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Arginase II

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Target id: 1245

Nomenclature: Arginase II

Abbreviated Name: ARG2

Family: Arginase

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 354 14q24.1 ARG2 arginase 2
Mouse - 354 12 C3 Arg2 arginase type II
Rat - 354 6q24 Arg2 arginase 2
Previous and Unofficial Names Click here for help
AII type II arginase | arginase 2 | kidney-type arginase | non-hepatic arginase | Mitochondrial arginase
Database Links Click here for help
Alphafold P78540 (Hs), O08691 (Mm), O08701 (Rn)
BRENDA 3.5.3.1
ChEMBL Target CHEMBL1795148 (Hs)
Ensembl Gene ENSG00000081181 (Hs), ENSMUSG00000021125 (Mm), ENSRNOG00000053811 (Rn)
Entrez Gene 384 (Hs), 11847 (Mm), 29215 (Rn)
Human Protein Atlas ENSG00000081181 (Hs)
KEGG Enzyme 3.5.3.1
KEGG Gene hsa:384 (Hs), mmu:11847 (Mm), rno:29215 (Rn)
OMIM 107830 (Hs)
Pharos P78540 (Hs)
SynPHARM 83384 (in complex with compound 9 [PMID: 23472952])
UniProtKB P78540 (Hs), O08691 (Mm), O08701 (Rn)
Wikipedia ARG2 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of human Arginase-2 complexed with inhibitor 9.
PDB Id:  4HZE
Ligand:  compound 9 [PMID: 23472952]
Resolution:  1.6Å
Species:  Human
References:  3
Enzyme Reaction Click here for help
EC Number: 3.5.3.1

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 8.1 pKi 2
⤷ pKi 8.1 (Ki 8.5x10-9 M) [2]
compound 9 [PMID: 23472952] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 3
⤷ pIC50 6.3 (IC50 5.09x10-7 M) [3]
Immunopharmacology Comments
The role of ARG2 in immuno-oncology is reviewed in [1].
Immuno Process Associations
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes, IEA only
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GO:0045087 innate immune response IEA
Immuno Process:  T cell (activation)
GO Annotations:  Associated to 3 GO processes, IEA only
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GO:0002250 adaptive immune response IEA
GO:1905403 negative regulation of activated CD8-positive, alpha-beta T cell apoptotic process IEA
GO:2000562 negative regulation of CD4-positive, alpha-beta T cell proliferation IEA
Immuno Process:  B cell (activation)
GO Annotations:  Associated to 1 GO processes, IEA only
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GO:0002250 adaptive immune response IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 2 GO processes, IEA only
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GO:0002829 negative regulation of type 2 immune response IEA
GO:2000562 negative regulation of CD4-positive, alpha-beta T cell proliferation IEA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 7 GO processes
GO:0032720 negative regulation of tumor necrosis factor production IMP
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GO:0032651 regulation of interleukin-1 beta production IEA
GO:0032696 negative regulation of interleukin-13 production IEA
GO:0032700 negative regulation of interleukin-17 production IEA
GO:0071641 negative regulation of macrophage inflammatory protein 1 alpha production IEA
GO:0071644 negative regulation of chemokine (C-C motif) ligand 4 production IEA
GO:0071650 negative regulation of chemokine (C-C motif) ligand 5 production IEA
Immuno Process:  Chemotaxis & migration
GO Annotations:  Associated to 4 GO processes, IEA only
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GO:0071641 negative regulation of macrophage inflammatory protein 1 alpha production IEA
GO:0071644 negative regulation of chemokine (C-C motif) ligand 4 production IEA
GO:0071650 negative regulation of chemokine (C-C motif) ligand 5 production IEA
GO:2000562 negative regulation of CD4-positive, alpha-beta T cell proliferation IEA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:2000562 negative regulation of CD4-positive, alpha-beta T cell proliferation IEA

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. Colleluori DM, Ash DE. (2001) Classical and slow-binding inhibitors of human type II arginase. Biochemistry, 40 (31): 9356-62. [PMID:11478904]

3. 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 II. Last modified on 16/03/2017. Accessed on 08/06/2023. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1245.