Organic Letters,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Oct. 3, 2024
A
modular
site-selective
iron-catalyzed
radical
amination
of
a
number
phenol-containing
biomolecules
such
as
tyrosine-containing
peptides,
estrogens,
and
other
phenol-based
pharmaceuticals
has
been
developed.
The
method
features
the
use
cost-efficient
combination
FeBr
RSC Advances,
Journal Year:
2025,
Volume and Issue:
15(12), P. 9159 - 9179
Published: Jan. 1, 2025
This
review
provides
an
account
of
the
site-selective
cleavage
peptides
and
proteins
at
aromatic
amino
acid
residues,
developed
over
last
seven
decades
(1958–2024).
Chemical & Biomedical Imaging,
Journal Year:
2024,
Volume and Issue:
2(9), P. 615 - 630
Published: Aug. 23, 2024
The
development
of
peptide-based,
radiometal-labeled
PET
imaging
agents
has
seen
an
increase
in
attention
due
to
the
favorable
properties
peptide
backbone
exhibits.
These
include
high
selectivity
and
affinity
proteins
cells
directly
linked
various
types
cancers.
In
addition,
rapid
clearance
from
circulation
low
toxicity
allow
for
unique
approaches
engineering
a
viable
peptide-based
agent.
Utilizing
peptides
as
allows
modifications
improve
metabolic
stability,
target
cell
affinity,
image
quality
capabilities
reduce
toxicity.
Select
radiolabeled
have
already
been
FDA
approved,
with
many
more
late-stage
trials.
This
review
summarizes
current
state
field
well
explores
methods
used
by
researchers
modify
peptides,
concluding
look
at
future
therapy
diagnostics.
The Journal of Physical Chemistry A,
Journal Year:
2024,
Volume and Issue:
128(10), P. 1902 - 1912
Published: March 4, 2024
In
this
paper,
we
present
a
new
finding,
the
basis
electronic
activity
(BEA)
of
molecular
systems;
it
corresponds
to
significant,
although
nonreactive,
vibrationally
induced
that
takes
place
in
any
system.
Although
molecule's
BEA
is
composed
an
equal
number
local
contributions
as
vibrational
degrees
freedom,
our
results
indicate
only
stretching
modes
contribute
it.
To
account
for
activity,
descriptor,
bond
flux
(BEF),
introduced.
The
BEF
combined
with
force
constant
potential
well
hosting
gives
rise
effective
reactivity
index
(EBR),
which
turns
out
be
first
density
functional
theory-based
descriptor
simultaneously
accounts
structural
and
effects.
Besides
quantifying
reactivity,
EBR
provides
compare
reactivities
bonds
inserted
different
chemical
environments
paves
way
exertion
selective
control
enhance
or
inhibit
their
reactivities.
concepts
formulated
paper
associated
computational
tools
are
illustrated
characterization
set
representative
molecules.
all
cases,
BEFs
follow
same
linear
pattern,
whose
slopes
intensity
quantify
bonds.
Chemical Communications,
Journal Year:
2024,
Volume and Issue:
unknown
Published: Jan. 1, 2024
This
highlight
provides
an
account
of
the
discovery
and
advances
in
tyrosine-click
(Y-click)
reaction
its
extensive
application
mapping
proteins,
imaging
living
cells,
fields
analytical
medicinal
chemistry.
Journal of the American Chemical Society,
Journal Year:
2025,
Volume and Issue:
unknown
Published: Jan. 30, 2025
Modular
chemical
postmodification
of
peptides
is
a
promising
strategy
that
supports
the
optimization
and
innovation
hit
peptide
therapeutics
by
enabling
rapid
derivatization.
However,
current
methods
are
primarily
limited
to
traditional
bio-orthogonal
strategies
ligation
techniques,
which
require
preintroduction
non-natural
amino
acids
impose
fixed
limit
diversity.
Here,
we
developed
Tyrosine-1,2,3-Triazine
Ligation
(YTL)
strategy,
constructs
novel
linkages
(pyridine
pyrimidine)
through
"one-pot,
two-step"
process
combining
SNAr
IEDDA
reactions,
promoting
modular
post
modification
Tyr-containing
peptides.
After
optimizing
YTL
establishing
standard
procedures,
successfully
applied
it
solid-phase
various
biorelated
peptides,
such
as
synthesis
dual-mode
imaging
probes
long-acting
GLP-1
analogs.
As
proof
concept,
library
384
amphipathic
was
constructed
using
based
on
96-well
microfiltration
plates.
modifications
were
then
performed
screened
template
tripeptide
RYR,
leading
generation
20
derivatives.
The
antibacterial
activity
these
derivatives
systematically
characterized,
identifying
Z8
potential
candidate.