Unraveling the complexity of histone-arginine methyltransferase CARM1 in cancer: From underlying mechanisms to targeted therapeutics

Coactivator-associated arginine methyltransferase 1 (CARM1), a type I protein arginine methyltransferase (PRMT), has been widely reported to catalyze arginine methylation of histone and non-histone substrates, which is closely associated with the occurrence and progression of cancer. Recently, accumulating studies have demonstrated the oncogenic role of CARM1 in many types of human cancers. More importantly, CARM1 has been emerging as an attractive therapeutic target for discovery of new candidate anti-tumor drugs. Therefore, in this review, we summarize the molecular structure of CARM1 and its key regulatory pathways, as well as further discuss the rapid progress in better understanding of the oncogenic functions of CARM1. Moreover, we further demonstrate several representative targeted CARM1 inhibitors, especially focusing on demonstrating their designing strategies , potential therapeutic applications. Together, these inspiring findings would shed new light on elucidating the underlying mechanisms of CARM1 and provide a clue on discovery of more potent and selective CARM1 inhibitors for the future targeted cancer therapy.

Automated summary

CARM1 is a type I protein arginine methyltransferase that catalyzes arginine methylation of histone and non-histone substrates, and is closely related to cancer occurrence and progression. This review summarizes the molecular structure of CARM1, its regulatory pathways, and discusses its oncogenic functions in tumor development. Furthermore, representative CARM1 inhibitors are demonstrated, focusing on their design strategies and potential therapeutic applications. These findings shed light on the understanding of CARM1 mechanisms and provide insights for the development of targeted cancer therapy.