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Cbz-B3A provides a novel strategy to block translation via 4EBP1 phosphorylation that may also be an effective treatment for these devastating diseases
About
We have discovered a small molecule inhibitor (Cbz-B3A) of mTORC1 signaling. This process is mediated by ubiquilins, thus linking mTOR signaling to protein homeostasis. Cbz-B3A preferentially inhibits the phosphorylation of certain binding proteins and blocks most of the translation process. Cbz-B3A slows cellular growth of human tumor cell lines, but is not cytotoxic. Cbz-B3A has very different characteristics than previously described mTOR inhibitors. It is a specific inhibitor of the mTORC1 complex, while rapamycin, TORIN and other inhibitors also block mTORC2. In contrast to rapamycin, which preferentially inhibits the phosphorylation of p70s6k, or TORIN, which inhibits the phosphorylation of all mTOR substrates.
Key Benefits
Cbz-B3A does not appear to interact directly with mTORC1 but rather inhibition is mediated by ubiquilins 2 and 4. Unlike other mTOR inhibitors, Cbz-B3A efficiently blocks 4EBP1 phosphorylation but only partially inhibits the phosphorylation of p70s6k. Cbz-B3A provides a novel strategy to block translation via 4EBP1 phosphorylation that may also be an effective treatment for these devastating diseases