Drug intelligence / Profile preview

PRMT7 inhibitor

Development stage
Preclinical
Lead developer
City of Hope
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Intratumoral
01

Overview

PRMT7 inhibitors are a class of epigenetic modulators that target Protein Arginine Methyltransferase 7 (PRMT7), the only type III PRMT, which catalyzes monomethyl arginine (MMA) modifications. In the context of oncology, particularly Acute Myeloid Leukemia (AML), PRMT7 has been identified as a crucial negative regulator of MHC-I expression. Inhibition or degradation of PRMT7 (e.g., via PROTACs) has been shown to remarkably upregulate MHC-I levels on AML cells, thereby enhancing anti-tumor immunity and increasing susceptibility to CD8+ T cell-mediated killing. Research conducted by institutions such as the City of Hope and the Icahn School of Medicine at Mount Sinai suggests that targeting PRMT7 could be a promising strategy to convert immune-cold AML into a state more responsive to immunotherapy, without significantly impairing normal hematopoiesis.

Other names
PRMT7 inhibitorsPRMT-7 inhibitorsPRMT 7 inhibitorsProtein arginine methyltransferase 7 inhibitorPRMT7 PROTACPRMT-7 PROTACPRMT 7 PROTACPRMT7 degraderPRMT-7 degraderPRMT 7 degrader
02

Targets

PRMT7 (Protein arginine methyltransferase 7)PRMT9

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