Takeda G protein–coupled receptor 5 (TGR5): an attractive therapeutic target for aging-related cardiovascular diseases
Frontiers in Pharmacology,
Год журнала:
2025,
Номер
16
Опубликована: Март 20, 2025
Aging
is
an
independent
risk
factor
for
many
chronic
diseases,
including
cancer
and
cardiovascular,
pulmonary,
neurodegenerative
diseases.
In
recent
years,
the
mechanisms
of
aging-related
cardiovascular
diseases
(CVDs)
have
been
studied
intensively.
Takeda
G
protein-coupled
receptor
5
(TGR5)
a
membrane
bile
acids
that
has
found
to
play
important
role
in
various
disease
processes,
such
as
inflammation,
oxidative
stress,
metabolic
disorders,
all
which
contribute
CVDs.
this
review,
we
summarise
TGR5
CVDs
propose
attractive
therapeutic
target
based
on
its
mechanism
involvement,
may
future
drug
design.
Язык: Английский
Salidroside attenuates NASH through regulating bile acid-FXR/TGR5 signaling pathway via targeting gut microbiota
International Journal of Biological Macromolecules,
Год журнала:
2025,
Номер
unknown, С. 142276 - 142276
Опубликована: Март 1, 2025
Язык: Английский
Function and therapeutic potential of Amuc_1100, an outer membrane protein of Akkermansia muciniphila: A review
International Journal of Biological Macromolecules,
Год журнала:
2025,
Номер
unknown, С. 142442 - 142442
Опубликована: Март 1, 2025
Язык: Английский
A perspective on thrombogenesis through gut microbiota-derived bile acids and platelet activation
Nature Cardiovascular Research,
Год журнала:
2025,
Номер
unknown
Опубликована: Апрель 11, 2025
Язык: Английский
Crosstalk Between Bile Acids and Intestinal Epithelium: Multidimensional Roles of Farnesoid X Receptor and Takeda G Protein Receptor 5
International Journal of Molecular Sciences,
Год журнала:
2025,
Номер
26(9), С. 4240 - 4240
Опубликована: Апрель 29, 2025
Bile
acids
and
their
corresponding
intestinal
epithelial
receptors,
the
farnesoid
X
receptor
(FXR),
G
protein-coupled
bile
acid
(TGR5),
play
crucial
roles
in
physiological
pathological
processes
of
cells.
These
receptors
are
involved
regulation
absorption,
signal
transduction,
cellular
proliferation
repair,
senescence,
energy
metabolism,
modulation
gut
microbiota.
A
comprehensive
literature
search
was
conducted
using
PubMed,
employing
keywords
such
as
acid,
receptor,
FXR
(nr1h4),
TGR5
(gpbar1),
cells,
proliferation,
differentiation,
microbiota,
inflammatory
bowel
disease
(IBD),
colorectal
cancer
(CRC),
irritable
syndrome
(IBS),
with
a
focus
on
publications
available
English.
This
review
examines
diverse
effects
signaling
pathways
metabolism
Additionally,
it
explores
interactions
between
acids,
well
implications
these
for
host
health,
particularly
relation
to
prevalent
diseases.
Finally,
highlights
importance
developing
highly
specific
ligands
context
metabolic
disorders.
Язык: Английский
The functions of gut microbiota-mediated bile acid metabolism in intestinal immunity
Journal of Advanced Research,
Год журнала:
2025,
Номер
unknown
Опубликована: Май 1, 2025
Bile
acids,
derived
from
cholesterol
in
the
liver,
consist
a
steroidal
core.
Primary
bile
acids
and
secondary
metabolized
by
gut
microbiota
make
up
acid
pool,
which
modulate
nuclear
hormone
receptors
to
regulate
immunity.
Disruptions
crosstalk
between
flora
are
intimately
associated
with
development
course
of
gastrointestinal
inflammation.
This
review
provides
an
extensive
summary
production,
transport
metabolism.
It
also
delves
into
impact
metabolism
on
body
explores
involvement
acid-microbiota
interactions
various
disease
states.
Furthermore,
potential
targeting
signaling
as
means
prevent
treat
inflammatory
bowel
is
proposed.
In
this
review,
we
primarily
address
functions
diseases.
Firstly,
summarize
signalling
factors
influencing
metabolism,
highlighting
immune
function
microbially
conjugated
unique
roles
different
receptors.
Subsequently,
emphasize
vital
role
maintaining
healthy
regulating
intestinal
barrier
function,
energy
Finally
explore
differences
states,
offering
new
perspectives
restoring
host's
health
ecosystem
microbiota-bile
acid-bile
receptor
axis.
Язык: Английский
Design, Synthesis, and Biological Evaluation of Covalently Mucoadhesive Derivatives as Nonsystemic Intestine-Targeted TGR5 Agonists
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
unknown
Опубликована: Сен. 25, 2024
Takeda
G-protein-coupled
receptor
5
(TGR5)
is
considered
a
promising
therapeutic
target
for
treating
type
2
diabetes
mellitus
(T2DM),
obesity,
and
other
metabolism-related
diseases.
Although
many
TGR5
agonists
have
been
identified,
they
might
cause
some
side
effects
in
the
gallbladder
heart.
To
reduce
these
improve
glucose-lowering
capability,
we
first
designed
synthesized
series
of
4-phenoxynicotinamide
intestine-targeted
agonist
derivatives
containing
maleimides
chains
with
different
linker
lengths.
All
compounds
demonstrated
significant
agonistic
activity,
among
which
compound
Язык: Английский
Ramulus Mori (Sangzhi) alkaloids ameliorate high-fat diet induced obesity in rats by modulating gut microbiota and bile acid metabolism
Frontiers in Endocrinology,
Год журнала:
2024,
Номер
15
Опубликована: Дек. 20, 2024
The
objective
of
this
study
is
to
investigate
the
ability
Ramulus
Mori
(Sangzhi)
alkaloid
tablets
(SZ-A)
ameliorate
obesity
and
lipid
metabolism
disorders
in
rats
subjected
a
high-fat
diet
(HFD)
through
metagenomics,
untargeted
lipidomics,
targeted
bile
acid
(BA),
BA
pathways,
providing
novel
perspective
on
management
metabolic
disorders.
Язык: Английский