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RCOR1 degrader
- Development stage
- Preclinical
- Lead developer
- RejuvenRx
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01
Overview
RCOR1 degrader is an experimental small molecule therapeutic being developed by RejuvenRx for the treatment of various cancers. It functions through the mechanism of targeted protein degradation (TPD), specifically targeting REST Corepressor 1 (RCOR1), also known as CoREST. RCOR1 acts as a central scaffold for the CoREST complex, which recruits epigenetic modifiers such as Lysine-specific demethylase 1 (LSD1) and Histone deacetylases 1 and 2 (HDAC1/2) to silence specific gene loci. In many cancers, the CoREST complex is involved in maintaining an undifferentiated state and suppressing genes that would otherwise promote cell cycle arrest or apoptosis. By degrading RCOR1, this agent destabilizes the entire CoREST complex, leading to the loss of its repressive function and the re-expression of therapeutic target genes. The program is currently in the preclinical stage of development.
- Other names
- RCOR1 small molecule degraderRCOR-1 small molecule degraderRCOR 1 small molecule degraderCoREST degraderRCOR1 degrader (RejuvenRx)
02
Targets
HDAC1 (Histone Deacetylase 1)HDAC2 (Histone deacetylase 2)KBTBD4 (Kelch repeat and BTB domain-containing protein 4)KDM1A (LSD1)RCOR1 (CoREST Complex)
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