Weixue Huang

Single-Atom Modification Enables Reversal of Degradation Selectivity between NSD2 and GSPT1

Abstract Both NSD2 and GSPT1 represent compelling targets for anticancer drug discovery. Herein, we carried out single-atom modification of LLC0424, an NSD2 degrader with GSPT1 neosubstrate engagement, to yield two structurally analogous molecules with divergent modes of action:...