Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T88285
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| Former ID |
TTDR01246
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| Target Name |
Lactoylglutathione lyase
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| Gene Name |
GLO1
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| Synonyms |
Aldoketomutase; Glx I; GlxI; Glyoxalase I; Ketone-aldehyde mutase; Methylglyoxalase; S-D-lactoylglutathione methylglyoxal lyase; GLO1
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| Target Type |
Clinical Trial
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| 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.
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| BioChemical Class |
Carbon-sulfur lyases
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| Target Validation |
T88285
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| UniProt ID | |||||
| EC Number |
EC 4.4.1.5
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| Sequence |
MAEPQPPSGGLTDEAALSCCSDADPSTKDFLLQQTMLRVKDPKKSLDFYTRVLGMTLIQK
CDFPIMKFSLYFLAYEDKNDIPKEKDEKIAWALSRKATLELTHNWGTEDDETQSYHNGNS DPRGFGHIGIAVPDVYSACKRFEELGVKFVKKPDDGKMKGLAFIQDPDGYWIEILNPNKM ATLM |
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| Drugs and Mode of Action | |||||
| Drug(s) | NARINGENIN | Drug Info | Phase 1 | Discovery agent | [1] |
| Inhibitor | 2-Sulfhydryl-Ethanol | Drug Info | [2] | ||
| BAICALEIN | Drug Info | [3] | |||
| CYANIDIN | Drug Info | [4] | |||
| KAEMPFEROL | Drug Info | [3] | |||
| NARINGENIN | Drug Info | [3] | |||
| PELARGONIDIN CHLORIDE | Drug Info | [4] | |||
| S-(N-4bromophenyl-N-hydroxycarbamoyl)glutathione | Drug Info | [5] | |||
| S-(N-4chlorophenyl-N-hydroxycarbamoyl)glutathione | Drug Info | [5] | |||
| S-(N-butyl-N-hydroxycarbamoyl)glutathione | Drug Info | [5] | |||
| S-(N-ethyl-N-hydroxycarbamoyl)glutathione | Drug Info | [5] | |||
| S-(N-heptyl-N-hydroxycarbamoyl)glutathione | Drug Info | [5] | |||
| S-(N-hexyl-N-hydroxycarbamoyl)glutathione | Drug Info | [5] | |||
| S-(N-Hydroxy-N-Iodophenylcarbamoyl)Glutathione | Drug Info | [2] | |||
| S-(N-methyl-N-hydroxycarbamoyl)glutathione | Drug Info | [5] | |||
| S-(N-pentyl-N-hydroxycarbamoyl)glutathione | Drug Info | [5] | |||
| S-(N-phenyl-N-hydroxycarbamoyl)glutathione | Drug Info | [5] | |||
| S-(N-propyl-N-hydroxycarbamoyl)glutathione | Drug Info | [5] | |||
| S-Benzyl-Glutathione | Drug Info | [6] | |||
| S-p-bromobenzyl glutatione | Drug Info | [7] | |||
| S-P-Nitrobenzyloxycarbonylglutathione | Drug Info | [6] | |||
| 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 1 | ClinicalTrials.gov (NCT01091077) A Pilot Study of the Grapefruit Flavonoid Naringenin for HCV Infection. U.S. National Institutes of Health. | ||||
| REF 2 | DrugBank 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 3 | Bioorg 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 4 | Bioorg 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 5 | 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. | ||||
| REF 6 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
| REF 7 | J Med Chem. 2009 Aug 13;52(15):4650-6.Inhibition of glyoxalase I: the first low-nanomolar tight-binding inhibitors. | ||||
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