Chemical proteomics reveals hesperidin and hesperetin as AKR1C1/2 inhibitors with chemosensitization effect

The natural flavanone hesperidin and its aglycone hesperetin were identified as human aldo-keto reductase family 1 member C1 (AKR1C1) and AKR1C2 inhibitors via chemoproteomic profiling, which provides mechanistic insight into their chemosensitization effects in cancer therapy.