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Glyoxalase 1 (GLO1)

Target: GLO1
Molecular classification: Enzyme

Overview

Glyoxalase 1 (GLO1) is a ubiquitous enzyme crucial for detoxifying methylglyoxal (MG), a cytotoxic byproduct of glycolysis. GLO1 catalyzes the conversion of MG, after it reacts with glutathione, into S-D-lactoylglutathione, which is further processed. It's a therapeutic target in cancer (inhibition) and potentially in conditions involving oxidative stress/AGE accumulation (activation).

Other names: Lactoylglutathione lyaseMethylglyoxalaseAldoketomutaseKetone-aldehyde mutase(R)-S-lactoylglutathione methylglyoxal-lyase

Mechanism of action

GLO1 catalyzes the conversion of methylglyoxal-glutathione hemithioacetal to S-D-lactoylglutathione. Inhibitors block this enzymatic activity. Activators increase GLO1 expression or activity.

Biological functions

Detoxification of methylglyoxalMaintenance of cellular viability

Disease associations

CancerOxidative stress-related diseasesAdvanced glycation end-product (AGE)-related diseases

Safety considerations

Inhibition of GLO1 may have off-target effects due to its ubiquitous naturePotential for drug resistance in cancer cells with elevated GLO1 expressionBalancing GLO1 inhibition in cancer with potential impact on normal cells.

Interacting drugs

Candesartan

8 more in the full profile.

Biomarkers

GLO1 expression levels in tumor tissue (for cancer therapy)Methylglyoxal levels (indicator of GLO1 activity/dysfunction)

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