Pharmaceutics,
Год журнала:
2023,
Номер
16(1), С. 4 - 4
Опубликована: Дек. 19, 2023
The
proper
viral
assembly
relies
on
both
nucleic
acids
and
structural
proteins.
Thus
a
biologically
active
agent
that
provides
the
degradation
of
one
these
key
proteins
and/or
destroys
factory
could
suppress
replication
efficiently.
nucleocapsid
protein
(N-protein)
is
for
SARS-CoV-2
virus.
As
bioactive
agent,
we
offer
modular
nanotransporter
(MNT)
developed
by
us,
which,
in
addition
to
an
antibody
mimetic
N-protein,
contains
amino
acid
sequence
attraction
Keap1
E3
ubiquitin
ligase.
This
should
lead
subsequent
N-protein.
We
have
shown
functional
properties
modules
within
MNT
permit
its
internalization
into
target
cells,
endosome
escape
cytosol,
binding
Using
flow
cytometry
western
blotting,
demonstrated
significant
N-protein
when
A549
A431
cells
transfected
with
plasmid
coding
were
incubated
MNTs.
proposed
MNTs
open
up
new
approach
treatment
diseases.
ACS Omega,
Год журнала:
2025,
Номер
10(5), С. 4745 - 4753
Опубликована: Янв. 30, 2025
Among
the
various
strategies
being
developed
in
field
of
protein
degraders,
HyTags
remain
relatively
underexplored,
despite
their
advantages
over
PROTACs.
Their
synthesis
typically
involves
multistep
procedures,
including
use
coupling
reagents
and
protection/deprotection
steps.
To
develop
a
more
sustainable
streamlined
approach,
we
designed
versatile
multicomponent
platform
that
generates
with
diverse
linkers
hydrophobic
moieties
high
yields.
Using
(+)-JQ1
as
POI
ligand,
synthesized
series
BRD4-targeting
discovered
compound
23
induces
degradation
BRD4
via
autophagy-lysosome
pathway
through
ER
stress.
This
finding
further
supports
valuable
application
this
synthetic
methodology
search
for
effective
degraders.
Frontiers in Pharmacology,
Год журнала:
2025,
Номер
16
Опубликована: Фев. 11, 2025
Drug
discovery
plays
a
crucial
role
in
medicinal
chemistry,
serving
as
the
cornerstone
for
developing
new
treatments
to
address
wide
range
of
diseases.
This
review
emphasizes
significance
advanced
strategies,
such
Click
Chemistry,
Targeted
Protein
Degradation
(TPD),
DNA-Encoded
Libraries
(DELs),
and
Computer-Aided
Design
(CADD),
boosting
drug
process.
Chemistry
streamlines
synthesis
diverse
compound
libraries,
facilitating
efficient
hit
lead
optimization.
TPD
harnesses
natural
degradation
pathways
target
previously
undruggable
proteins,
while
DELs
enable
high-throughput
screening
millions
compounds.
CADD
employs
computational
methods
refine
candidate
selection
reduce
resource
expenditure.
To
demonstrate
utility
these
methodologies,
we
highlight
exemplary
small
molecules
discovered
past
decade,
along
with
summary
marketed
drugs
investigational
that
exemplify
their
clinical
impact.
These
examples
illustrate
how
techniques
directly
contribute
advancing
chemistry
from
bench
bedside.
Looking
ahead,
Artificial
Intelligence
(AI)
technologies
interdisciplinary
collaboration
are
poised
growing
complexity
discovery.
By
fostering
deeper
understanding
transformative
this
aims
inspire
innovative
research
directions
further
advance
field
chemistry.
Molecules,
Год журнала:
2024,
Номер
29(7), С. 1573 - 1573
Опубликована: Апрель 1, 2024
Moonlighting
enzymes
are
multifunctional
proteins
that
perform
multiple
functions
beyond
their
primary
role
as
catalytic
enzymes.
Extensive
research
and
clinical
practice
have
demonstrated
pivotal
roles
in
the
development
progression
of
cancer,
making
them
promising
targets
for
drug
development.
This
article
delves
into
notable
moonlighting
enzymes,
including
GSK-3,
GAPDH,
ENO1,
with
a
particular
emphasis
on
an
enigmatic
phosphatase,
PTP4A3.
We
scrutinize
distinct
cancer
mechanisms
dictate
ability
to
switch
roles.
Lastly,
we
discuss
potential
innovative
approach
develop
drugs
targeting
these
enzymes:
target
protein
degradation.
strategy
holds
promise
effectively
tackling
context
therapy.
