Potent and selective LSD1 inhibitor DC551040 reveals a promising combination therapy for AML with insight into epigenetic dysregulation - PubMed
4 hours ago
- #LSD1 inhibitor
- #AML
- #epigenetic therapy
- DC551040 is a potent and selective LSD1 inhibitor with potential for AML treatment.
- The inhibitor shows good tolerability in Phase I clinical trials (CTR20222026).
- Crystal structure analysis reveals a new binding pocket for LSD1 inhibitors.
- Transcriptomic and proteomic analyses indicate activation of immune and inflammation pathways post-treatment.
- Combination therapy with homoharringtonine (HHT) shows synergistic antitumor effects in models.
- The study provides insights into epigenetic dysregulation and proposes a new AML therapy approach.