Drug intelligence / Profile preview

AMI-1

Development stage
Unknown
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

AMI-1 (Arginine Methyltransferase Inhibitor 1) is a cell-permeable, small molecule inhibitor of protein arginine N-methyltransferases (PRMTs). It was originally identified as a potent inhibitor of PRMT1, PRMT3, PRMT4 (CARM1), and PRMT6, acting by competing with the binding of peptide substrates rather than the S-adenosyl-L-methionine (SAM) cofactor. In immunological research, AMI-1 has been shown to influence the balance between inflammatory T cells and Foxp3+ regulatory T cells (Tregs). Specifically, in models of ulcerative colitis, AMI-1 treatment reduces PRMT5 expression and DNA methyltransferase 1 (DNMT1) binding to the Foxp3 promoter, thereby promoting Treg differentiation and alleviating intestinal inflammation. While it is a valuable tool for studying epigenetic regulation and arginine methylation, it is primarily utilized as a research reagent and is not currently in clinical development.

Other names
7,7'-carbonylbis(azanediyl)bis(4-hydroxynaphthalene-2-sulfonic acid)Protein Arginine Methyltransferase Inhibitor 1
02

Targets

Human immunodeficiency virus type 1 reverse transcriptasePRMT1 (Protein Arginine Methyltransferase 1)PRMT3 (Protein arginine N-methyltransferase 3)PRMT4 (Protein arginine N-methyltransferase 4)PRMT5 (Protein arginine N-methyltransferase 5)PRMT6

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