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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

Contents:

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 P04839 (Hs), Q61093 (Mm)
ChEMBL Target CHEMBL1287627 (Hs)
Ensembl Gene ENSG00000165168 (Hs), ENSMUSG00000015340 (Mm), ENSRNOG00000003622 (Rn)
Entrez Gene 1536 (Hs), 13058 (Mm), 66021 (Rn)
Human Protein Atlas ENSG00000165168 (Hs)
KEGG Gene hsa:1536 (Hs), mmu:13058 (Mm), rno:66021 (Rn)
OMIM 300481 (Hs)
Pharos P04839 (Hs)
RefSeq Nucleotide NM_000397 (Hs), NM_007807.5 (Mm), NM_023965 (Rn)
RefSeq Protein NP_000388 (Hs), NP_031833.3 (Mm), NP_076455 (Rn)
UniProtKB P04839 (Hs), Q61093 (Mm)
Wikipedia CYBB (Hs)

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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
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
Immuno Process:  Inflammation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Cellular 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. 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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