Development of 99mTc-Labeled Complexes with a Niraparib HYNIC Derivative for PARP-Positive Tumor Imaging
Molecular Pharmaceutics,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 8, 2025
As
an
enzyme
that
plays
important
role
in
DNA
repair,
poly(ADP-ribose)
polymerase-1
(PARP-1)
has
become
a
popular
target
for
cancer
therapy.
Nuclear
medicine
molecular
imaging
technology,
supplemented
by
radiolabeled
PARP-1
inhibitors,
can
accurately
determine
the
expression
level
of
at
lesion
sites
to
help
patients
choose
appropriate
treatment
plan.
In
this
work,
niraparib
was
modified
with
hydrazinonicotinamide
(HYNIC)
group
generate
ligand
NPBHYNIC,
which
vitro
affinity
(IC50)
450.90
nM
PARP-1.
The
NPBHYNIC
labeled
technetium-99m
and
six
different
coligands
yield
[99mTc]Tc-(X/tricine)-NPBHYNIC
(X
=
TPPTS,
TPPMS,
PSA,
PDA,
NIC
ISONIC).
These
complexes
were
hydrophilic
exhibited
good
stability
vitro,
low
levels
these
taken
up
nontarget
organs
tissues
Kunming
mice.
Among
complexes,
[99mTc]Tc-(TPPTS/tricine)-NPBHYNIC
[99mTc]Tc-(NIC/tricine)-NPBHYNIC
selected
biodistribution
HeLa
tumor-bearing
BALB/c
nude
mice
2
h
post
injection.
results
revealed
tumor
uptake
(1.02
±
0.07%
ID/g)
greater
than
(0.36
0.05%
ID/g).
Additionally,
biodistribution,
single-photon
emission
computed
tomography/computed
tomography
(SPECT/CT)
radioautography
experiments,
significantly
reduced
blocked
group,
indicating
specificity.
Therefore,
it
potential
use
as
niraparib-based
agent
targets
Язык: Английский
Development of Novel 99mTc-Labeled Hydrazinoicotinamide-Modified Ubiquicidin 29-41 Complexes with Improved Target-to-Nontarget Ratios for Bacterial Infection Imaging
Yuhao Jiang,
Qianna Wang,
Guangxing Yin
и другие.
ACS Pharmacology & Translational Science,
Год журнала:
2025,
Номер
8(2), С. 470 - 483
Опубликована: Фев. 4, 2025
To
develop
novel
99mTc-labeled
ubiquicidin
29-41
derivatives
for
bacterial
infection
SPECT
imaging
aiming
at
achieving
a
high
target-to-nontarget
ratio
and
lower
nontarget
organ
uptake,
6-hydrazinoicotinamide
(HYNIC)
derivative
(HYNIC-UBI
29-41)
was
designed
synthesized.
It
then
radiolabeled
with
ternary
ligands,
including
TPPTS,
PDA,
2,6-PDA,
NIC,
ISONIC,
PSA,
4-PSA,
PES,
to
obtain
eight
HYNIC-UBI
complexes.
All
the
complexes
demonstrated
hydrophilicity,
exhibited
good
in
vitro
stability,
specifically
bound
Staphylococcus
aureus
vitro.
Biodistribution
studies
mice
that
[99mTc]Tc-tricine/TPPTS-HYNIC-UBI
resulted
increased
abscess-to-muscle
abscess-to-blood
ratios
as
well
decreased
uptake.
Furthermore,
it
able
distinguish
between
sterile
inflammation.
Single-photon
emission
computed
tomography
(SPECT)
revealed
visible
accumulation
site
of
infection,
indicating
is
potential
radiotracer
infection.
Язык: Английский
Synthesis and Evaluation of 99mTc-Labeled DPro-Gly-Containing Tracers Targeting PSMA
Molecular Pharmaceutics,
Год журнала:
2024,
Номер
unknown
Опубликована: Сен. 19, 2024
The
specific
expression
of
prostate-specific
membrane
antigen
(PSMA)
makes
it
an
ideal
target
for
the
diagnosis
and
treatment
prostate
cancer.
Currently,
many
Язык: Английский
Synthesis and Evaluation of 99mTc-Labeled l-Aspartic Acid as a EuK Polymer Linker for Targeting PSMA to a Novel SPECT Tumor Tracer
Journal of Medicinal Chemistry,
Год журнала:
2024,
Номер
67(23), С. 21617 - 21628
Опубликована: Дек. 3, 2024
The
development
of
novel
tracers
targeting
prostate-specific
membrane
antigen
(PSMA)
has
great
potential
for
improving
the
diagnosis
and
treatment
prostate
cancer
(PCa).
This
study
aimed
to
improve
absolute
tumor
uptake
tumor-to-background
ratios
(TBRs)
this
PSMA
tracer
by
increasing
number
pharmacophores,
Glu-urea-Lys
(EuK),
that
specifically
bind
PSMA.
We
successfully
synthesized
four
radioligands
prepared
a
total
12
stable
radiotracers
coordinating
Язык: Английский