AMI-1 is a specific arginine methyltransferase inhibitor (a pan-PRMT inhibitor) with IC50 value of 1.63μM for PRMT1. It inhibited methylation of GFP-Npl3 and cellular proteins. Dose-dependent reduction of nuclear receptor-mediated transactivation, including an estrogen response element (ERE) and an androgen response element, could be observed in MCF7 cells transfected with a luciferase reporter post treatment with AMI-1 at 5, 50 and 100μM[3]. AMI-1 inhibited the expression of COX2 on mRNA level in TGF-β–stimulated cells. AMI-1 (50μl at a concentration of 0.1 mg/ml in PBS 2h before OVA challenge) administered to AIPI (Ag-induced pulmonary inflammation) rats reduced COX2 production and humoral immune response, and it abrogated mucus secretion and collagen generation[4].
作用机制
AMI-1 inhibits arginine methylation by inserting into the arginine-binding pocket.[3]
To evaluate the effect of AMI-1 on the proliferation and viability of Rh30 cells, results showed that AMI-1 significantly reduced cell proliferation and viability.
Int J Mol Sci. 2021 Jul 27;22(15):8023.
RD cells
123.9 µM
72 h
To evaluate the effect of AMI-1 on the proliferation and viability of RD cells, results showed that AMI-1 significantly reduced cell proliferation and viability.
Int J Mol Sci. 2021 Jul 27;22(15):8023.
mouse spleen cells
100 µM
To evaluate the cytotoxicity of AMI-1 on mouse spleen cells, results showed no cytotoxicity at 100 µM
Front Immunol. 2017 May 23;8:596.
Tregs
100 µM
3 days
To evaluate the effect of AMI-1 on Foxp3 expression in Tregs, results showed that AMI-1 treatment increased the percentage of CD4+Foxp3+ T cells
Front Immunol. 2017 May 23;8:596.
SKOV3 cells
200 μM
24, 48, 72 h
To evaluate the effect of PRMT1 inhibition on BRD4 phosphorylation, results showed that AMI-1 treatment significantly reduced the phosphorylation level of BRD4.
Cell Death Dis. 2023 Sep 22;14(9):624.
A2780 cells
200 μM
24, 48, 72 h
To evaluate the effect of PRMT1 inhibition on BRD4 phosphorylation, results showed that AMI-1 treatment significantly reduced the phosphorylation level of BRD4.
Cell Death Dis. 2023 Sep 22;14(9):624.
HEK293T cells
200 μM
24, 48, 72 h
To evaluate the effect of PRMT1 inhibition on BRD4 phosphorylation, results showed that AMI-1 treatment significantly reduced the phosphorylation level of BRD4.
AMI-1 treatment significantly reduced the formation of colorectal adenomas in C57BL/6J-ApcMin/+mice and improved the survival rate of the mice.
Genome Med. 2021 Apr 14;13(1):58
Mice
DSS-induced colitis model
Intraperitoneal injection
200 mg/kg
Once daily for 7 days
To evaluate the therapeutic effect of AMI-1 on DSS-induced colitis model, results showed that AMI-1 treatment reduced disease severity and increased Tregs frequency and function
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