Top ▲

Arginase I

Click here for help

Target id: 1244

Nomenclature: Arginase I

Abbreviated Name: ARG1

Family: Arginase

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 322 6q23.2 ARG1 arginase 1
Mouse - 323 10 A4 Arg1 arginase, liver
Rat - 323 1p12 Arg1 arginase 1
Previous and Unofficial Names Click here for help
Liver arginase | AI type I arginase | PGIF | cytosolic arginase | arginase
Database Links Click here for help
Alphafold P05089 (Hs), Q61176 (Mm), P07824 (Rn)
BRENDA 3.5.3.1
ChEMBL Target CHEMBL1075097 (Hs), CHEMBL4630836 (Mm), CHEMBL3232699 (Rn)
Ensembl Gene ENSG00000118520 (Hs), ENSMUSG00000019987 (Mm), ENSRNOG00000013304 (Rn)
Entrez Gene 383 (Hs), 11846 (Mm), 29221 (Rn)
Human Protein Atlas ENSG00000118520 (Hs)
KEGG Enzyme 3.5.3.1
KEGG Gene hsa:383 (Hs), mmu:11846 (Mm), rno:29221 (Rn)
OMIM 608313 (Hs)
Pharos P05089 (Hs)
SynPHARM 83383 (in complex with compound 9 [PMID: 23472952])
UniProtKB P05089 (Hs), Q61176 (Mm), P07824 (Rn)
Wikipedia ARG1 (Hs)
Selected 3D Structures Click here for help
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 Click here for help
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 go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
2(S)-amino-6-boronohexanoic acid Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.3 pKd 2
⤷ pKd 8.3 (Kd 5x10-9 M) [2]
A1P Small molecule or natural product Hs Inhibition 5.7 pKd 3
⤷ pKd 5.7 (Kd 2x10-6 M) [3]
Description: Dissociation constant measured using surface plasmon resonance assay.
A1P Small molecule or natural product Primary target of this compound 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] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.7 pIC50 4
⤷ pIC50 6.7 (IC50 2.23x10-7 M) [4]
Immunopharmacology Comments
The role of ARG1 in immuno-oncology is reviewed in [1].

References

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 03/12/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1244.