Estrogen and progesterone receptors: from molecular structures to clinical targets

Cell Mol Life Sci. 2009 Aug;66(15):2405-26. doi: 10.1007/s00018-009-0017-3. Epub 2009 Mar 31.


Research involving estrogen and progesterone receptors (ER and PR) have greatly contributed to our understanding of cell signaling and transcriptional regulation. In addition to the classical ER and PR nuclear actions, new signaling pathways have recently been identified due to ER and PR association with cell membranes and signal transduction proteins. Bio-informatics has unveiled how ER and PR recognize their ligands, selective modulators and co-factors, which has helped to implement them as key targets in the treatment of benign and malignant tumors. Knowledge regarding ER and PR is vast and complex; therefore, this review will focus on their isoforms, signaling pathways, co-activators and co-repressors, which lead to target gene regulation. Moreover it will highlight ER and PR involvement in benign and malignant diseases as well as pharmacological substances influencing cell signaling and provide established and new structural insights into the mechanism of activation and inhibition of these receptors.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Computational Biology
  • Estradiol / chemistry
  • Estradiol / metabolism
  • Humans
  • Ligands
  • Models, Molecular
  • Molecular Sequence Data
  • Phylogeny
  • Progesterone / chemistry
  • Progesterone / metabolism
  • Protein Isoforms / chemistry
  • Protein Isoforms / genetics
  • Protein Isoforms / metabolism
  • Protein Structure, Tertiary
  • Receptors, Estrogen / chemistry
  • Receptors, Estrogen / classification
  • Receptors, Estrogen / genetics
  • Receptors, Estrogen / metabolism*
  • Receptors, Progesterone / chemistry
  • Receptors, Progesterone / classification
  • Receptors, Progesterone / genetics
  • Receptors, Progesterone / metabolism*
  • Receptors, Steroid / agonists
  • Receptors, Steroid / antagonists & inhibitors
  • Selective Estrogen Receptor Modulators / chemistry
  • Selective Estrogen Receptor Modulators / metabolism
  • Sequence Alignment
  • Signal Transduction / physiology*


  • Ligands
  • Protein Isoforms
  • Receptors, Estrogen
  • Receptors, Progesterone
  • Receptors, Steroid
  • Selective Estrogen Receptor Modulators
  • Progesterone
  • Estradiol