Compound class:
Synthetic organic
Comment: MI-3 inhibits the interaction between MLL oncoproteins (re-arranged lysine (K)-specific methyltransferases) and the tumour suppressor protein menin (MEN1, O00255) [1]. MI-3 represents a novel molecular mechanism with potential application in the treatment of aggressive leukemias with MLL rearrangements.
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No information available. |
Mechanism Of Action and Pharmacodynamic Effects |
The MLL-menin interaction is implicated the in leukemogenic activity (or oncogenic transformation) of MLL fusion oncoproteins, with MLL-menin being a component of the MLL SET1-like histone methyl transferase complex which regulates HOX gene expression [2-3]. MI-2 treatment reverses the leukemogenic activity of MLL fusion proteins by downregulating the expression of HOXA9 and MEIS1, inhibits proliferation and promotes apoptosis of MLL leukemia cells [1]. |