Arginases are key enzymes that hydrolyze L-arginine to urea and L-ornithine in the urea cycle.
The two arginase isoforms, arginase 1 (ARG1) and arginase 2 (ARG2), regulate the proliferation of cancer cells, migration, and apoptosis; affect immunosuppression; and promote the synthesis of polyamines, leading to the development of cancer. Arginases also compete with nitric oxide synthase (NOS) for L-arginine, and their participation has also been confirmed in cardiovascular diseases, stroke, and inflammation.
ARG1 is a much more explored isoform of arginase localized in the cytosol and is expressed mainly in the liver.
ARG2, also called mitochondrial arginase, is expressed in extrahepatic tissues, i.e., the kidneys, small intestine, prostate, and mammary gland.
Arginases are biomarkers and can be used to track disease progression [33]. Targeting ARG1 and ARG2 has been proposed for various diseases. Currently, a dual inhibitor of arginases is under validation in clinical trials in patients with solid tumors; OATD-02 targets both extracellular and intracellular ARG1 and ARG2.
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