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glutathione-disulfide reductase

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Target not currently curated in GtoImmuPdb

Target id: 2613

Nomenclature: glutathione-disulfide reductase

Family: 1.-.-.- Oxidoreductases

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 522 8p12 GSR glutathione-disulfide reductase
Mouse - 500 8 20.69 cM Gsr glutathione reductase
Rat - 424 16q12.3 Gsr glutathione-disulfide reductase
Previous and Unofficial Names Click here for help
glutathione reductase, mitochondrial | glutathione reductase
Database Links Click here for help
Alphafold
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal Structure of human Glutathione Reductase complexed with a Fluoro-Analogue of the Menadione Derivative M5
PDB Id:  2GH5
Resolution:  1.7Å
Species:  Human
References:  1
Image of receptor 3D structure from RCSB PDB
Description:  Catalytic cycle of human glutathione reductase near 1 A resolution
PDB Id:  3DJG
Resolution:  1.8Å
Species:  Human
References:  2
Enzyme Reaction Click here for help
EC Number: 1.8.1.7

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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
carmustine Small molecule or natural product Approved drug Primary target of this compound N/A Inhibition 4.2 pIC50 3
pIC50 4.2 (IC50 7.1x10-5 M) [3]
Description: The enzyme inhibition assay uses purified S. cerevisiae glutathione reductase
oxiglutatione Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition - -
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Inhibitor Comments
Apart from the CHEMBL listing of oxiglutatione as an approved drug acting at glutathione reductase and one PubMed reference describing a its use in a single clinical case study [4], there is very little information available about this drug and its mechanism of action.
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Hemolytic anemia due to glutathione reductase deficiency
Orphanet: ORPHA90030

References

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1. Bauer H, Fritz-Wolf K, Winzer A, Kühner S, Little S, Yardley V, Vezin H, Palfey B, Schirmer RH, Davioud-Charvet E. (2006) A fluoro analogue of the menadione derivative 6-[2'-(3'-methyl)-1',4'-naphthoquinolyl]hexanoic acid is a suicide substrate of glutathione reductase. Crystal structure of the alkylated human enzyme. J Am Chem Soc, 128 (33): 10784-94. [PMID:16910673]

2. Berkholz DS, Faber HR, Savvides SN, Karplus PA. (2008) Catalytic cycle of human glutathione reductase near 1 A resolution. J Mol Biol, 382 (2): 371-84. [PMID:18638483]

3. Liu X, Sturla SJ. (2009) Profiling patterns of glutathione reductase inhibition by the natural product illudin S and its acylfulvene analogues. Mol Biosyst, 5 (9): 1013-24. [PMID:19668867]

4. Nakatani Y, Nishimura A, Sugiyama K. (2013) Successful treatment of corneal wasp sting-induced panuveitis with vitrectomy. J Ophthalmic Inflamm Infect, 3 (1): 18. [PMID:23514564]

How to cite this page

1.-.-.- Oxidoreductases: glutathione-disulfide reductase. Last modified on 13/08/2015. Accessed on 26/09/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=2613.