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Targeting Human SET1/MLL Family of Proteins

Targeting Human SET1/MLL Family of Proteins

Masoud Vedadi, Levi Blazer, Mohammad S Eram, Dalia Barsyte-Lovejoy, Cheryl H Arrowsmith, Taraneh Hajian

Protein Sci. 2017 Apr;26(4):662-676.

PMID: 28160335

Abstract:

The SET1 family of proteins, and in particular MLL1, are essential regulators of transcription and key mediators of normal development and disease. Here, we summarize the detailed characterization of the methyltransferase activity of SET1 complexes and the role of the key subunits, WDR5, RbBP5, ASH2L, and DPY30. We present new data on full kinetic characterization of human MLL1, MLL3, SET1A, and SET1B trimeric, tetrameric, and pentameric complexes to elaborate on substrate specificities and compare our findings with what has been reported before. We also review exciting recent work identifying potent inhibitors of oncogenic MLL1 function through disruption of protein-protein interactions within the MLL1 complex.

Chemicals Related in the Paper:

Catalog Number	Product Name	CAS Number	Price
AP1561178173	SGC0946	1561178-17-3	Price
IAR42416111	MLL1/WDR5/Ash2L/RbBP5 human		Price
IAR42416121	Ash2L human		Price
IAR42416122	DPY30 human		Price

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