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2017 ; 26
(4
): 662-676
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Targeting human SET1/MLL family of proteins
#MMPMID28160335
Vedadi M
; Blazer L
; Eram MS
; Barsyte-Lovejoy D
; Arrowsmith CH
; Hajian T
Protein Sci
2017[Apr]; 26
(4
): 662-676
PMID28160335
show ga
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.