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Updated: Jul 16, 2025

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
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Research progress on tamoxifen and its analogs associated with nuclear receptors

Ning Dong1, Yongli Du1, Yong Zheng1

  • 1School of Chemistry & Chemical Engineering, Qilu University of Technology (Shandong Academy of Sciences), Jinan, 250353, China.

Future Medicinal Chemistry
|September 14, 2023
PubMed

Insights

Tamoxifen analogs show promise for treating breast, liver cancer, and osteoporosis by modulating estrogen receptors (ERs) and ERRβ/γ. Research guides development of novel tamoxifen-based therapies.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Endocrinology

Background:

  • Tamoxifen is a crucial drug for breast cancer, liver cancer, and osteoporosis.
  • Its triphenylethylene structure serves as a basis for developing novel receptor modulators.
  • Selective estrogen receptor modulators (SERMs) are vital in treating hormone-dependent diseases.

Purpose of the Study:

  • To summarize research on tamoxifen analogs modulating estrogen receptors (ERα), ERRβ, and ERRγ.
  • To review structure-activity relationships of these novel tamoxifen analogs.
  • To guide the development of new tamoxifen analogs for nuclear receptor-mediated diseases.

Main Methods:

  • Literature review of published research on tamoxifen analogs.
  • Analysis of structural modifications and their impact on receptor modulation.
  • Correlation of tamoxifen analog activity with disease treatment potential.

Main Results:

  • Over 20 novel tamoxifen analogs have been synthesized.
  • Specific analogs demonstrate potent modulation of ERα (16 compounds), ERRβ (1 inverse agonist), and ERRγ (6 inverse agonists).
  • Established structure-activity relationships for these receptor modulators.

Conclusions:

  • Tamoxifen analogs offer diverse therapeutic potential beyond breast cancer.
  • Targeting ERα, ERRβ, and ERRγ with tamoxifen derivatives is a promising strategy.
  • Further research into these analogs can lead to novel treatments for various diseases.
Keywords:
ERRβ inverse agonistERRγ inverse agonistsERα modulatorsSARTamoxifen and its analogs

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