Arginase I | Arginase | IUPHAR Guide to IMMUNOPHARMACOLOGY

Top ▲

Arginase I

Target id: 1244

Nomenclature: Arginase I

Abbreviated Name: ARG1

Family: Arginase

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

   GtoImmuPdb view: ON :     Arginase I has curated data in GtoImmuPdb

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - ARG1 arginase 1
Mouse - - Arg1 arginase, liver
Rat - - Arg1 arginase 1
Previous and Unofficial Names
Liver arginase | AI type I arginase | PGIF | cytosolic arginase | arginase
Database Links
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human Arginase-1 complexed with inhibitor 9.
Ligand:  compound 9 [PMID: 23472952]
Resolution:  1.3Å
Species:  Human
References:  4
Enzyme Reaction
EC Number:
Description Reaction Reference
L-arginine + H2O <=> L-ornithine + urea

Download all structure-activity data for this target as a CSV file

Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
2(S)-amino-6-boronohexanoic acid Hs Inhibition 8.3 pKd 2
pKd 8.3 (Kd 5x10-9 M) [2]
A1P Hs Inhibition 5.7 pKd 3
pKd 5.7 (Kd 2x10-6 M) [3]
Description: Dissociation constant measured using surface plasmon resonance assay.
A1P Hs Inhibition 5.4 pKi 3
pKi 5.4 (Ki 4x10-6 M) [3]
Description: Measured using an enzyme kinetics assay.
compound 9 [PMID: 23472952] Hs Inhibition 6.7 pIC50 4
pIC50 6.7 (IC50 2.23x10-7 M) [4]


Show »

1. Adams JL, Smothers J, Srinivasan R, Hoos A. (2015) Big opportunities for small molecules in immuno-oncology. Nat Rev Drug Discov, 14 (9): 603-22. [PMID:26228631]

2. Baggio R, Elbaum D, Kanto ZF, Carroll PJ, Cavalli RC, Ash DE, Christianson DW. (1997) Inhibition of Mn2+2-Arginase by Borate Leads to the Design of a Transition State Analogue Inhibitor, 2(S)-Amino-6-boronohexanoic Acid. J. Am. Chem. Soc., 119 (34): 8107–8108.

3. Ilies M, Di Costanzo L, North ML, Scott JA, Christianson DW. (2010) 2-aminoimidazole amino acids as inhibitors of the binuclear manganese metalloenzyme human arginase I. J. Med. Chem., 53 (10): 4266-76. [PMID:20441173]

4. Van Zandt MC, Whitehouse DL, Golebiowski A, Ji MK, Zhang M, Beckett RP, Jagdmann GE, Ryder TR, Sheeler R, Andreoli M et al.. (2013) Discovery of (R)-2-amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic acid and congeners as highly potent inhibitors of human arginases I and II for treatment of myocardial reperfusion injury. J. Med. Chem., 56 (6): 2568-80. [PMID:23472952]

How to cite this page

Arginase: Arginase I. Last modified on 16/03/2017. Accessed on 20/01/2019. IUPHAR/BPS Guide to PHARMACOLOGY,