Context-specific applications of CARM1 inhibitors: functional profiles of EZM2302 and TP-064.

ABSTRACT:

Background

Coactivator-associated arginine methyltransferase 1 (CARM1) regulates diverse cellular processes-including transcription, cell cycle progression, metabolism, and autophagy-through asymmetric dimethylation of both histone and non-histone substrates. Although TP-064 and EZM2302 both inhibit CARM1, they may elicit distinct biological effects.

Methods

We employed immunoblotting, subcellular fractionation, histone extraction, chromatin immunoprecipitation assay, quantitative PCR, and confocal microscopy to compare the effects of TP-064 and EZM2302. Substrate methylation and autophagic responses were evaluated under nutrient-deprived conditions.

Results

Both TP-064 and EZM2302 inhibited CARM1-dependent methylation of non-histone substrates, including p300, GAPDH,

SUBMITTER: Cho Y 

PROVIDER: S-EPMC12576987 | biostudies-literature | 2025 Oct

REPOSITORIES: biostudies-literature