PROTAC-Based Therapeutics for Targeting HPV Oncoproteins in Head and Neck Cancers
Nano TransMed,
Год журнала:
2025,
Номер
unknown, С. 100071 - 100071
Опубликована: Янв. 1, 2025
Язык: Английский
CRBN‐PROTACs in Cancer Therapy: From Mechanistic Insights to Clinical Applications
Chemical Biology & Drug Design,
Год журнала:
2024,
Номер
104(5)
Опубликована: Ноя. 1, 2024
Cereblon
(CRBN),
a
member
of
the
E3
ubiquitin
ligase
complex,
has
gained
significant
attention
as
therapeutic
target
in
cancer.
CRBN
regulates
degradation
various
proteins
cancer
progression,
including
transcription
factors
and
signaling
molecules.
PROTACs
(proteolysis-targeting
chimeras)
are
novel
approach
that
uses
cell's
system
to
remove
disease-causing
selectively.
CRBN-dependent
work
by
tagging
harmful
for
destruction
through
ubiquitin-proteasome
system.
This
strategy
offers
several
advantages
over
traditional
protein
inhibition
methods,
potential
overcome
drug
resistance.
Recent
progress
developing
CRBN-based
shown
promising
preclinical
results
both
hematologic
malignancies
solid
tumors.
Additionally,
have
enhanced
our
understanding
CRBN's
role
cancer,
potentially
serving
biomarkers
patient
stratification
predicting
responses.
In
this
review,
we
delineate
mechanisms
action
(CRBN-PROTACs),
summarize
recent
advances
clinical
applications,
provide
perspective
on
future
development.
Язык: Английский
Prodrug Approach as a Strategy to Enhance Drug Permeability
Pharmaceuticals,
Год журнала:
2025,
Номер
18(3), С. 297 - 297
Опубликована: Фев. 21, 2025
Absorption
and
permeability
are
critical
physicochemical
parameters
that
must
be
balanced
to
achieve
optimal
drug
uptake.
These
key
factors
closely
linked
the
maximum
absorbable
dose
required
provide
appropriate
plasma
levels
of
drugs.
Among
various
strategies
employed
enhance
solubility
permeability,
prodrug
design
stands
out
as
a
highly
effective
versatile
approach
for
improving
properties
enabling
optimization
biopharmaceutical
pharmacokinetic
while
mitigating
adverse
effects.
Prodrugs
compounds
with
reduced
or
no
activity
that,
through
bio-reversible
chemical
enzymatic
processes,
release
an
active
parental
drug.
The
application
this
technology
has
led
significant
advancements
in
during
phase,
it
offers
broad
potential
further
development.
Notably,
approximately
13%
drugs
approved
by
U.S.
Food
Drug
Administration
(FDA)
between
2012
2022
were
prodrugs.
In
review
article,
we
will
explore
describing
examples
market
We
also
describe
use
optimize
PROteolysis
TArgeting
Chimeras
(PROTACs)
using
conjugation
technologies.
highlight
some
new
technologies
prodrugs
enrich
properties,
contributing
developing
safe
Язык: Английский
Research progress of ATR small molecule inhibitors in cancer therapy
European Journal of Medicinal Chemistry,
Год журнала:
2025,
Номер
296, С. 117804 - 117804
Опубликована: Май 24, 2025
Язык: Английский
Precision-engineered PROTACs minimize off-tissue effects in cancer therapy
Jianghua Shi,
Luo Wang,
Xuanwei Zeng
и другие.
Frontiers in Molecular Biosciences,
Год журнала:
2024,
Номер
11
Опубликована: Ноя. 22, 2024
Proteolysis-targeting
chimeras
(PROTACs)
offer
a
groundbreaking
approach
to
selectively
degrade
disease-related
proteins
by
utilizing
the
ubiquitin-proteasome
system.
While
this
strategy
shows
great
potential
in
preclinical
and
clinical
settings,
off-tissue
effects
remain
major
challenge,
leading
toxicity
healthy
tissues.
This
review
explores
recent
advancements
aimed
at
improving
PROTAC
specificity,
including
tumor-specific
ligand-directed
PROTACs,
pro-PROTACs
activated
tumor
environments,
E3
ligase
overexpression
strategies.
Innovations
such
as
PEGylation
nanotechnology
also
play
role
optimizing
efficacy.
These
developments
hold
promise
for
safer,
more
effective
cancer
therapies,
though
challenges
translation.
Язык: Английский