An overview on Estrogen receptors signaling and its ligands in breast cancer

Eur J Med Chem. 2022 Nov 5:241:114658. doi: 10.1016/j.ejmech.2022.114658. Epub 2022 Aug 8.

Abstract

Estrogen governs the regulations of various pathological and physiological actions throughout the body in both males and females. Generally, 17β-estradiol an endogenous estrogen is responsible for different health problems in pre and postmenopausal women. The major activities of endogenous estrogen are executed by nuclear estrogen receptors (ERs) ERα and ERβ while non-genomic cytoplasmic pathways also govern cell growth and apoptosis. Estrogen accomplished a fundamental role in the formation and progression of breast cancer. In this review, we have hyphenated different studies regarding ERs and a thorough and detailed study of estrogen receptors is presented. This review highlights different aspects of estrogens ranging from receptor types, their isoforms, structures, signaling pathways of ERα, ERβ and GPER along with their crystal structures, pathological roles of ER, ER ligands, and therapeutic strategies to overcome the resistance.

Keywords: Breast cancer; ER ligands; Estrogen pathways; Estrogen receptors.

Publication types

  • Review

MeSH terms

  • Breast Neoplasms* / drug therapy
  • Estradiol
  • Estrogen Receptor alpha / metabolism
  • Estrogen Receptor beta / metabolism
  • Estrogens / metabolism
  • Female
  • Humans
  • Ligands
  • Male
  • Receptors, Estrogen* / metabolism

Substances

  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Estrogens
  • Ligands
  • Receptors, Estrogen
  • Estradiol