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Endothelial NOS

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Target not currently curated in GtoImmuPdb

Target id: 1249

Nomenclature: Endothelial NOS

Abbreviated Name: eNOS

Family: Nitric oxide synthases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1203 7q36.1 NOS3 nitric oxide synthase 3
Mouse - 1202 5 11.32 cM Nos3 nitric oxide synthase 3, endothelial cell
Rat - 1202 Nos3 nitric oxide synthase 3
Previous and Unofficial Names Click here for help
endothelial nitric oxide synthase | EC-NOS | endothelial NOS | constitutive NOS | cNOS | Nitric oxide synthase 3 / NOSIII | nitric oxide synthase 3 (endothelial cell) | nitric oxide synthase 3
Database Links Click here for help
Alphafold P29474 (Hs)
BRENDA 1.14.13.39
CATH/Gene3D 3.40.50.360
ChEMBL Target CHEMBL4803 (Hs), CHEMBL2643 (Mm), CHEMBL1075230 (Rn)
DrugBank Target P29474 (Hs)
Ensembl Gene ENSG00000164867 (Hs), ENSMUSG00000028978 (Mm), ENSRNOG00000009348 (Rn)
Entrez Gene 4846 (Hs), 18127 (Mm), 24600 (Rn)
Human Protein Atlas ENSG00000164867 (Hs)
KEGG Enzyme 1.14.13.39
KEGG Gene hsa:4846 (Hs), mmu:18127 (Mm), rno:24600 (Rn)
Pharos P29474 (Hs)
UniProtKB P29474 (Hs), P70313 (Mm), Q62600 (Rn)
Wikipedia NOS3 (Hs)
Enzyme Reaction Click here for help
EC Number: 1.14.13.39
Products Click here for help
Product Species Reference
NO Human
L-citrulline Human
Cofactors Click here for help
Cofactor Species Comments Reference
Zn2+ Human
NADPH Human
heme Human
flavin adenine dinucleotide Human
flavin mononucleotide Human
BH4 Human
oxygen Human
Endogenous Substrate (Human)
L-arginine

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
L-NNA Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pKi 1
⤷ pKi 7.5 (Ki 3x10-8 M) [1]
tilarginine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.4 pKi 3
⤷ pKi 6.4 (Ki 4x10-7 M) [3]
GW274150 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 4.5 pIC50 2
⤷ pIC50 4.5 (IC50 3.4x10-5 M) [2]
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 3 GO processes
GO:0034097 response to cytokine IEP
GO:0036017 response to erythropoietin IEP
GO:0071356 cellular response to tumor necrosis factor IEP

References

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1. Collins JL, Shearer BG, Oplinger JA, Lee S, Garvey EP, Salter M, Duffy C, Burnette TC, Furfine ES. (1998) N-Phenylamidines as selective inhibitors of human neuronal nitric oxide synthase: structure-activity studies and demonstration of in vivo activity. J Med Chem, 41 (15): 2858-71. [PMID:9667974]

2. Connolly S, Aberg A, Arvai A, Beaton HG, Cheshire DR, Cook AR, Cooper S, Cox D, Hamley P, Mallinder P et al.. (2004) 2-aminopyridines as highly selective inducible nitric oxide synthase inhibitors. Differential binding modes dependent on nitrogen substitution. J Med Chem, 47 (12): 3320-3. [PMID:15163211]

3. Shearer BG, Lee S, Franzmann KW, White HA, Sanders DC, Kiff RJ, Garvey EP, Furfine ES. (1997) Conformationally restricted arginine analogues as inhibitors of human nitric oxide synthase. Bioorganic and Medicinal Chemistry Letters, 7: 1763-1768. DOI: 10.1016/S0960-894X(97)00309-0

Contributors

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