The role of PRMT1 in cellular regulation and disease: Insights into biochemical functions and emerging inhibitors for cancer therapy

•We discussed the biochemical properties, cellular functions, and significant roles of PRMT1 in various diseases.•We reviewed the key regulatory mechanisms of PRMT1 in cancer development and explored its feasibility as a potential therapeutic target.•We summarized the currently developed inhibitors targeting PRMT1, discussing their mechanisms, activities, advantages, and disadvantages.•We suggested that synthesized small molecule inhibitors show better potential in cancer treatment and discussed future directions for synthesizing more effective PRMT1 inhibitors. Protein Arginine Methyltransferase 1 (PRMT1), a primary protein arginine methyltransferase, plays a pivotal role in cellular regulation, influencing processes such as gene expression, signal transduction, and cell differentiation. Dysregulation of PRMT1 has been linked to the development of various cancers, establishing it as a key target for therapeutic intervention. This review synthesizes the biochemical characteristics, structural domains, and functional mechanisms of PRMT1, focusing on its involvement in tumorigenesis. Additionally, the development and efficacy of emerging PRMT1 inhibitors as potential cancer therapies are examined. By employing molecular modeling and insights from existing literature, this review posits that targeting PRMT1’s methyltransferase activity could disrupt cancer progression, providing valuable insights for future drug development. [Display omitted]