Structure of estradiol metal chelate and estrogen receptor complex: The basis for designing a new class of selective estrogen receptor modulators

Min Jun Li, Harry M. Greenblatt, Orly Dym, Shira Albeck, Adi Pais, Chidambaram Gunanathan, David Milstein, Hadassa Degani, Joel L. Sussman

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

Selective estrogen receptor modulators, such as 17β-estradiol derivatives bound to metal complexes, have been synthesized as targeted probes for the diagnosis and treatment of breast cancer. Here, we report the detailed 3D structure of estrogen receptor α ligand-binding domain (ERα-LBD) bound with a novel estradiol-derived metal complex, estradiol-pyridine tetra acetate europium(III), at 2.6 Å resolution. This structure provides important information pertinent to the design of novel functional ERα targeted probes for clinical applications.

Original languageEnglish
Pages (from-to)3575-3580
Number of pages6
JournalJournal of Medicinal Chemistry
Volume54
Issue number10
DOIs
Publication statusPublished - May 26 2011

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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