Target General Infomation
Target ID
T76158
Former ID
TTDR01232
Target Name
Glutathione reductase, mitochondrial
Gene Name
GR3
Synonyms
GR; GRase; Glutathione reductase; GR3
Target Type
Research
Function
Maintains high levels of reduced glutathione in the cytosol.
BioChemical Class
Oxidoreductases acting on a sulfur group of donors
Target Validation
T76158
UniProt ID
EC Number
EC 1.8.1.7
Sequence
MVYDLIVIGGGSGGMAAARRAARHNAKVALVEKSRLGGTCVNVGCVPKKIMFNAASVHDI
LENSRHYGFDTKFSFNLPLLVERRDKYIQRLNNIYRQNLSKDKVDLYEGTASFLSENRIL
IKGTKDNNNKDNGPLNEEILEGRNILIAVGNKPVFPPVKGIENTISSDEFFNIKESKKIG
IVGSGYIAVELINVIKRLGIDSYIFARGNRILRKFDESVINVLENDMKKNNINIVTFADV
VEIKKVSDKNLSIHLSDGRIYEHFDHVIYCVGRSPDTENLNLEKLNVETNNNYIVVDENQ
RTSVNNIYAVGDCCMVKKSKEIEDLNLLKLYNEETYLNKKENVTEDIFYNVQLTPVAINA
GRLLADRLFLKKTRKTNYKLIPTVIFSHPPIGTIGLSEEAAIQIYGKENVKIYESKFTNL
FFSVYDIEPELKEKTYLKLVCVGKDELIKGLHIIGLNADEIVQGFAVALKMNATKKDFDE
TIPIHPTAAEEFLTLQPWMK
Drugs and Mode of Action
Drug(s) Methylene blue Drug Info Approved Acquired methemoglobinemia [1]
Inhibitor 1-(2'-chlorophenyl)penta-1,4-dien-3-one Drug Info [2]
2,4,6 trinitrobenzene sulfonate 1,3-bis (2-chlorethyl)-1-nitrosourea Drug Info [3]
3,6-Dihydroxy-Xanthene-9-Propionic Acid Drug Info [4]
3,7-Bis-dimethylamino-phenothiazin-5-ylium Drug Info [5]
3-(Prop-2-Ene-1-Sulfinyl)-Propene-1-Thiol Drug Info [4]
3-Sulfinoalanine Drug Info [4]
4-nitrobenzo[c][1,2,5]thiadiazole Drug Info [6]
Flavin-Adenine Dinucleotide Drug Info [4]
Glutathionylspermidine Disulfide Drug Info [4]
Meta-Nitro-Tyrosine Drug Info [4]
Methylene blue Drug Info [1]
Nicotinamide-Adenine-Dinucleotide Drug Info [4]
Oxidized glutathione Drug Info [3]
Oxidized Glutathione Disulfide Drug Info [7]
Trans-(1S(R),2S(R))-2-Hydroxycyclooctyl nitrate Drug Info [8]
Trans-(R(S))-2-Hydroxy-1-phenylethyl nitrate Drug Info [8]
References
REF 1Recombinant Plasmodium falciparum glutathione reductase is inhibited by the antimalarial dye methylene blue. FEBS Lett. 1998 Feb 6;422(3):311-4.
REF 2J Med Chem. 2005 Nov 17;48(23):7400-10.Irreversible inactivation of trypanothione reductase by unsaturated Mannich bases: a divinyl ketone as key intermediate.
REF 3The purification and properties of glutathione reductase from the cestode Moniezia expansa. Int J Biochem Cell Biol. 1995 Apr;27(4):393-401.
REF 4How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 5J Med Chem. 2004 Nov 18;47(24):5972-83.5-substituted tetrazoles as bioisosteres of carboxylic acids. Bioisosterism and mechanistic studies on glutathione reductase inhibitors as antimalarials.
REF 6Bioorg Med Chem Lett. 2006 Apr 15;16(8):2283-92. Epub 2006 Feb 3.Specific inhibitors of Plasmodium falciparum thioredoxin reductase as potential antimalarial agents.
REF 7DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
REF 8Bioorg Med Chem Lett. 2009 Jul 1;19(13):3661-3. Epub 2009 Apr 24.In vitro inhibition of human erythrocyte glutathione reductase by some new organic nitrates.

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