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ARGINASE
TARGETED LIBRARY

2,000 Compounds

HIGHLIGHTS

►Two isoforms in humans Arginase1 (Arg 1, cytosol), Arginase 2 (Arg2 mitochondria)
►Both catalyze the hydrolysis of L arginine to L ornithine and urea through a mechanism involving one hydroxide and two manganese ions
►Implicated in cancer immunosuppression and cancer tumor growth: an increased metabolism of L Arg by myeloid derived suppressor cells producing Arg 1 inhibits T lymphocyte response
►Other TIs include the following asthma, erectile dysfunction, cystic fibrosis, and atherosclerosis

Major Hindrances

►A strong binder is required to displace the hydroxide and replace it in the manganese coordination network
►X Ray structures of arginase cavity indicate a small volume, allowing little structural diversity
between the metal coordinating and the amino acid moiety of the ligand
►Almost all the published Arg inhibitors exhibit insufficient differences in affinity to provide isoform
selective inhibition in cultured cells or in vivo

Examples of Structures

Medicinal and Computational Chemistry Dept., ChemDiv, Inc.
12760 High Bluff Dr, San Diego, CA, 92130
Phone: + 1 916 234 0888
Fax: +1 858 794 4931
Email: ChemDiv@chemdiv.com

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