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PRMT7 PROTAC
- Development stage
- Preclinical
- Lead developer
- Icahn School of Medicine
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01
Overview
PRMT7 PROTAC is a proteolysis-targeting chimera (PROTAC) designed to selectively degrade Protein Arginine Methyltransferase 7 (PRMT7). PRMT7 is a type III PRMT that catalyzes monomethyl arginine (MMA) modifications and has been identified as a negative regulator of MHC-I expression in acute myeloid leukemia (AML). By degrading PRMT7, this compound upregulates MHC-I on the surface of AML cells, thereby enhancing their susceptibility to CD8+ T cell-mediated killing and promoting anti-tumor immunity. Research suggests that PRMT7 degradation is a potential strategy to overcome the immune-cold nature of AML without significantly impairing normal hematopoiesis.
- Other names
- PRMT7 targeted degraderPRMT-7 targeted degraderPRMT 7 targeted degrader
02
Targets
CRL4-CRBN (Cereblon-based E3 ubiquitin ligase complex)PRMT7 (Protein arginine methyltransferase 7)
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