroscience,
Journal Year:
2023,
Volume and Issue:
16
Published: Nov. 30, 2023
The
prevalence
of
allergic
conjunctivitis
in
itchy
eyes
has
increased
constantly
worldwide
owing
to
environmental
pollution.
Currently,
anti-allergic
and
antihistaminic
eye
drops
are
used;
however,
there
many
unknown
aspects
about
the
neural
circuits
that
transmit
eyes.
We
focused
on
gastrin-releasing
peptide
(GRP)
GRP
receptor
(GRPR),
which
reportedly
involved
itch
transmission
spinal
somatosensory
system,
determine
whether
system
is
neurotransmission
trigeminal
sensory
system.
First,
instillation
mediators,
such
as
histamine
(His)
non-histaminergic
mediator
chloroquine
(CQ),
exhibited
concentration-dependent
high
levels
scratching
behavior,
with
a
significant
sex
differences
observed
case
His.
Histological
analysis
revealed
His
CQ
significantly
activity
GRPR-expressing
neurons
caudal
part
nucleus
medulla
oblongata
GRPR
transgenic
mice.
administered
antagonist
or
bombesin-saporin
ablate
neurons,
followed
by
instillation,
decrease
CQ-induced
eye-scratching
behavior
toxin
experiments.
Intracisternal
administration
neuromedin
C
(NMC),
agonist,
resulted
dose-dependent
excessive
facial
despite
absence
an
stimulus
face.
To
our
knowledge,
this
first
study
demonstrate
were
transmitted
centrally
via
NMC
evoked
itching.