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cytochrome b-245 beta chain

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Target id: 3002

Nomenclature: cytochrome b-245 beta chain

Abbreviated Name: NOX2

Family: NADPH oxidases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 6 570 Xp21.1-p11.4 CYBB cytochrome b-245 beta chain
Mouse 6 570 X A1.1 Cybb cytochrome b-245, beta polypeptide
Rat - 570 Xq12 Cybb cytochrome b-245 beta chain
Previous and Unofficial Names Click here for help
cytochrome b-245 | cytochrome b-245, beta polypeptide | GP91-PHOX | NADPH oxidase 2 | cytochrome b-245, heavy chain
Database Links Click here for help
Alphafold
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
Pharos
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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 Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.9 pKi 2
pKi 5.9 (Ki 1.34x10-6 M) [2]
GKT136901 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.8 pKi 3
pKi 5.8 (Ki 1.53x10-6 M) [3]
Description: Cell free assay of ROS production by NOX2 membranes.
setanaxib Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 5.8 pKi 1
pKi 5.8 (Ki 1.75x10-6 M) [1]
NSC 780521 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.0 pIC50 4
pIC50 6.0 (IC50 1.049x10-6 M) [4]
Description: Inhibition of PMA-induced superoxide production in human PMNs.
Immuno Process Associations
Immuno Process:  Antigen presentation
GO Annotations:  Associated to 1 GO processes
GO:0002479 antigen processing and presentation of exogenous peptide antigen via MHC class I, TAP-dependent TAS
Immuno Process:  Inflammation
GO Annotations:  Associated to 3 GO processes
GO:0006954 inflammatory response ISS
GO:0043312 neutrophil degranulation TAS
GO:0045087 innate immune response IMP
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 1 GO processes, IEA only
click arrow to show/hide IEA associations
GO:0032760 positive regulation of tumor necrosis factor production IEA
Immuno Process:  Cellular signalling
GO Annotations:  Associated to 1 GO processes
GO:0043312 neutrophil degranulation TAS

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. 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]

3. 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]

4. 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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