Structure-function relationships in estrogen receptors and the characterization of novel selective estrogen receptor modulators with unique pharmacological profiles

Benita S. Katzenellenbogen, Jun Sun, William R. Harrington, Dennis M. Kraichely, Deshanie Ganessunker, John A. Katzenellenbogen

Research output: Contribution to journalArticle

Abstract

This article summarizes recent research on the development of estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ) subtype-selective ligands based on our understanding of structure-activity relationships in these two estrogen receptors and differences in their ligand binding domains and activation function domains. The use of these ligands should enable greater understanding of the unique biologies mediated by ERα versus ERβ and may, as well, provide selective estrogen receptor modulators having unique biological and pharmacological profiles optimal for prevention and treatment of breast cancer, for menopausal hormone replacement, for prevention of osteoporosis, and for potential cardiovascular benefit.

Original languageEnglish (US)
Pages (from-to)6-15
Number of pages10
JournalAnnals of the New York Academy of Sciences
Volume949
StatePublished - Jan 1 2001

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Keywords

  • Coactivators
  • ERα
  • ERβ
  • SERMs

ASJC Scopus subject areas

  • Neuroscience(all)
  • Biochemistry, Genetics and Molecular Biology(all)
  • History and Philosophy of Science

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