EPZ015666, a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an antitumour effect in retinoblastoma.

Xing Liu, JianZhong He, Longbing Mao, Yanyan Zhang, WenWen Cui, Sujuan Duan, Alan Jiang, Yang Gao, Yi Sang, Guofu Huang

Experimental eye research 2021 Jan

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Retinoblastoma (RB) is the most common intraocular malignant tumour in infants, and chemotherapy has been the primary therapy method in recent years. PRMT5 is an important member of the protein arginine methyltransferase family, which plays an important role in various tumours. Our study showed that PRMT5 was overexpressed in retinoblastoma and played an important role in retinoblastoma cell growth. EPZ015666 is a novel PRMT5 inhibitor, and we found that it inhibited retinoblastoma cell proliferation and led to cell cycle arrest at the G1 phase. At the same time, EPZ015666 regulated cell cycle related protein (P53, P21, P27, CDK2) expression. In brief, our study showed that PRMT5 promoted retinoblastoma growth, the PRMT5 inhibitor EPZ015666 inhibited retinoblastoma in vitro by regulating P53-P21/P27-CDK2 signaling pathways and slowed retinoblastoma growth in a xenograft model. Copyright © 2020. Published by Elsevier Ltd.

Citation

Xing Liu, JianZhong He, Longbing Mao, Yanyan Zhang, WenWen Cui, Sujuan Duan, Alan Jiang, Yang Gao, Yi Sang, Guofu Huang. EPZ015666, a selective protein arginine methyltransferase 5 (PRMT5) inhibitor with an antitumour effect in retinoblastoma. Experimental eye research. 2021 Jan;202:108286