Department of Structural Biology, Weizmann Institute of Science, Rehovot 76100, Israel.
J Med Chem. 2011 May 26;54(10):3575-80. doi: 10.1021/jm200192y. Epub 2011 Apr 19.
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.
选择性雌激素受体调节剂，如与金属配合物结合的 17β-雌二醇衍生物，已被合成为用于诊断和治疗乳腺癌的靶向探针。在这里，我们报告了与新型雌二醇衍生的金属配合物，即雌二醇-吡啶四乙酸铕（III）结合的雌激素受体 α 配体结合域（ERα-LBD）的详细 3D 结构，分辨率为 2.6Å。该结构提供了与设计用于临床应用的新型功能性 ERα 靶向探针相关的重要信息。
