cytochrome b-245 beta chain | NADPH oxidases | IUPHAR/BPS Guide to PHARMACOLOGY

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cytochrome b-245 beta chain

Target not currently curated in GtoImmuPdb

Target id: 3002

Nomenclature: cytochrome b-245 beta chain

Abbreviated Name: NOX2

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 6 570 Xp21.1-p11.4 CYBB cytochrome b-245 beta chain
Mouse 6 570 Chromosome X, 4.30 cM; X A1.1 Cybb cytochrome b-245, beta polypeptide
Rat - 570 Xq12 Cybb cytochrome b-245 beta chain
Previous and Unofficial Names
cytochrome b-245 | cytochrome b-245, beta polypeptide | GP91-PHOX | NADPH oxidase 2 | cytochrome b-245, heavy chain
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia

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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] Hs Inhibition 5.9 pKi 2
pKi 5.9 (Ki 1.34x10-6 M) [2]
GKT136901 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.
GKT137831 Hs Inhibition 5.8 pKi 1
pKi 5.8 (Ki 1.75x10-6 M) [1]
NSC 780521 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.

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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