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ARTICLE Structure of Estradiol Metal Chelate and Estrogen Receptor Complex: The Basis for Designing a New Class of Selective Estrogen Receptor Modulators

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


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 R ligand-binding domain (ERR-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 ERR targeted probes for clinical applications. Estrogens and their main targets, estrogen receptors (ERR and ERβ), play key roles not only in the maintenance of normal sexual and reproductive function but also in the progression of numerous diseases. 1,2 In ER-positive breast cancers, estrogenrecepto

Year: 2014
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