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NADPH oxidase 1

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Target id: 3001

Nomenclature: NADPH oxidase 1

Abbreviated Name: NOX1

Family: NADPH oxidases

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 6 564 Xq22.1 NOX1 NADPH oxidase 1
Mouse 6 591 X E3 Nox1 NADPH oxidase 1
Rat 6 563 Xq32 Nox1 NADPH oxidase 1
Gene and Protein Information Comments
The longest protein isoform of the human gene is 564 aa long, and known as NOH-1L [2]. NOH-1Lv (isoform 2) is 515 aa and isoform 3 is 527 aa.
Previous and Unofficial Names Click here for help
GP91-2 | MOX1 | NOH1 | GP91 phox homolog | NADH/NADPH mitogenic oxidase subunit p65-mox
Database Links Click here for help
Alphafold Q9Y5S8 (Hs), Q8CIZ9 (Mm), Q9WV87 (Rn)
ChEMBL Target CHEMBL1287628 (Hs), CHEMBL1075231 (Rn)
Ensembl Gene ENSG00000007952 (Hs), ENSMUSG00000031257 (Mm), ENSRNOG00000048706 (Rn)
Entrez Gene 27035 (Hs), 237038 (Mm), 114243 (Rn)
Human Protein Atlas ENSG00000007952 (Hs)
KEGG Gene hsa:27035 (Hs), mmu:237038 (Mm), rno:114243 (Rn)
OMIM 300225 (Hs)
Pharos Q9Y5S8 (Hs)
RefSeq Nucleotide NM_007052 (Hs), NM_172203 (Mm), NM_053683 (Rn)
RefSeq Protein NP_008983 (Hs), NP_757340 (Mm), NP_446135 (Rn)
UniProtKB Q9Y5S8 (Hs), Q8CIZ9 (Mm), Q9WV87 (Rn)
Wikipedia NOX1 (Hs)

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
compound 7c [PMID: 22041175] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 7.0 pKi 3
⤷ pKi 7.0 (Ki 1.01x10-7 M) [3]
setanaxib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.8 pKi 1
⤷ pKi 6.8 (Ki 1.4x10-7 M) [1]
GKT136901 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 6.8 pKi 4
⤷ pKi 6.8 (Ki 1.6x10-7 M) [4]
Description: Cell free assay of ROS production by NOX1 membranes.
NSC 780521 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 5
⤷ pIC50 6.0 (IC50 1.019x10-6 M) [5]
Description: Inhibition of PMA-induced superoxide production in HEK293 cells expressing hNOX1.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Cytokine production & signalling

References

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1. Aoyama T, Paik YH, Watanabe S, Laleu B, Gaggini F, Fioraso-Cartier L, Molango S, Heitz F, Merlot C, Szyndralewiez C et al.. (2012) Nicotinamide adenine dinucleotide phosphate oxidase in experimental liver fibrosis: GKT137831 as a novel potential therapeutic agent. Hepatology, 56 (6): 2316-27. [PMID:22806357]

2. Bánfi B, Maturana A, Jaconi S, Arnaudeau S, Laforge T, Sinha B, Ligeti E, Demaurex N, Krause KH. (2000) A mammalian H+ channel generated through alternative splicing of the NADPH oxidase homolog NOH-1. Science, 287 (5450): 138-42. [PMID:10615049]

3. Gaggini F, Laleu B, Orchard M, Fioraso-Cartier L, Cagnon L, Houngninou-Molango S, Gradia A, Duboux G, Merlot C, Heitz F et al.. (2011) Design, synthesis and biological activity of original pyrazolo-pyrido-diazepine, -pyrazine and -oxazine dione derivatives as novel dual Nox4/Nox1 inhibitors. Bioorg Med Chem, 19 (23): 6989-99. [PMID:22041175]

4. Laleu B, Gaggini F, Orchard M, Fioraso-Cartier L, Cagnon L, Houngninou-Molango S, Gradia A, Duboux G, Merlot C, Heitz F et al.. (2010) First in class, potent, and orally bioavailable NADPH oxidase isoform 4 (Nox4) inhibitors for the treatment of idiopathic pulmonary fibrosis. J Med Chem, 53 (21): 7715-30. [PMID:20942471]

5. Lu J, Risbood P, Kane Jr CT, Hossain MT, Anderson L, Hill K, Monks A, Wu Y, Antony S, Juhasz A et al.. (2017) Characterization of potent and selective iodonium-class inhibitors of NADPH oxidases. Biochem Pharmacol, 143: 25-38. [PMID:28709950]

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