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Akira Yokoi, Yoshihiko Kotake, Kentaro Takahashi, Tadashi Kadowaki, Yoshiko Matsumoto, Yukinori Minoshima, Naoko H. Sugi, Koji Sagane, Makoto Hamaguchi, Masao Iwata and Yoshiharu Mizui Biological validation that SF3b is a target of the antitumor macrolide pladienolide FEBS Journal 278

Article first published online: 31 OCT 2011 | DOI: 10.1111/j.1742-4658.2011.08387.x

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Pladienolide is an antitumor macrolide that binds to the SF3b complex. We identified a mutation in the SF3B1 gene in the pladienolide-resistant cells. The mutation confers resistance to the inhibitory action of pladienolide on cell proliferation and splicing by impairing the ability of pladienolide to bind to SF3b. Our results clearly demonstrate that pladienolide exerts its potent activity by targeting SF3b.

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