Estrogen receptor signalling: Bases for drug actions

Maria Marino, Filippo Acconcia, Paolo Ascenzi

Research output: Contribution to journalArticlepeer-review


Estrogen receptors (ERα and ERβ) mediate the effects of 17β-estradiol (E2) and account for E2 role on growth, development, and homeostasis maintenance in different tissues and organs. ERα and ERβ function as ligand-dependent transcription factors which directly bind to specific estrogen responsive element (ERE) present into DNA and, in turn, regulate the transcription of E2-sensitive genes. In addition, ERα and ERβ, without direct binding to DNA, regulate transcription indirectly by binding to other transcription factors activating or inactivating the transcription of E2-dependent-ERE-devoid genes. Along with these two E2 mechanisms, it has been recently uncovered that a third signalling pathway, involving cytoplasmic proteins and rapid membrane-initiated responses, serves largely for mitogenic E2-induced effects. The commitment of ERβ in these rapid E2-induced effects is openly debated. This review will focus and summarize the latest findings regarding the multiple E2 molecular mechanisms and underlines the development of our understanding of anti-cancer drugs acting as ER signalling modulators.

Original languageEnglish
Pages (from-to)305-314
Number of pages10
JournalCurrent Drug Targets: Immune, Endocrine and Metabolic Disorders
Issue number3
Publication statusPublished - Sep 2005


  • 17β-estradiol
  • Estrogen receptors
  • Estrogen-related cancer
  • Selective estrogen receptor modulators
  • Signalling pathways

ASJC Scopus subject areas

  • Endocrinology, Diabetes and Metabolism
  • Immunology and Allergy


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