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

20 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

Fingerprint

Selective Estrogen Receptor Modulators
Estrogen Receptors
Estradiol
Metals
Coordination Complexes
Europium
Acetates
Breast Neoplasms
Ligands

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Structure of estradiol metal chelate and estrogen receptor complex : The basis for designing a new class of selective estrogen receptor modulators. / Li, Min Jun; Greenblatt, Harry M.; Dym, Orly; Albeck, Shira; Pais, Adi; Gunanathan, Chidambaram; Milstein, David; Degani, Hadassa; Sussman, Joel L.

In: Journal of Medicinal Chemistry, Vol. 54, No. 10, 26.05.2011, p. 3575-3580.

Research output: Contribution to journalArticle

Li, Min Jun ; Greenblatt, Harry M. ; Dym, Orly ; Albeck, Shira ; Pais, Adi ; Gunanathan, Chidambaram ; Milstein, David ; Degani, Hadassa ; Sussman, Joel L. / Structure of estradiol metal chelate and estrogen receptor complex : The basis for designing a new class of selective estrogen receptor modulators. In: Journal of Medicinal Chemistry. 2011 ; Vol. 54, No. 10. pp. 3575-3580.
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