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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
.