Estrogen receptor agonists/antagonists in breast cancer therapy: A critical review

A Jameera Begam1, S Jubie1, M J Nanjan2

  • 1Department of Pharmaceutical Chemistry, JSS College of Pharmacy, Udhagamandalam, India; A Constituent College of JSS University, Mysore, India.

Bioorganic Chemistry
|March 10, 2017
PubMed

Insights

Newer breast cancer therapies are needed as Tamoxifen is the sole option for estrogen-related tumors. This review explores selective estrogen receptor modulators and antagonists for improved breast cancer treatment.

Area of Science:

  • Oncology
  • Endocrinology
  • Pharmacology

Background:

  • Estrogen's tissue-selective actions are crucial for breast cancer therapeutics.
  • Estrogens, both endogenous and exogenous, play a role in breast cancer development.
  • Tamoxifen has been the primary treatment for estrogen receptor-positive breast tumors for over 30 years.

Purpose of the Study:

  • To review novel therapeutic candidates for breast cancer.
  • To focus on selective estrogen receptor modulators and estrogen antagonists.
  • To provide an overview of estrogen receptors, signaling, and their role in breast carcinogenesis.

Main Methods:

  • Literature review of selective estrogen receptor modulators.
  • Analysis of estrogen antagonists, including sulfatase and aromatase inhibitors.
  • Critical overview of estrogen receptor structure and signaling pathways.

Main Results:

  • Identified selective estrogen receptor modulators and antagonists as key therapeutic targets.
  • Highlighted the involvement of estrogen receptor signaling in breast cancer.
  • Discussed the limitations of current therapies and the need for novel agents.

Conclusions:

  • Selective estrogen receptor modulators and antagonists offer promising avenues for breast cancer therapy.
  • Understanding estrogen receptor signaling is vital for developing effective breast cancer treatments.
  • There is a significant need for novel therapeutic strategies beyond Tamoxifen for estrogen-related breast cancers.

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