Abstract:
:Akt signaling pathway has attracted much attention as a promising target for cancer therapeutics. Herein, we report that Isobavachalcone (IBC), a natural chalcone, potently abrogates Akt signaling and exerts anti-proliferative effects on several human cancer cell lines. Modeling results from the Sybyl/FlexiDock program suggest that IBC potentially binds to the ATP-binding pocket of Akt, which is confirmed by the observations that IBC inhibits Akt1 kinase in vitro. Further studies reveal that IBC significantly abates Akt phosphorylation at Ser-473 and Akt kinase activity in cells, which subsequently leads to inhibition of Akt downstream substrates and evokes significant levels of apoptosis associated with mitochondria pathway.
journal_name
Cancer Lettjournal_title
Cancer lettersauthors
Jing H,Zhou X,Dong X,Cao J,Zhu H,Lou J,Hu Y,He Q,Yang Bdoi
10.1016/j.canlet.2010.01.035subject
Has Abstractpub_date
2010-08-28 00:00:00pages
167-77issue
2eissn
0304-3835issn
1872-7980pii
S0304-3835(10)00070-4journal_volume
294pub_type
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