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BIIB021, a novel Hsp90 inhibitor, sensitizes esophageal squamous cell carcinoma to radiation.
[esophageal squamous cell carcinoma]
BIIB
021
is
a
novel
,
orally
available
inhibitor
of
heat
shock
protein
90
(
Hsp
90
)
that
is
currently
in
phase
I
/
II
clinical
trials
.
BIIB
021
induces
the
apoptosis
of
various
types
of
tumor
cells
in
vitro
and
in
vivo
.
The
aim
of
this
study
is
to
investigate
the
effect
of
BIIB
021
on
the
radiosensitivity
of
esophageal
squamous
cell
carcinoma
(
ESCC
)
.
The
results
indicated
that
BIIB
021
exhibited
strong
antitumor
activity
in
ESCC
cell
lines
,
either
as
a
single
agent
or
in
combination
with
radiation
.
BIIB
021
significantly
downregulated
radioresistant
proteins
including
EGFR
,
Akt
,
Raf-
1
of
ESCC
cell
lines
,
increased
apoptotic
cells
and
enhanced
G
2
arrest
that
is
more
radiosensitive
cell
cycle
phase
.
These
results
suggest
that
this
synthetic
Hsp
90
inhibitor
simultaneously
affects
multiple
pathways
involved
in
tumor
development
and
progression
in
the
ESCC
setting
and
may
represent
a
better
strategy
for
the
treatment
of
ESCC
patients
,
either
as
a
monotherapy
or
a
radiosensitizer
.
Diseases
Validation
Diseases presenting
"tumor development"
symptom
congenital adrenal hyperplasia
dystrophic epidermolysis bullosa
esophageal squamous cell carcinoma
familial hypocalciuric hypercalcemia
liposarcoma
lymphangioleiomyomatosis
oral submucous fibrosis
primary effusion lymphoma
severe combined immunodeficiency
wolf-hirschhorn syndrome
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