TY - JOUR
T1 - Structure of estradiol metal chelate and estrogen receptor complex
T2 - The basis for designing a new class of selective estrogen receptor modulators
AU - Li, Min-Jun
AU - Greenblatt, Harry M.
AU - Dym, Orly
AU - Albeck, Shira
AU - Pais, Adi
AU - Gunanathan, Chidambaram
AU - Milstein, David
AU - Degani, Hadassa
AU - Sussman, Joel
PY - 2011/5/26
Y1 - 2011/5/26
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=79957708369&partnerID=8YFLogxK
U2 - 10.1021/jm200192y
DO - 10.1021/jm200192y
M3 - Article
SN - 0022-2623
VL - 54
SP - 3575
EP - 3580
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 10
ER -