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Overview of AKR1C3: Inhibitor Achievements and Disease Insights

Yang Liu1, Siyu He2, Ying Chen3

  • 1School of Pharmacy, China Pharmaceutical University, Nanjing 211198, People's Republic of China.

Journal of Medicinal Chemistry
|May 29, 2020
PubMed

Insights

Human aldo-keto reductase family 1 member C3 (AKR1C3) regulates hormones and cell growth. This review summarizes AKR1C3 inhibitors for metabolic diseases and cancers, offering insights for future drug discovery.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • Human aldo-keto reductase family 1 member C3 (AKR1C3) is a key enzyme involved in hormone regulation and prostaglandin synthesis.
  • Overexpression of AKR1C3 is linked to metabolic diseases and various carcinomas, contributing to drug resistance.
  • There is a growing need for effective AKR1C3 inhibitors due to its pathological roles.

Purpose of the Study:

  • To review the physiological and pathological functions of AKR1C3.
  • To summarize recent advancements in the development of selective AKR1C3 inhibitors.
  • To provide perspectives on current challenges and future directions for AKR1C3 inhibitor drug discovery.

Main Methods:

  • Literature review of physiological and pathological roles of AKR1C3.
  • Comprehensive summary of recent studies on selective AKR1C3 inhibitors.
  • Analysis of current challenges and therapeutic potential of AKR1C3 inhibitors.

Main Results:

  • AKR1C3 plays a significant role in hormone activity regulation and prostaglandin F synthesis.
  • AKR1C3 overexpression is implicated in metabolic disorders and hormone-dependent/independent cancers.
  • Recent research has focused on developing potent and selective AKR1C3 inhibitors to overcome drug resistance.

Conclusions:

  • Understanding AKR1C3's function is crucial for developing targeted therapies.
  • Selective AKR1C3 inhibitors show promise in treating associated diseases.
  • Further research is needed to address current limitations and optimize AKR1C3 inhibitor development for therapeutic benefit.

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