2iok
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Human estrogen receptor alpha ligand-binding domain in complex with compound 1D
OverviewOverview
A novel class of indole ligands for estrogen receptor alpha have been, discovered which exhibit potent affinity and high selectivity., Substitution of the bazedoxifene skeleton to the linker present in the HTS, lead 1a provided 22b which was found to be 130-fold alpha-selective and, acted as an antagonist of estradiol activity in uterine tissue and MCF-7, cancer cells.
About this StructureAbout this Structure
2IOK is a Single protein structure of sequence from Homo sapiens with as ligand. Full crystallographic information is available from OCA.
ReferenceReference
Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha., Dykstra KD, Guo L, Birzin ET, Chan W, Yang YT, Hayes EC, DaSilva CA, Pai LY, Mosley RT, Kraker B, Fitzgerald PM, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML, Bioorg Med Chem Lett. 2007 Apr 15;17(8):2322-8. Epub 2007 Jan 25. PMID:17289385
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