Bioconjugate Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: May 12, 2025
Click
chemistry
to
allow
in
vivo
conjugation
of
a
fluorophore
porphyrin
(Por)-tetrazine
(Tz)
with
the
human
epidermal
growth
factor
receptor
2
(HER2)-targeting
trastuzumab
conjugated
trans-cyclooctene
(TCO)
is
described
here.
In
vitro
experiments
confirmed
successful
click
reactions
between
Por-Tz
and
trastuzumab-TCO
validated
preserved
immunoreactivity
(no
significant
change
HER2
binding,
p
>
0.05).
Positron
emission
tomography
(PET)
[89Zr]Zr-DFO-trastuzumab-TCO
demonstrated
17.1
±
2.9%
injected
dose
per
gram
tumor
at
48
h
postinjection.
Optical
imaging
showed
an
∼10-fold
increase
group
for
when
compared
alone.
This
preclinical
data
demonstrate
pretargeted
approach
dual
PET
optical
HER2-expressing
tumors.
Angewandte Chemie International Edition,
Journal Year:
2023,
Volume and Issue:
62(33)
Published: May 11, 2023
Photoresponsive
materials
offer
excellent
spatiotemporal
control
over
biological
processes
and
the
emerging
phototherapeutic
methods
are
expected
to
have
significant
effects
on
targeted
cancer
therapies.
Recent
examples
show
that
combination
of
photoactivatable
approaches
with
bioorthogonal
chemistry
enhances
precision
phototherapies
profound
implications
foreseen
particularly
in
treatment
disperse/diffuse
tumors.
The
extra
level
on-target
selectivity
improved
spatial/temporal
considerably
intensified
related
bioorthogonally
assisted
phototherapy
research.
anticipated
growth
further
developments
field
justifies
timeliness
a
brief
summary
state
art.
RSC Advances,
Journal Year:
2024,
Volume and Issue:
14(11), P. 7383 - 7413
Published: Jan. 1, 2024
The
fundamentals
of
bio-orthogonal
click
chemistry
are
investigated,
while
exploring
mechanistic
intricacies,
demonstrating
the
adaptability
and
promise
this
methodology.
Chemical Reviews,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Dec. 2, 2024
Click
chemistry
has
become
one
of
the
most
powerful
construction
tools
in
field
organic
chemistry,
materials
science,
and
polymer
as
it
offers
hassle-free
platforms
for
high-yielding
synthesis
novel
easy
functionalization
strategies.
The
absence
harsh
reaction
conditions
or
complicated
workup
procedures
allowed
rapid
development
biofunctional
polymeric
materials,
such
biopolymers,
tailor-made
surfaces,
stimulus-responsive
polymers,
etc.
In
this
review,
we
discuss
various
types
click
reactions─including
azide-alkyne
cycloadditions,
nucleophilic
radical
thiol
reactions,
a
range
cycloadditions
(Diels-Alder,
tetrazole,
nitrile
oxide,
etc.),
sulfur
fluoride
exchange
(SuFEx)
reaction,
oxime-hydrazone
reactions─and
their
use
formation
study
polymers.
Following
that,
state-of-the-art
biological
applications
"click"-biofunctionalized
including
both
passive
(e.g.,
biosensing
bioimaging)
"active"
ones
that
aim
to
direct
changes
biosystems,
e.g.,
drug
delivery,
antiviral
action,
tissue
engineering.
conclusion,
have
outlined
future
directions
existing
challenges
click-based
polymers
medicinal
clinical
applications.
Advanced Materials,
Journal Year:
2024,
Volume and Issue:
36(33)
Published: June 17, 2024
The
development
of
bioorthogonal
activation
in
drug
release
represents
a
promising
avenue
for
precise
and
safe
anticancer
treatment.
However,
two
significant
limitations
currently
hinder
their
clinical
application:
i)
the
necessity
separate
administration
precursor
its
corresponding
activator,
leading
to
poor
accumulation
potential
side
effects;
ii)
reliance
on
exogenous
metal
or
organic
activators
triggering
activation,
which
often
exhibit
low
efficiency
systemic
toxicity
when
extending
living
animals.
To
overcome
these
limitations,
nitric
oxide
(NO)-mediated
codelivery
nanoassembly,
termed
TTB-NH
Azide-alkyne
cycloaddition
of
cyclooct-2-yn-1-ol
and
2-(azidophenyl)boronic
acid
proceeded
rapidly
at
room
temperature
with
complete
regioselectivity
to
afford
a
triazole
having
boronate
ester
group.
The
secondary
interaction
form
ion
contributed
rate
acceleration
the
control
regioselectivity.
an
imine
or
hemiaminal
was
also
evaluated.
The Journal of Organic Chemistry,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Jan. 12, 2025
The
development
of
bioorthogonal
reactions
is
expected
to
propel
further
advances
in
chemical
biology.
In
this
study,
we
demonstrate
Staudinger–Diels–Alder
(SDA)
ligation
as
a
candidate
for
new
reaction.
This
reaction
ligates
two
molecules
via
strong
C–C
bonds
at
room
temperature.
We
found
that
the
aryl
substituent
azide-benzocyclobutene
(azide-BCB)
had
influence
on
molecule's
tolerance
water.
particular,
Cl-substituted
azide-BCBs
generated
ligated
product
high
yield,
even
presence
Mechanistic
investigations
using
DFT
methods
revealed
hydrophobic
electron-withdrawing
substituents
suppressed
side
SDA
ligation.
RSC Advances,
Journal Year:
2025,
Volume and Issue:
15(9), P. 7127 - 7138
Published: Jan. 1, 2025
Non-toxic
prodrugs
have
proved
of
great
value
in
medicinal
chemistry
programmes
for
cancer,
due
to
their
ability
selectively
deliver
toxic
components
at
tumour
sites
once
they
are
activated
by
a
localised
mechanism.
Since
activation
the
prodrug
afford
drug
is
prerequisite
success
approach,
much
interest
has
focused
on
chemical
and
enzymatic
mechanisms
activating
prodrugs.
Bioorthogonal
positively
impacted
this
area
providing
biocompatible
reactions
that
enable
on-demand
active
release.
However,
be
effective,
it
essential
one
bioorthogonal
reaction
tumour,
order
initiate
on-target
prodrug.
Polymers
such
as
poly(ethylene
glycol)
(PEG)
known
target
solid
tumours
passive
targeting
via
enhanced
permeability
retention
(EPR)
effect.
In
paper,
feasibility
derivatising
long
PEG
chains
activators
(PEG-azide
PEG-tetrazine)
Staudinger
ligation
tetrazine
reactions,
respectively,
evaluated.
The
molecular
weight
activator
type
linkage
moiety
were
shown
significantly
affect
rate
hence
vitro
cytotoxicity
studies
breast
cancer
cells
(MCF-7
MDA-MB-231)
showed
∼68-76%
restoration
parent
drug's
ligation-based
strategy,
100%
strategy.
Restoration
doxorubicin's
intercalate
with
DNA
upon
PEG-activators
was
also
demonstrated
fluorescence
spectroscopy.
Moreover,
conjugation
10
kDa
polymer
improved
its
serum
stability
comparison
other
reported
completely
lose
over
same
period
time.
combined
targeting/bioorthogonal
approach
therefore
been
using
range
prodrugs,
mechanisms,
assays.
Topics in Current Chemistry,
Journal Year:
2024,
Volume and Issue:
382(1)
Published: Feb. 24, 2024
Abstract
Visualization
of
biomolecules
in
their
native
environment
or
imaging-aided
understanding
more
complex
biomolecular
processes
are
one
the
focus
areas
chemical
biology
research,
which
requires
selective,
often
site-specific
labeling
targets.
This
challenging
task
is
effectively
addressed
by
bioorthogonal
chemistry
tools
combination
with
advanced
synthetic
methods.
Today,
smart
elements
toolbox
allows
selective
installation
multiple
markers
to
selected
targets,
enabling
multicolor
multimodal
imaging
biomolecules.
Furthermore,
recent
developments
bioorthogonally
applicable
probe
design
that
meet
growing
demands
superresolution
microscopy
enable
questions
be
addressed.
These
novel,
probes
highly
sensitive,
low-background,
single-
multiphoton
biological
species
and
events
live
organisms
at
resolutions
comparable
size
biomolecule
interest.
Herein,
latest
fluorescent
schemes
will
discussed
context
cellulo/in
vivo
(multicolor
and/or
superresolved)
schemes.
The
second
part
focuses
on
importance
genetically
engineered
minimal
tags,
a
particular
interest
protein
tagging
applications
answer
questions.
