SGC-iMLLT (Chemical Probe 92) is a cell penetrant, potent and selective inhibitor of YEATS domain MLLT1/3 histone interaction. SGC-iMLLT downregulates MYC and DDN genes, while increases CD86 in MV4;11 AML cells.
cell penetrant, potent and selective inhibitor of YEATS domain MLLT1/3 histone interaction
Angewandte Chemie (International ed. in English), 57(50), 16302-16307 (2018-10-06)
YEATS domain (YD) containing proteins are an emerging class of epigenetic targets in drug discovery. Dysregulation of these modified lysine-binding proteins has been linked to the onset and progression of cancers. We herein report the discovery and characterisation of the
ENL is a transcriptional coactivator that recruits elongation machinery to active cis-regulatory elements upon binding of its YEATS domain-a chromatin reader module-to acylated lysine side chains. Discovery chemistry for the ENL YEATS domain is highly motivated by its significance in
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