Molecular structural characteristics of estrogen receptor modulators as determinants of estrogen receptor selectivity

Mini Rev Med Chem. 2008 Aug;8(9):943-51. doi: 10.2174/138955708785132747.

Abstract

This review will discuss the structural determinants and requirements necessary for estrogen receptors alpha and beta selectivity and ligand-receptor binding affinity. In addition, strategies likely to result in the development of a pharmacophore model that account for the differences in estrogenic effects between different ligands will be discussed.

Publication types

  • Review

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical / methods*
  • Drug Design*
  • Estrogen Receptor Modulators / pharmacology*
  • Estrogen Receptor alpha / metabolism*
  • Estrogens / chemistry
  • Humans
  • Ligands
  • Models, Molecular
  • Protein Conformation
  • Pyridines / chemistry
  • Receptors, Estrogen / metabolism*
  • Software
  • Structure-Activity Relationship
  • Technology, Pharmaceutical / methods*

Substances

  • ESR1 protein, human
  • Estrogen Receptor Modulators
  • Estrogen Receptor alpha
  • Estrogens
  • Ligands
  • Pyridines
  • Receptors, Estrogen