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SG5 is a small molecule inhibitor targeting the PRMT5-MTA complex, currently in preclinical development by Sungening for the treatment of solid tumors. PRMT5 (Protein Arginine Methyltransferase 5) is an epigenetic enzyme that methylates arginine residues on various proteins. In cancers characterized by MTAP (methylthioadenosine phosphorylase) deletion, the metabolite methylthioadenosine (MTA) accumulates and binds to PRMT5, creating a unique molecular vulnerability. SG5 is designed to selectively target this PRMT5-MTA complex, inducing synthetic lethality specifically in MTAP-deficient tumor cells while minimizing effects on healthy tissues that lack MTA accumulation.
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