Discovery of an MLLT1/3 YEATS domain chemical probe
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 first small molecule chemical probe, SGC‐iMLLT, for the YD of MLLT1 (ENL/YEATS1) and MLLT3 (AF9/YEATS3). SGC‐iMLLT is a potent and selective inhibitor of MLLT1/3 ‐ histone interactions. Excellent selectivity over other human...Expand abstract
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Copyright © 2018 The Authors. Published by Wiley-VCH Verlag GmbH & Co. KGaA.
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