Protein arginine methyltransferase 7 modulators in disease therapy: Current progress and emerged opportunity.

Protein arginine methyltransferase 7 (PRMT7) is an essential epigenetic and post-translational regulator in eukaryotic organisms. Dysregulation of PRMT7 is intimately related to multiple types of human diseases, particularly cancer. In addition, PRMT7 exerts multiple effects on cellular processes such as growth, migration, invasion, apoptosis, and drug resistance in various cancers, making it as a promising target for anti-tumor therapeutics. In this review, we initially provide an overview of the structure and biological functions of PRMT7, along with its association with diseases. Subsequently, we summarized the PRMT inhibitors in clinical trials and the co-crystal structural of PRMT7 inhibitors. Moreover, we also focus on recent progress in the design and development of modulators targeting PRMT7, including isoform-selective and non-selective PRMT7 inhibitors, and the dual-target inhibitors based on PRMT7, from the perspectives of rational design, pharmacodynamics, pharmacokinetics, and the clinical status of these modulators. Finally, we also provided the challenges and prospective directions for PRMT7 targeting drug discovery in cancer therapy.