Cysteine-Specific 18F and NIR Dual Labeling of Peptides via Vinyltetrazine Bioorthogonal Conjugation for Molecular Imaging
Journal of Medicinal Chemistry,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 4, 2025
Radiolabeled
peptides
are
vital
for
positron
emission
tomography
(PET)
imaging,
yet
the
18F-labeling
remain
challenging
due
to
harsh
conditions
and
time-consuming
premodification
requirements.
Herein,
we
developed
a
novel
vinyltetrazine-mediated
bioorthogonal
approach
highly
efficient
18F-radiolabeling
of
native
peptide
under
mild
conditions.
This
enabled
radiosynthesis
various
tumor-targeting
PET
tracers,
including
targeting
neurofibromin
receptor
(18F-P10a),
integrin
αvβ3
(18F-P12a),
platelet-derived
growth
factor
β
(18F-ZPDGFRβ),
with
radiochemical
yield
exceeding
90%.
Preliminary
evaluations
revealed
excellent
hydrophilicity
across
these
18F-P12a
effectively
visualizing
expression
(tumor
uptake:
1.57
±
0.54%ID/g
at
2
h).
Additionally,
explored
potential
development
PET/near-infrared
(NIR)
dual-labeling
agents
using
this
method.
The
dual-modality
agent
18F-Cy5-P12d
enables
specificity
colocalized
imaging
1.35
0.24%ID/g
Overall,
strategy
offers
versatile
platform
radiolabeling
development.
Язык: Английский
Advances in prostate-specific membrane antigen-targeted theranostics: from radionuclides to near-infrared fluorescence technology
Frontiers in Immunology,
Год журнала:
2025,
Номер
15
Опубликована: Янв. 10, 2025
Prostate-Specific
Membrane
Antigen
(PSMA)
is
a
highly
expressed
and
structurally
unique
target
specific
to
prostate
cancer
(PCa).
Diagnostic
therapeutic
approaches
in
nuclear
medicine,
coupling
PSMA
ligands
with
radionuclides,
have
shown
significant
clinical
success.
PSMA-PET/CT
effectively
identifies
tumors
metastatic
lymph
nodes
for
imaging
purposes,
while
177Lu-PSMA-617
(Pluvicto)
has
received
FDA
approval
treating
castration-resistant
PCa
(mCRPC).
Despite
their
success,
radionuclide-based
diagnostic
methods
face
limitations
such
as
high
costs
side
effects.
Recently,
near-infrared
(NIR)
fluorescence
phototherapy
advanced
significantly
biomedical
applications.
It's
benefits,
deep
tissue
penetration,
real-time
precision,
minimal
effects,
driven
broader
adoption,
especially
fluorescence-guided
surgery
(FGS).
This
review
suggests
combining
NIR
dyes
enable
targeted,
high-resolution
superior
signal-to-background
ratios,
facilitating
precise
FGS.
techniques
can
also
aid
pathological
diagnosis
ex
vivo
specimens.
Furthermore,
photosensitizers
allows
localized
photothermal
(PTT)
or
photodynamic
therapy
(PDT)
under
irradiation,
producing
heat
reactive
oxygen
species
(ROS)
treat
PCa.
aims
extend
the
success
of
targeting
by
exploring
advances
NIR-based
FGS
phototherapy,
presenting
promising
new
approach.
Язык: Английский
Gastrin-Releasing Peptide Receptor Targeting PET/CT With 68Ga-NOTA-RM26 in the Assessment of Glioma and Combined Multiregional Biopsies
Clinical Nuclear Medicine,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 14, 2025
Purpose
The
aim
of
this
study
was
to
investigate
the
value
68
Ga-NOTA-RM26
(
Ga-RM26),
a
gastrin-releasing
peptide
receptor–targeting
antagonist
labeled
with
radionuclide
Ga,
in
diagnosis
high-grade
gliomas
and
combination
multiregional
biopsies
using
PET/CT.
Patients
Methods
After
institutional
review
board
approval
informed
consent,
total
35
patients
suspected
glioma
lesions
were
enrolled
study.
All
underwent
Ga-RM26
PET/CT
scans
within
2
weeks
before
surgery.
Results
There
8
grade
II
gliomas,
6
III
18
IV
32
lesions.
diagnosed
74.4%
(27/32)
all
tumor
types,
almost
successfully
(23/24,
95.8%).
Among
9
negative
lesions,
there
low-grade
(grade
II).
significantly
higher
SUV
max
,
mean
lesion-to-background
ratio
(T/B
ratio)
compared
P
<
0.001).
In
addition,
high
correlation
between
immunohistochemical
staining
score
parameters
(SUV
T/B
on
0.001),
verified
by
multiple-point
samples
guided
Conclusions
could
noninvasively
diagnose
be
promising
PET
tracer
for
predicting
grading
This
pilot
indicated
that
uptake
correlates
WHO
glioma,
preoperative
may
helpful
guide
biopsy
gliomas.
Язык: Английский
Imaging Strategies for Delineating Glioma Margins: Aiming at Precise Therapy
Fundamental Research,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 1, 2025
Язык: Английский
Dual-Labeled Small Peptides in Cancer Imaging and Fluorescence-Guided Surgery: Progress and Future Perspectives
Pharmaceuticals,
Год журнала:
2025,
Номер
18(2), С. 143 - 143
Опубликована: Янв. 22, 2025
Dual-labeled
compounds
that
combine
radiolabeling
and
fluorescence
labeling
represent
a
significant
advancement
in
precision
oncology.
Their
clinical
implementation
enhances
patient
care
outcomes
by
leveraging
the
high
sensitivity
of
radioimaging
for
tumor
detection
taking
advantage
fluorescence-based
optical
visualization
surgical
guidance.
Non-invasive
facilitates
immediate
identification
both
primary
tumors
metastases,
while
imaging
assists
decision-making
during
surgery
offering
spatial
distinction
between
malignant
non-malignant
tissue.
These
advancements
hold
promise
enhancing
personalization
cancer
treatment.
The
development
dual-labeled
molecular
probes
targeting
various
biomarkers
is
crucial
addressing
heterogeneity
inherent
pathology
recent
studies
had
already
demonstrated
impact
(NCT03699332,
NCT03407781).
This
review
focuses
on
application
small
peptides
treatment
types.
It
summarizes
targeted
to
date,
tracing
their
from
initial
discovery
latest
peptidomimetics.
Through
comprehensive
analysis
preclinical
studies,
demonstrates
potential
these
improve
detection,
localization,
resection.
Additionally,
it
highlights
evolving
landscape
dual-modality
imaging,
emphasizing
its
critical
role
advancing
personalized
effective
therapy.
synthesis
current
research
underscores
diagnostic
accuracy
therapeutic
Язык: Английский
Diagnostic Value of Gastrin-Releasing Peptide Receptor-Targeted PET Imaging in Oncology: A Systematic Review
Seminars in Nuclear Medicine,
Год журнала:
2025,
Номер
unknown
Опубликована: Янв. 1, 2025
Язык: Английский
Predicting intraoperative 5-ALA-induced tumor fluorescence via MRI and deep learning in gliomas with radiographic lower-grade characteristics
Journal of Neuro-Oncology,
Год журнала:
2024,
Номер
171(3), С. 589 - 598
Опубликована: Ноя. 19, 2024
Abstract
Purpose
Lower-grade
gliomas
typically
exhibit
5-aminolevulinic
acid
(5-ALA)-induced
fluorescence
in
only
20–30%
of
cases,
a
rate
that
can
be
increased
by
doubling
the
administered
dose
5-ALA.
Fluorescence
depict
anaplastic
foci,
which
precisely
sampled
to
avoid
undergrading.
We
aimed
analyze
whether
deep
learning
model
could
predict
intraoperative
based
on
preoperative
magnetic
resonance
imaging
(MRI).
Methods
evaluated
cohort
163
glioma
patients
categorized
intraoperatively
as
fluorescent
(n
=
83)
or
non-fluorescent
80).
The
MR
images
lacking
high-grade
characteristics
(e.g.,
necrosis
irregular
ring
contrast-enhancement)
consisted
T1,
T1-post
gadolinium,
and
FLAIR
sequences.
preprocessed
MRIs
were
fed
into
an
encoder-decoder
convolutional
neural
network
(U-Net),
pre-trained
for
tumor
segmentation
using
those
three
MRI
used
outputs
bottleneck
layer
U-Net
Variational
Autoencoder
(VAE)
features
classification.
identified
utilized
most
effective
Random
Forest
classifier
principal
component
analysis
(PCA)
partial
least
square
discriminant
(PLS-DA)
algorithms.
performance
tenfold
cross-validation
procedure.
Results
Our
proposed
approach's
was
assessed
mean
balanced
accuracy,
sensitivity,
specificity.
optimal
results
obtained
employing
top-performing
selected
PCA,
resulting
accuracy
80%
sensitivity
specificity
84%
76%,
respectively.
Conclusions
findings
highlight
potential
model,
coupled
with
classifier,
pre-operative
prediction
fluorescence.
achieved
high
extracted
brain
segmentation.
While
still
improved,
it
has
evaluating
when
administer
5-ALA
typical
radiographic
features.
Graphical
abstract
Язык: Английский
Advancements in nanotechnology for diagnostics: a literature review, part II: advanced techniques in nuclear and optical imaging
Nanomedicine,
Год журнала:
2024,
Номер
unknown, С. 1 - 24
Опубликована: Дек. 13, 2024
Modern
molecular
imaging
routes,
such
as
nuclear
and
optical
imaging,
derive
significant
advantages
from
nanoparticles,
where
multimodality
use
multipurpose
are
key
benefits.
Nanoparticles
also
showcase
benefits
over
traditional
agents
in
including
improved
resolution,
penetration,
specificity.
The
goal
of
this
literature
review
was
to
explore
recent
advancements
nanomaterials
within
these
techniques
expand
on
the
current
state
nanomedicine
modalities.
This
derives
findings
relevant
reviews,
original
research
papers,
in-human
clinical
trials,
patents
literature.
Au-
Fe
oxide-based
nanosystems
just
ubiquitous
more
modern
modalities
due
their
multimodal
diagnostic
therapeutic
potential.
It
is
repeatedly
highlighted
literature,
patents,
trials
that
specifically
theranostics,
present
innovative
methods
years,
enabling
researchers
clinicians
overcome
limitations
unimodal
further
advancing
accuracy
diagnosis
treatment
important
pathologies,
particularly
cancer.
Overall,
nanoparticle-based
represents
a
transformative
approach
advanced
modalities,
offering
new
approaches
conventional
currently
being
applied
settings.
Язык: Английский