Target Information

Target General Infomation
Target ID
T88285
Former ID
TTDR01246
Target Name
Lactoylglutathione lyase
Gene Name
GLO1
Synonyms
Aldoketomutase; Glx I; GlxI; Glyoxalase I; Ketone-aldehyde mutase; Methylglyoxalase; S-D-lactoylglutathione methylglyoxal lyase; GLO1
Target Type
Clinical Trial
Function
Catalyzes the conversion of hemimercaptal, formed from methylglyoxal and glutathione, to S-lactoylglutathione. Involved in the regulation of TNF-induced transcriptional activity of NF- kappa-B. Required for normal osteoclastogenesis.
BioChemical Class
Carbon-sulfur lyases
Target Validation
T88285
UniProt ID
Q04760
EC Number
EC 4.4.1.5
Sequence
MAEPQPPSGGLTDEAALSCCSDADPSTKDFLLQQTMLRVKDPKKSLDFYTRVLGMTLIQK
CDFPIMKFSLYFLAYEDKNDIPKEKDEKIAWALSRKATLELTHNWGTEDDETQSYHNGNS
DPRGFGHIGIAVPDVYSACKRFEELGVKFVKKPDDGKMKGLAFIQDPDGYWIEILNPNKM
ATLM
Drugs and Mode of Action
Drug(s) NARINGENIN Drug Info Phase 1 Discovery agent [522980]
Inhibitor 2-Sulfhydryl-Ethanol Drug Info [551391]
BAICALEIN Drug Info [529300]
CYANIDIN Drug Info [531133]
KAEMPFEROL Drug Info [529300]
NARINGENIN Drug Info [529300]
PELARGONIDIN CHLORIDE Drug Info [531133]
S-(N-4bromophenyl-N-hydroxycarbamoyl)glutathione Drug Info [535065]
S-(N-4chlorophenyl-N-hydroxycarbamoyl)glutathione Drug Info [535065]
S-(N-butyl-N-hydroxycarbamoyl)glutathione Drug Info [535065]
S-(N-ethyl-N-hydroxycarbamoyl)glutathione Drug Info [535065]
S-(N-heptyl-N-hydroxycarbamoyl)glutathione Drug Info [535065]
S-(N-hexyl-N-hydroxycarbamoyl)glutathione Drug Info [535065]
S-(N-Hydroxy-N-Iodophenylcarbamoyl)Glutathione Drug Info [551391]
S-(N-methyl-N-hydroxycarbamoyl)glutathione Drug Info [535065]
S-(N-pentyl-N-hydroxycarbamoyl)glutathione Drug Info [535065]
S-(N-phenyl-N-hydroxycarbamoyl)glutathione Drug Info [535065]
S-(N-propyl-N-hydroxycarbamoyl)glutathione Drug Info [535065]
S-Benzyl-Glutathione Drug Info [551393]
S-p-bromobenzyl glutatione Drug Info [530262]
S-P-Nitrobenzyloxycarbonylglutathione Drug Info [551393]
Pathways
BioCyc Pathway Methylglyoxal degradation I
KEGG Pathway Pyruvate metabolism
NetPath Pathway TCR Signaling Pathway
PathWhiz Pathway Pyruvaldehyde Degradation
Pyruvate Metabolism
Reactome Pyruvate metabolism
References
Ref 522980ClinicalTrials.gov (NCT01091077) A Pilot Study of the Grapefruit Flavonoid Naringenin for HCV Infection. U.S. National Institutes of Health.
Ref 529300Bioorg Med Chem. 2008 Apr 1;16(7):3969-75. Epub 2008 Jan 24.Structure-activity relationship of human GLO I inhibitory natural flavonoids and their growth inhibitory effects.
Ref 530262J Med Chem. 2009 Aug 13;52(15):4650-6.Inhibition of glyoxalase I: the first low-nanomolar tight-binding inhibitors.
Ref 531133Bioorg Med Chem. 2010 Oct 1;18(19):7029-33. Epub 2010 Aug 9.Delphinidin, a dietary anthocyanidin in berry fruits, inhibits human glyoxalase I.
Ref 535065Role of hydrophobic interactions in binding S-(N-aryl/alkyl-N-hydroxycarbamoyl)glutathiones to the active site of the antitumor target enzyme glyoxalase I. J Med Chem. 2000 Oct 19;43(21):3981-6.
Ref 551391DrugBank 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 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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