Diethylaminobenzaldehyde Is a Covalent, Irreversible Inactivator of ALDH7A1
Copyright policy )Diethylaminobenzaldehyde Is a Covalent, Irreversible Inactivator of ALDH7A1
There is growing interest in aldehyde dehydrogenases (ALDHs) because of their overexpression in cancer stem cells and the ability to mediate resistance to cancer drugs. Here, we report the first crystal structure of an aldehyde dehydrogenase complexed with the inhibitor 4-diethylaminobenzaldehyde (DEAB). Contrary to the widely held belief that DEAB is a reversible inhibitor of ALDHs, we show that DEAB irreversibly inactivates ALDH7A1 via formation of a stable, covalent acyl-enzyme species.
- University of Missouri United States
Models, Molecular, Binding Sites, Hydrogen Bonding, Aldehyde Dehydrogenase, Crystallography, X-Ray, NAD, Protein Structure, Secondary, Protein Structure, Tertiary, Benzaldehydes, Drug Discovery, Humans, Enzyme Inhibitors, Protein Binding
Models, Molecular, Binding Sites, Hydrogen Bonding, Aldehyde Dehydrogenase, Crystallography, X-Ray, NAD, Protein Structure, Secondary, Protein Structure, Tertiary, Benzaldehydes, Drug Discovery, Humans, Enzyme Inhibitors, Protein Binding
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