The protein arginine methyltransferase 5 (PRMT5) is our next topic in the Biologics campaign!
PRMT5 is a type II arginine methyltransferase that catalyzes symmetric dimethylation marks on histones and non-histone proteins. PRMT5 is involved in many vital human biological functions such as RNA splicing, cell cycle, cell death, and metabolic signaling.
The role of PRMT5 in various cancers is particularly well-documented. Besides, emerging studies have demonstrated the pathological contribution of PRMT5 in driving or reducing inflammatory diseases, such as diabetes, cardiovascular diseases, and neurodegenerative disorders. The current knowledge on PRMT5 can be used to improve the outcomes of patients with related conditions. Also, researchers established the link of PRMT5 to inflammation through its methyltransferase activity on the NF-κB signaling pathway. This demonstrates the pathological relevance of the PRMT5/NF-κB axis in pancreatic cancer, colon cancer, and heart disease.
The first-in-class PRMT5 inhibitor was reported only in 2015. Now, the following improved compounds are under clinical trials (phase I) in solid tumors, non-Hodgkin lymphoma, myelodysplastic syndrome, and AML. Additional info about the current state of PRMT5 function and targeting in cancer is here.