Existing inhibitors for lysine-specific histone demethylase 1A (LSD1), a key driver for small cell lung cancer (SCLC) carcinogenesis, have notable limitations. Here, the authors employ structure-based engineering to develop a histone H3-competitive LSD1 inhibitor to enhance specificity and reduce off-target effects in SCLC cells through transcriptional regulation and epigenetic reprogramming.
- Takumitsu Machida
- Yingbo Gong
- Tomoaki Tanaka
