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Killer Artificial Antigen Presenting Cells (KaAPC) for Efficient In Vitro Depletion of Human Antigen-specific T Cells
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Aldo-Keto Reductase AKR1C1-AKR1C4: Functions, Regulation, and Intervention for Anti-cancer Therapy

Chen-Ming Zeng1, Lin-Lin Chang1, Mei-Dan Ying1

  • 1Zhejiang Province Key Laboratory of Anti-cancer Drug Research, Institute of Pharmacology and Toxicology, College of Pharmaceutical Sciences, Zhejiang University Hangzhou, China.

Frontiers in Pharmacology
|March 30, 2017
PubMed

Insights

Aldo-keto reductases (AKR1C1-AKR1C4) are involved in cancer development and drug resistance through both catalytic and non-catalytic functions. This review explores these roles and potential small molecule inhibitors for cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Aldo-keto reductases (AKR1C1-AKR1C4) are enzymes crucial for various metabolic processes.
  • Their expression is linked to cancer malignancy and therapeutic resistance.
  • Research has primarily focused on their catalytic roles in cancers like prostate and breast cancer.

Purpose of the Study:

  • To review the catalytic-dependent functions of AKR1C isoforms.
  • To explore the emerging understanding of their catalytic-independent roles in biological regulation.
  • To summarize small molecule inhibitors targeting AKR1C family members.

Main Methods:

  • Literature review of studies on AKR1C enzymes.
  • Analysis of research on catalytic and non-catalytic functions.
  • Compilation of information on small molecule inhibitors.

Main Results:

  • AKR1C enzymes exhibit broad substrate specificity, impacting biosynthesis, metabolism, and detoxification.
  • Both catalytic and catalytic-independent functions of AKR1Cs are implicated in cancer progression and drug resistance.
  • Various small molecule inhibitors targeting AKR1Cs have been identified.

Conclusions:

  • AKR1C enzymes play multifaceted roles in cancer, involving both enzymatic activity and non-enzymatic functions.
  • Targeting AKR1Cs offers potential therapeutic strategies for overcoming cancer malignancy and drug resistance.
  • Further research into catalytic-independent functions and inhibitor development is warranted.
Keywords:
aldo–keto reductasescatalytic-dependentcatalytic-independentinhibitortherapy

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