TY - JOUR AU - Zeng, Chen-Ming AU - Chang, Lin-Lin AU - Ying, Mei-Dan AU - Cao, Ji AU - He, Qiao-Jun AU - Zhu, Hong AU - Yang, Bo PY - 2017 M3 - Review TI - Aldo–Keto Reductase AKR1C1–AKR1C4: Functions, Regulation, and Intervention for Anti-cancer Therapy JO - Frontiers in Pharmacology UR - https://www.frontiersin.org/articles/10.3389/fphar.2017.00119 VL - 8 SN - 1663-9812 N2 - Aldo–keto reductases comprise of AKR1C1–AKR1C4, four enzymes that catalyze NADPH dependent reductions and have been implicated in biosynthesis, intermediary metabolism, and detoxification. Recent studies have provided evidences of strong correlation between the expression levels of these family members and the malignant transformation as well as the resistance to cancer therapy. Mechanistically, most studies focus on the catalytic-dependent function of AKR1C isoforms, like their impeccable roles in prostate cancer, breast cancer, and drug resistance due to the broad substrates specificity. However, accumulating clues showed that catalytic-independent functions also played critical roles in regulating biological events. This review summarizes the catalytic-dependent and -independent roles of AKR1Cs, as well as the small molecule inhibitors targeting these family members. ER -