Alda-1
Organic compound
From Wikipedia, the free encyclopedia
Alda-1 is an organic compound that enhances the enzymatic activity of human ALDH2.[1] Alda-1 has been proposed as a potential treatment for the alcohol flush reaction experienced by people with genetically deficient ALDH2.[2]
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| Formula | C15H11Cl2NO3 |
| Molar mass | 324.16 g·mol−1 |
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Mechanism of action
Ethanol is metabolized to acetaldehyde in people, which is then metabolized to acetic acid primarily by ALDH2.[1] People have various ALDH2 alleles. ALDH2*1 is a common allele (wild type), but about 40% of people of East Asian ethnicity have one or two copies of the dominant ALDH2*2 instead, which causes ALDH2 deficiency. If deficient people drink ethanol, they suffer from alcohol flush reaction due to acetaldehyde accumulation.[3]
Four Alda-1 molecules bind to each monomer of ALDH2 tetramer. This enhances NAD+ binding to ALDH2. NAD+ is required by ALDH2 for its enzymatic activity,[4] which is why Alda-1 increases ALDH2 activity by 2.1 fold if ALDH2 is coded by ALDH2*1 and by 11 fold if it is coded ALDH2*2.[2]
History
Chen et al. first reported Alda-1 in 2008.[2][1] Alda-1 is the first known aldehyde dehydrogenase activator.[3]