2iog

From Proteopedia

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Revision as of 20:40, 12 November 2007

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spinqualitylabelsall models 2iog, resolution 1.60Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image

Human estrogen receptor alpha ligand-binding domain in complex with compound 11F

Contents 1 Overview 2 Disease 3 About this Structure 4 Reference

Overview

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.

Disease

Known diseases associated with this structure: Atherosclerosis, susceptibility to OMIM:[133430], Breast cancer OMIM:[133430], Estrogen resistance OMIM:[133430], HDL response to hormone replacement, augmented OMIM:[133430], Migraine, susceptibility to OMIM:[133430], Myocardial infarction, susceptibility to OMIM:[133430]

About this Structure

2IOG is a Single protein structure of sequence from Homo sapiens with IOG as ligand. Full crystallographic information is available from OCA.

Reference

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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