Activity of a tamoxifen-raloxifene hybrid ligand for estrogen receptors at an AP-1 site

Ross V. Weatherman, David C. Carroll, Thomas (Tom) Scanlan

Research output: Contribution to journalArticle

16 Citations (Scopus)

Abstract

To test the effect of ligand flexibility on the selective transcriptional activities of ERα and ERβ from an AP-1 site, an analogue of raloxifene was made that removed the ketone functionality and made the ligand more planar and conformationally more similar to 4-hydroxytamoxifen. Desketoraloxifene was found to be a much stronger activator at an AP-1 site with ERα than with ERβ, mimicking 4-hydroxytamoxifen more than raloxifene.

Original languageEnglish (US)
Pages (from-to)3129-3131
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number24
DOIs
StatePublished - Dec 17 2001
Externally publishedYes

Fingerprint

Transcription Factor AP-1
Tamoxifen
Estrogen Receptors
Ligands
Ketones
Raloxifene Hydrochloride
afimoxifene

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Activity of a tamoxifen-raloxifene hybrid ligand for estrogen receptors at an AP-1 site. / Weatherman, Ross V.; Carroll, David C.; Scanlan, Thomas (Tom).

In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 24, 17.12.2001, p. 3129-3131.

Research output: Contribution to journalArticle

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