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PMID: 28352233 Published · epublish English Journal Article Review

Aldo-Keto Reductase AKR1C1-AKR1C4: Functions, Regulation, and Intervention for Anti-cancer Therapy.

Frontiers in pharmacology ·Vol. 8 ·2017-00-00 ·Pages 119

Zeng CM, Chang LL, Ying MD, Cao J, He QJ, Zhu H, Yang B

Abstract

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.

Keywords
aldo–keto reductases catalytic-dependent catalytic-independent inhibitor therapy
Authors & Affiliations
7 authors, click to expand affiliations / ORCID
Zeng Chen-Ming
Zhejiang Province Key Laboratory of Anti-cancer Drug Research, Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University Hangzhou, China.
Chang Lin-Lin
Zhejiang Province Key Laboratory of Anti-cancer Drug Research, Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University Hangzhou, China.
Ying Mei-Dan
Zhejiang Province Key Laboratory of Anti-cancer Drug Research, Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University Hangzhou, China.
Cao Ji
Zhejiang Province Key Laboratory of Anti-cancer Drug Research, Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University Hangzhou, China.
He Qiao-Jun
Zhejiang Province Key Laboratory of Anti-cancer Drug Research, Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University Hangzhou, China.
Zhu Hong
Zhejiang Province Key Laboratory of Anti-cancer Drug Research, Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University Hangzhou, China.
Yang Bo
Zhejiang Province Key Laboratory of Anti-cancer Drug Research, Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University Hangzhou, China.
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Article Info
Journal
Frontiers in pharmacology
Abbr.
Front Pharmacol
ISSN
1663-9812
DOI
10.3389/fphar.2017.00119
Published
2017-00-00
Epub
2017-00-14
Pages
119
Language
English
Region
Switzerland
NLM ID
101548923
PMCID
PMC5349110
External Links
PubMed source DOI: 10.3389/fphar.2017.00119 PMC Full Text View journal details
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