ArticleJournal of medicinal chemistry2025
Discovery of LD-110 as an Effective LSD1 PROTAC Degrader for the Treatment of Esophagus Squamous Cancer.
Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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12 authors.
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Abstract
LSD1, a pivotal epigenetic regulator mediating histone demethylation, is an attractive therapeutic target due to its oncogenic roles in cancers. Although numerous small-molecule inhibitors of LSD1 were advanced to clinical trials, only one PROTAC-based degrader was reported most recently. Here, we report a potent and efficacious proteolysis-targeting chimera (PROTAC) degrader, LSD1, designated as LD-110. Biochemically, LD-110 promotes LSD1 degradation and increases the level of H3K4 dimethylation in a ubiquitin-proteasome-dependent manner. Biologically, LD-110 inhibits the growth and survival of multiple esophagus squamous cancer cell (ESCC) lines by inducing apoptosis with much greater effectiveness than its small-molecule warhead LI-1. Finally, LD-110 effectively suppresses tumor growth in a KYSE-150 xenograft tumor model without obvious signs of toxicity, while LI-1 is largely ineffective. Collectively, LD-110 is a promising therapeutic candidate for PROTAC-based targeted therapy of ESCC through LSD1 degradation and can also be used as a versatile tool for probing LSD1 biology.
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