Compound class:
Synthetic organic
Comment: MI-503 inhibits the interaction between MLL oncoproteins (re-arranged lysine methyltransferase 2A; KMT2A; a.k.a. MLL1) and the tumour suppressor protein menin (MEN1, O00255), by binding directly to MLL binding site on menin [1]. MI-503 is active in vivo, exhibiting selective antiproliferative effects on cells harbouring MLL rearrangements. It represents a highly optimised molecular scaffold for clinical lead identification in the development of drugs for the treatment of aggressive MLL-rearranged leukemias.
|
|
References |
1. Borkin D, He S, Miao H, Kempinska K, Pollock J, Chase J, Purohit T, Malik B, Zhao T, Wang J et al.. (2015)
Pharmacologic inhibition of the Menin-MLL interaction blocks progression of MLL leukemia in vivo. Cancer Cell, 27 (4): 589-602. [PMID:25817203] |