Arginase I | Arginase | IUPHAR Guide to IMMUNOPHARMACOLOGY

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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
BRENDA
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human Arginase-1 complexed with inhibitor 9.
PDB Id:  4HWW
Ligand:  compound 9 [PMID: 23472952]
Resolution:  1.3Å
Species:  Human
References:  4
Enzyme Reaction
EC Number: 3.5.3.1
Description Reaction Reference
L-arginine + H2O <=> L-ornithine + urea

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

Inhibitors
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]

References

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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, http://guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1244.