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Aromatase inhibitors: structural features and biochemical characterization

Yanyan Hong1, Shiuan Chen

  • 1Department of Surgical Research, Beckman Research Institute of the City of Hope, 1500 E. Duarte Rd., Duarte, CA 91010, USA.

Annals of the New York Academy of Sciences
|January 31, 2007
PubMed

Insights

Aromatase inhibitors (AIs) offer new breast cancer treatments by blocking estrogen synthesis. Research shows aromatase is also present in other cancers, suggesting AIs could be effective there too.

Area of Science:

  • Biochemistry
  • Oncology
  • Endocrinology

Background:

  • Aromatase synthesizes estrogens, crucial for estrogen-dependent breast tumor growth.
  • Estrogen-induced growth factors drive cancer cell proliferation.
  • Aromatase inhibitors (AIs) target estrogen biosynthesis for cancer treatment.

Purpose of the Study:

  • To explore the role of aromatase and AIs in breast cancer and other malignancies.
  • To investigate the expression of aromatase in various cancer types.
  • To review current AI therapies and natural product-derived AIs.

Main Methods:

  • Reverse transcription polymerase chain reaction (RT-PCR) to detect aromatase expression.
  • Immunohistochemical techniques for protein localization of aromatase.
  • Review of FDA-approved AIs and natural anti-aromatase compounds.

Main Results:

  • Aromatase is expressed in endocrine tissues and their tumors, as well as liver, lung, and colon cancers.
  • FDA-approved AIs like anastrozole, letrozole, and exemestane are effective in breast cancer treatment.
  • Natural compounds like flavones and coumarins exhibit anti-aromatase activity.

Conclusions:

  • Aromatase inhibitors show promise for treating not only breast cancer but also other aromatase-expressing cancers.
  • Further research into AI structure-function relationships and novel AI development is ongoing.
  • Understanding aromatase's molecular mechanisms aids in designing more effective inhibitors.

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