Research of novel anticancer agents targeting arginase inhibition

Arginase plays an important part in l-arginine metabolism. This metalloenzyme also regulates polyamine biosynthesis, nitric oxide production and the T-cell-mediated immune response, which are all involved in the growth and control of cancer. Research over the past decades has reported arginase as an attractive target for cancer treatment, and inhibition of arginase could be a promising strategy for cancer therapy. Herein, we present the available data on the role of arginase in cancer development. The principal synthetic and natural arginase inhibitors are outlined and followed by their mechanism of action. Among them, some molecules have shown their anticancer effects. The perspectives of arginase inhibitors as new anticancer agents will be discussed.