Structural highlights
Publication Abstract from PubMed
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.
Diethylaminobenzaldehyde Is a Covalent, Irreversible Inactivator of ALDH7A1.,Luo M, Gates KS, Henzl MT, Tanner JJ ACS Chem Biol. 2015 Jan 6. PMID:25554827[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Luo M, Gates KS, Henzl MT, Tanner JJ. Diethylaminobenzaldehyde Is a Covalent, Irreversible Inactivator of ALDH7A1. ACS Chem Biol. 2015 Jan 6. PMID:25554827 doi:http://dx.doi.org/10.1021/cb500977q