General Information of Target

Target ID LDTP02072
Target Name Arginase-1 (ARG1)
Gene Name ARG1
Gene ID 383
Synonyms
Arginase-1; EC 3.5.3.1; Liver-type arginase; Type I arginase
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSAKSRTIGIIGAPFSKGQPRGGVEEGPTVLRKAGLLEKLKEQECDVKDYGDLPFADIPN
DSPFQIVKNPRSVGKASEQLAGKVAEVKKNGRISLVLGGDHSLAIGSISGHARVHPDLGV
IWVDAHTDINTPLTTTSGNLHGQPVSFLLKELKGKIPDVPGFSWVTPCISAKDIVYIGLR
DVDPGEHYILKTLGIKYFSMTEVDRLGIGKVMEETLSYLLGRKKRPIHLSFDVDGLDPSF
TPATGTPVVGGLTYREGLYITEEIYKTGLLSGLDIMEVNPSLGKTPEEVTRTVNTAVAIT
LACFGLAREGNHKPIDYLNPPK
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Arginase family
Subcellular location
Cytoplasm
Function
Key element of the urea cycle converting L-arginine to urea and L-ornithine, which is further metabolized into metabolites proline and polyamides that drive collagen synthesis and bioenergetic pathways critical for cell proliferation, respectively; the urea cycle takes place primarily in the liver and, to a lesser extent, in the kidneys.; Functions in L-arginine homeostasis in nonhepatic tissues characterized by the competition between nitric oxide synthase (NOS) and arginase for the available intracellular substrate arginine. Arginine metabolism is a critical regulator of innate and adaptive immune responses. Involved in an antimicrobial effector pathway in polymorphonuclear granulocytes (PMN). Upon PMN cell death is liberated from the phagolysosome and depletes arginine in the microenvironment leading to suppressed T cell and natural killer (NK) cell proliferation and cytokine secretion. In group 2 innate lymphoid cells (ILC2s) promotes acute type 2 inflammation in the lung and is involved in optimal ILC2 proliferation but not survival. In humans, the immunological role in the monocytic/macrophage/dendritic cell (DC) lineage is unsure.
TTD ID
T63224
Uniprot ID
P05089
DrugMap ID
TT7ZQEV
Ensemble ID
ENST00000356962.2
HGNC ID
HGNC:663
ChEMBL ID
CHEMBL1075097

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
AN3CA SNV: p.L31S .
HT115 SNV: p.E42Ter .
LN229 SNV: p.S2R .
MCC13 SNV: p.G154R .
NCIH82 SNV: p.S109C .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
MPP-AC
 Probe Info 
N.A.  LDD0428  [1]
TER-AC
 Probe Info 
N.A.  LDD0426  [1]
TPP-AC
 Probe Info 
N.A.  LDD0427  [1]
PAL-AfBPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Photonaproxen
 Probe Info 
N.A.  LDD0156  [2]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Manganese Small molecular drug DB06757
Ornithine Small molecular drug DB00129
Urea Small molecular drug DB03904
Investigative
Click To Hide/Show 10 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
N(5)-[(Hydroxyamino)(Imino)Methyl]-l-ornithine Small molecular drug DB03144
Ss-(2-hydroxyethyl)Thiocysteine Small molecular drug DB04530
2(S)-amino-6-boronohexanoic Acid . DB01983
Dehydro-2(S)-amino-6-boronohexanoic Acid . DB04585
Descarboxy-nor-n(Omega)-hydroxy-l-arginine . DB04197
Dinor-n(Omega)-hydroxy-l-arginine . DB02499
Nor-noha . DB02381
S-2-(Boronoethyl)-l-cysteine . DB03731
S-propylamine-l-cysteine . DB04648
S-{2-[Amino(Dihydroxy)-lambda~4~-sulfanyl]Ethyl}-d-cysteine . DB02689

References

1 Differently Tagged Probes for Protein Profiling of Mitochondria. Chembiochem. 2019 May 2;20(9):1155-1160. doi: 10.1002/cbic.201800735. Epub 2019 Mar 26.
2 Small Molecule Interactome Mapping by Photoaffinity Labeling Reveals Binding Site Hotspots for the NSAIDs. J Am Chem Soc. 2018 Mar 28;140(12):4259-4268. doi: 10.1021/jacs.7b11639. Epub 2018 Mar 15.
Mass spectrometry data entry: PXD007094