Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTV9A7R)

• DTT Name: Lactoylglutathione lyase (GLO1)
• Synonyms: S-D-lactoylglutathione methylglyoxal lyase; Methylglyoxalase; Ketone-aldehyde mutase; Glyoxalase I; GlxI; Glx I; GLO1; Aldoketomutase
• Gene Name: GLO1
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Carbon-sulfur lyases
• UniProt ID: LGUL_HUMAN
• TTD ID: T88285
• EC Number: EC 4.4.1.5
• Sequence:
  MAEPQPPSGGLTDEAALSCCSDADPSTKDFLLQQTMLRVKDPKKSLDFYTRVLGMTLIQK
  CDFPIMKFSLYFLAYEDKNDIPKEKDEKIAWALSRKATLELTHNWGTEDDETQSYHNGNS
  DPRGFGHIGIAVPDVYSACKRFEELGVKFVKKPDDGKMKGLAFIQDPDGYWIEILNPNKM
  ATLM
• 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.
• KEGG Pathway: Pyruvate metabolism (hsa00620)
• Reactome Pathway: Pyruvate metabolism (R-HSA-70268)

Molecular Interaction Atlas (MIA) of This DTT

2 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
BAICALEIN	DM4C7E6	Influenza virus infection	1E30-1E32	Phase 2	[1]
NARINGENIN	DMHAZLM	N. A.	N. A.	Phase 1	[1]

18 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-Sulfhydryl-Ethanol	DMJBO3D	Discovery agent	N.A.	Investigative	[2]
CYANIDIN	DMZBDO1	Discovery agent	N.A.	Investigative	[3]
KAEMPFEROL	DMHEMUB	Discovery agent	N.A.	Investigative	[1]
PELARGONIDIN CHLORIDE	DMAW0R7	Discovery agent	N.A.	Investigative	[3]
S-(N-4bromophenyl-N-hydroxycarbamoyl)glutathione	DM3FXPV	Discovery agent	N.A.	Investigative	[4]
S-(N-4chlorophenyl-N-hydroxycarbamoyl)glutathione	DMPURE8	Discovery agent	N.A.	Investigative	[4]
S-(N-butyl-N-hydroxycarbamoyl)glutathione	DMU7EQV	Discovery agent	N.A.	Investigative	[4]
S-(N-ethyl-N-hydroxycarbamoyl)glutathione	DMMETC2	Discovery agent	N.A.	Investigative	[4]
S-(N-heptyl-N-hydroxycarbamoyl)glutathione	DMV6T1Q	Discovery agent	N.A.	Investigative	[4]
S-(N-hexyl-N-hydroxycarbamoyl)glutathione	DMSWHMI	Discovery agent	N.A.	Investigative	[4]
S-(N-Hydroxy-N-Iodophenylcarbamoyl)Glutathione	DM1AHIW	Discovery agent	N.A.	Investigative	[2]
S-(N-methyl-N-hydroxycarbamoyl)glutathione	DM1C9W3	Discovery agent	N.A.	Investigative	[4]
S-(N-pentyl-N-hydroxycarbamoyl)glutathione	DM4E9J2	Discovery agent	N.A.	Investigative	[4]
S-(N-phenyl-N-hydroxycarbamoyl)glutathione	DMECAS0	Discovery agent	N.A.	Investigative	[4]
S-(N-propyl-N-hydroxycarbamoyl)glutathione	DMRFKZ6	Discovery agent	N.A.	Investigative	[4]
S-Benzyl-Glutathione	DMIQU8D	Discovery agent	N.A.	Investigative	[5]
S-p-bromobenzyl glutatione	DMFXJKB	Discovery agent	N.A.	Investigative	[6]
S-P-Nitrobenzyloxycarbonylglutathione	DMYBCEG	Discovery agent	N.A.	Investigative	[5]

References

• [1] Structure-activity relationship of human GLO I inhibitory natural flavonoids and their growth inhibitory effects. Bioorg Med Chem. 2008 Apr 1;16(7):3969-75.
• [2] DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41.
• [3] Delphinidin, a dietary anthocyanidin in berry fruits, inhibits human glyoxalase I. Bioorg Med Chem. 2010 Oct 1;18(19):7029-33.
• [4] Role 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.
• [5] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [6] Inhibition of glyoxalase I: the first low-nanomolar tight-binding inhibitors. J Med Chem. 2009 Aug 13;52(15):4650-6.