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Flavones Inhibit the Activity of AKR1B10, a Promising Therapeutic Target for Cancer Treatment

Publication at Faculty of Pharmacy in Hradec Králové |
2015

Abstract

AKR1B10 is an important human enzyme that participates in reduction of retinal, isoprenyl aldehydes as well as procarcinogens. It is indicated that AKR1B10 is implicated in the development of several cancers due to mentioned activities and it is regarded as a promising therapeutic target.

Natural plant compounds (phenolic compounds and alkaloids) were investigated as potential inhibitors of AKR1B10. Flavones (apigenin, luteolin and 7-hydroxyflavone) were described as a new structural type of inhibitors of AKR1B10.

They significantly inhibited the the AKR1B10 activity also in intact cells without considerable cytotoxic effects. They can serve as model compounds for the design and future development of structurally related AKR1B10 inhibitors with even better characterstics.