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

Bioorg Chem. 2017 Apr:71:257-274. doi: 10.1016/j.bioorg.2017.02.011. Epub 2017 Feb 23.

Abstract

Estrogens display intriguing tissue selective action that is of great biomedical importance in the development of optimal therapeutics for the prevention and treatment of breast cancer. There are also strong evidences to show that both endogenous and exogenous estrogens are involved in the pathogenesis of breast cancer. Tamoxifen has been the only drug of choice for more than 30years to treat patients with estrogen related (ER) positive breast tumors. There is a need therefore, for identifying newer, potential and novel candidates for breast cancer. Keeping this in view, the present review focuses on selective estrogen receptor modulators and estrogen antagonists such as sulfatase and aromatase inhibitors involved in breast cancer therapy. A succinct and critical overview of the structure of estrogen receptors, their signaling and involvement in breast carcinogenesis are herein described.

Keywords: Aromatase; Breast cancer; Estrogen receptor; Sulfatase; Tamoxifen.

Publication types

  • Review

MeSH terms

  • Animals
  • Aromatase / metabolism
  • Breast / drug effects*
  • Breast / enzymology
  • Breast / metabolism
  • Breast / pathology
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / enzymology
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Coumarins / chemistry
  • Coumarins / pharmacology
  • Coumarins / therapeutic use
  • Estrogen Antagonists / chemistry
  • Estrogen Antagonists / pharmacology
  • Estrogen Antagonists / therapeutic use*
  • Female
  • Humans
  • Receptors, Estrogen / metabolism
  • Selective Estrogen Receptor Modulators / chemistry
  • Selective Estrogen Receptor Modulators / pharmacology
  • Selective Estrogen Receptor Modulators / therapeutic use*
  • Sulfatases / antagonists & inhibitors
  • Sulfatases / metabolism

Substances

  • Coumarins
  • Estrogen Antagonists
  • Receptors, Estrogen
  • Selective Estrogen Receptor Modulators
  • Aromatase
  • Sulfatases