PRMT5 Inhibitors

PRMT5 inhibitors represent a diverse class of compounds designed to selectively target the PRMT5 enzyme, a key player in regulating cellular processes through arginine methylation. These inhibitors encompass various chemical structures and mechanisms to impede the function of PRMT5 within cellular contexts. Some compounds, like GSK3326595 developed by GlaxoSmithKline, exert potent and selective inhibition of PRMT5. Others, such as EPZ015666 (GSK3235025), a collaborative effort between Epizyme and GSK, demonstrate efficacy in curbing the proliferation of specific cancer cell lines.

SGC707, a compound formulated by the Structural Genomics Consortium (SGC), is another selective inhibitor exhibiting activity against certain cancer cell lines. Additionally, cyclic peptide-based inhibitors like CMP5 mimic the arginine substrate and showcase promising outcomes in targeting PRMT5 function. HLCL-61, identified through high-throughput screening, and compounds like CPI-360 and EPZ015686 demonstrate antiproliferative effects in different cancer cell models, showcasing the diversity in their chemical structures and modes of action against PRMT5.