The Journal of Physiology,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Nov. 22, 2024
Abstract
The
incretin
hormones
glucagon‐like
peptide‐1
(GLP‐1)
and
glucose‐dependent
insulinotropic
polypeptide
(GIP)
play
critical
roles
in
co‐ordinating
postprandial
metabolism,
including
modulation
of
insulin
secretion
food
intake.
They
are
secreted
from
enteroendocrine
cells
the
intestinal
epithelium
following
ingestion,
act
at
multiple
target
sites
pancreatic
islets
brain.
With
recent
development
agonists
targeting
GLP‐1
GIP
receptors
for
treatment
type
2
diabetes
obesity,
ongoing
new
incretin‐based
drugs
with
improved
efficacy,
there
is
great
interest
understanding
physiology
pharmacology
these
hormones.
image
Molecular Metabolism,
Journal Year:
2025,
Volume and Issue:
95, P. 102118 - 102118
Published: Feb. 28, 2025
Glucose-dependent
insulinotropic
polypeptide
(GIP)
was
the
first
incretin
identified
and
plays
an
essential
role
in
maintenance
of
glucose
tolerance
healthy
humans.
Until
recently
GIP
had
not
been
developed
as
a
therapeutic
thus
has
overshadowed
by
other
incretin,
glucagon-like
peptide
1
(GLP-1),
which
is
basis
for
several
successful
drugs
to
treat
diabetes
obesity.
However,
there
rekindling
interest
biology
recent
years,
great
part
due
pharmacology
demonstrating
that
both
GIPR
agonism
antagonism
may
be
beneficial
treating
obesity
diabetes.
This
apparent
paradox
reinvigorated
field,
led
new
lines
investigation,
deeper
understanding
GIP.
In
this
review,
we
provide
detailed
overview
on
multifaceted
nature
discuss
implications
signal
modification
various
diseases.
Following
its
classification
hormone,
emerged
pleiotropic
hormone
with
variety
metabolic
effects
outside
endocrine
pancreas.
The
numerous
render
interesting
candidate
development
pharmacotherapies
obesity,
diabetes,
drug-induced
nausea
bone
neurodegenerative
disorders.
Frontiers in Endocrinology,
Journal Year:
2025,
Volume and Issue:
16
Published: March 17, 2025
Glucose-dependent
insulinotropic
polypeptide
(GIP)
is
one
of
two
incretin
hormones
playing
key
roles
in
the
control
food
intake,
nutrient
assimilation,
insulin
secretion
and
whole-body
metabolism.
Recent
pharmacological
advances
clinical
trials
show
that
unimolecular
co-agonists
target
receptors
for
incretins
-
GIP
glucagon-like
peptide
1
(GLP-1)
offer
more
effective
treatment
strategies
obesity
type
2
diabetes
mellitus
(T2D)
compared
with
GLP-1
receptor
(GLP1R)
agonists
alone,
suggesting
previously
underappreciated
regulating
intake
body
weight.
The
mechanisms
by
which
regulates
energy
balance
remain
controversial
as
both
agonism
antagonism
(GIPR)
produce
weight
loss
improve
metabolic
outcomes
preclinical
models.
studies
have
shown
GIPR
signalling
central
nervous
system
(CNS),
especially
regions
brain
regulate
balance,
essential
its
action
on
appetite
regulation.
This
finding
has
sparked
interest
understanding
engages
circuits
to
reduce
In
this
review,
we
present
knowledge
around
actions
regulation
potential
GIPR/GLP1R
may
balance.
Diabetes Obesity and Metabolism,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Nov. 26, 2024
Abstract
Obesity
is
a
chronic
condition
demanding
effective
treatment
strategies,
among
which
pharmacotherapy
plays
critical
role.
As
glucagon‐like
peptide‐1
(GLP‐1)
agonist
approved
by
the
Food
and
Drug
Administration
(FDA)
for
long‐term
weight
management
in
adults
with
obesity,
liraglutide
semaglutide
have
great
loss
effect
through
reducing
food
intake
delaying
gastric
emptying.
The
emergence
of
unimolecular
polypharmacology,
utilizes
single
molecules
to
simultaneously
target
multiple
receptors
or
pathways,
marked
revolutionary
improvement
GLP‐1‐based
obesity
pharmacotherapy.
dual
tirzepatide
activates
both
GLP‐1
glucose‐dependent
insulinotropic
polypeptide
(GIP)
has
shown
enhanced
potency
compared
conventional
mono
agonist.
Furthermore,
emerging
data
suggests
that
GLP‐1/glucagon
(GCG)
agonist,
as
well
GLP‐1/GIP/GCG
triple
may
offer
superior
efficacy
over
This
review
summarizes
comprehensive
mechanisms
underlying
pronounced
advantages
GLP‐1/GIP
GLP‐1/GCG
reduction
obese
without
type
2
diabetes.
A
deeper
understanding
these
multitargeting
agonists
will
provide
insights
their
clinical
application
guide
development
new
drugs
treatment.
