Researchers develop first-in-class inhibitors against key leukemia protein

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IMAGE: An X-ray crystallography image showing an ASH1L inhibitor developed at U-M in complex with the protein.
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Credit: Grembecka / Cierpicki Labs
The protein made by the ASH1L gene plays a key role in the development of acute leukemia, along with other diseases. The ASH1L protein, however, has been challenging to target therapeutically.
Now a team of researchers led by Jolanta Grembecka, Ph.D., and Tomasz Cierpicki, Ph.D., from the University of Michigan has developed first-in-class small molecules to inhibit ASH1L's SET domain -- preventing critical molecular interactions in the development and progression of leukemia.

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