Development of a high-throughput in vitro assay to identify selective inhibitors for human ALDH1A1.
Chemico-Biological Interactions（2015）
Abstract
•Development of in vitro esterase-based HTS for discovery of modulators of ALDH1A1.•Identified 30 hits that selectively inhibited ALDH1A1 compared ALDH2 and ALDH3A1.•Determined first structure of human apo-ALDH1A1 and with its cofactor NADH.
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Key words
Aldehyde dehydrogenase,Retinaldehyde dehydrogenase,High-throughput screen,Small molecule inhibitors,Enzyme inhibition
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