NADPH oxidase 1 | NADPH oxidases | IUPHAR/BPS Guide to PHARMACOLOGY

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NADPH oxidase 1

Target not currently curated in GtoImmuPdb

Target id: 3001

Nomenclature: NADPH oxidase 1

Abbreviated Name: NOX1

Family: NADPH oxidases

Annotation status:  image of a grey circle Awaiting annotation/under development. Please contact us if you can help with annotation.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 6 564 Xq22.1 NOX1 NADPH oxidase 1
Mouse 6 563 Chromosome X, 55.69 cM 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
GP91-2 | MOX1 | NOH1 | GP91 phox homolog | NADH/NADPH mitogenic oxidase subunit p65-mox
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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
compound 7c [PMID: 22041175] Hs Inhibition 7.0 pKi 3
pKi 7.0 (Ki 1.01x10-7 M) [3]
GKT137831 Hs Inhibition 6.8 pKi 1
pKi 6.8 (Ki 1.4x10-7 M) [1]
GKT136901 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 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.

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]

How to cite this page

NADPH oxidases: NADPH oxidase 1. Last modified on 01/05/2018. Accessed on 18/07/2019. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=3001.