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Inducible NOS

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Target id: 1250

Nomenclature: Inducible NOS

Abbreviated Name: iNOS

Family: Nitric oxide synthases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1153 17q11.2 NOS2 nitric oxide synthase 2
Mouse - 1144 11 46.74 cM Nos2 nitric oxide synthase 2, inducible
Rat - 1147 10q25 Nos2 nitric oxide synthase 2
Previous and Unofficial Names Click here for help
NOS2A | HEP-NOS | nitric oxide synthase 2A (inducible, hepatocytes) | Nitric oxide synthase 2 inducible | Nitric oxide synthase 2 inducible macrophage | inducible NO synthase | Nitric oxide synthase 2 / NOSII | inducible macrophage NOS | nitric oxide synthase 2
Database Links Click here for help
Alphafold P35228 (Hs), P29477 (Mm), Q06518 (Rn)
BRENDA 1.14.13.39
CATH/Gene3D 3.40.50.360
ChEMBL Target CHEMBL4481 (Hs), CHEMBL3464 (Mm), CHEMBL3051 (Rn)
DrugBank Target P35228 (Hs)
Ensembl Gene ENSG00000007171 (Hs), ENSMUSG00000020826 (Mm), ENSRNOG00000057443 (Rn)
Entrez Gene 4843 (Hs), 18126 (Mm), 24599 (Rn)
Human Protein Atlas ENSG00000007171 (Hs)
KEGG Enzyme 1.14.13.39
KEGG Gene hsa:4843 (Hs), mmu:18126 (Mm), rno:24599 (Rn)
OMIM 163730 (Hs)
Pharos P35228 (Hs)
UniProtKB P35228 (Hs), P29477 (Mm), Q06518 (Rn)
Wikipedia NOS2 (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 6.2 pKi 2
⤷ pKi 6.2 (Ki 6.7x10-7 M) [2]
tilarginine Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.1 pKi 4
⤷ pKi 6.1 (Ki 8.6x10-7 M) [4]
GW274150 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.2 pIC50 3
⤷ pIC50 7.2 (IC50 7x10-8 M) [3]
Immunopharmacology Comments
The role of iNOS in immuno-oncology is reviewed in [1].
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling

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. 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]

3. 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]

4. 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

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