Aldehyde Dehydrogenase 2 (ALDH2), mitochondrial is a member of the ALDH superfamily that participates in multiple metabolic pathways including the oxidation of toxic biogenic and environmental aldehydes. ALDH2 is a key enzyme located in the mitochondrial matrix. It plays an important role in ethanol metabolism by converting acetaldehyde, a carcinogenic metabolite of ethanol to acetate. Imbalances of ALDH2 have been linked to both alcoholism and alcohol sensitivity in people. Reduced ALDH2 activity has been strongly correlated with reduced alcohol consumption and reduced incidences of alcoholism, which led to the development of selective ALDH2 inhibitors as antidipsotropic or alcohol aversive agents for treating alcoholism. Disulfiram, an alcohol-aversive drug inhibiting ALDH2 has been approved by the FDA and is used clinically for over 40 years for treating alcohol dependency. However, the drug is a non-specific alkylating agent leading to many adverse side effects and drug-drug interactions. Thus, novel and specific inhibitors of ALDH2 free of the negative side effects could be used in aversion therapy. BioVision’s Aldehyde Dehydrogenase 2 Inhibitor Screening Kit provides a quick and sensitive way of screening, studying and characterising potential inhibitors of ALDH2. In this assay, acetaldehyde is oxidised by ALDH2 to form NADH, which then couples with PicoProbe™ to generate a fluorescence signal measured at Ex/Em = 535/587 nm. The percentage inhibition can be determined by comparing the activity of ALDH2 treated with test inhibitor(s) vs untreated control.
Biochemical and cellular assays