This week in therapeutics

Indication

Target/marker/pathway

Summary

Licensing status

Publication and contact information

Cancer

Leukemia

Myeloid-lymphoid or mixed-lineage leukemia (MLL; HRX); WD repeat domain 5 (WDR5)

In vitro studies identified inhibitors of the protein-protein interaction between WDR5 and MLL protein-protein interactions that could help treat leukemias. In an enzymatic assay, peptide inhibitors of the MLL binding site on WDR5 blocked MLL's H3K4 methyltransferase activity. In leukemia cells with MLL fusion protein expression, the most potent peptide inhibitor blocked cell growth in leukemia cells with MLL fusion protein expression but not in leukemia cells expressing wild-type MLL. Next steps include improving the cellular potency and in vivo properties of the inhibitor peptides.

SciBX 6(1); doi:10.1038/scibx.2013.8
Published online Jan. 10, 2013

Patent applications filed; licensed by Ascentage Pharma Group Corp. Ltd.; available for partnerships

Karatas, H. et al. J. Am. Chem. Soc.; published online Dec. 4, 2012;
doi:10.1021/ja306028q
Contact: Shaomeng Wang, University of Michigan, Ann Arbor, Mich.
e-mail:
shaomeng@umich.edu