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Open access Sep 2026

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

Both NSD2 and GSPT1 represent compelling targets for anti-cancer 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: 424-ND, an NSD2-selective degrader, and 424-GD,...

Wei-Zhong Shen, Yi-Han Liu, Lian-Chao Liu et al. · 0 citations

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