Inducible NOS | Nitric oxide synthases | IUPHAR/MMV Guide to MALARIA PHARMACOLOGY

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Inducible NOS

Target id: 1250

Nomenclature: Inducible NOS

Abbreviated Name: iNOS

Family: Nitric oxide synthases

Contents:

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - - NOS2 nitric oxide synthase 2
Mouse - - Nos2 nitric oxide synthase 2
Rat - - Nos2 nitric oxide synthase 2
Previous and Unofficial Names
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
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), ENSRNOG00000011023 (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
EC Number: 1.14.13.39
Products
Product Species Reference
NO Human
L-citrulline Human
Cofactors
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

Download all structure-activity data for this target as a CSV file

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
L-NNA Hs Inhibition 6.2 pKi 2
⤷ pKi 6.2 (Ki 6.7x10-7 M) [2]
GW274150 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
GO Annotations:  Associated to 4 GO processes
GO:0002227 innate immune response in mucosa NAS
GO:0006954 inflammatory response TAS
GO:1900015 regulation of cytokine production involved in inflammatory response IDA
click arrow to show/hide IEA associations
GO:0071346 cellular response to interferon-gamma IEA
Immuno Process:  Immune regulation
GO Annotations:  Associated to 1 GO processes
GO:1900015 regulation of cytokine production involved in inflammatory response IDA
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 7 GO processes
GO:0019221 cytokine-mediated signaling pathway TAS
GO:0034612 response to tumor necrosis factor IMP
GO:0071345 cellular response to cytokine stimulus ISO
GO:0071347 cellular response to interleukin-1 IEP
GO:0071356 cellular response to tumor necrosis factor IEP
GO:1900015 regulation of cytokine production involved in inflammatory response IDA
click arrow to show/hide IEA associations
GO:0071346 cellular response to interferon-gamma 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. 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]

Contributors

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