Drug intelligence / Profile preview

iPRMT1

Development stage
Preclinical
Lead developer
Central South University
Modality
Small Molecules
Administration
Not Specified (preclinical Research Compound; Likely Oral Or Parenteral Based On Typical Small Molecule Administration Routes)
01

Overview

iPRMT1 is a potent and selective small molecule inhibitor of protein arginine N-methyltransferase 1 (PRMT1), an enzyme involved in the methylation of arginine residues on target proteins. PRMT1 plays a critical role in RNA alternative splicing, particularly through methylation of the splicing factor SRSF1, which affects exon inclusion events important for cancer cell growth. Overexpression of PRMT1 is associated with aberrant RNA splicing and tumorigenesis, especially in breast cancer. iPRMT1 inhibits PRMT1-mediated SRSF1 methylation, disrupts oncogenic exon inclusion events, and suppresses breast cancer cell growth both in vitro and in vivo. The compound demonstrates high selectivity for PRMT1 over other related enzymes[2][3][1]. It is being developed primarily as an experimental therapeutic agent for neoplasms such as breast cancer.

02

Targets

PRMT1 (Protein Arginine Methyltransferase 1)

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