Structural insights into the mechanisms of agonism and antagonism in oestrogen receptor isoforms

Here we summarise the results that have emerged from our structural studies on the oestrogen receptor (ER) ligand-binding domain. We have investigated the conformational effects of a variety of ligands on the structures of bo th ER isoforms. Each class of ligand (agonists, partial agonists and select ive oestrogen receptor modulators) induces a unique conformation in the rec eptor's ligand-dependent transcriptional activation function. Together thes e studies have broadened our understanding of ER function by providing a un ique insight into ER's ligand specificity and the structural changes that u nderlie receptor agonism and antagonism. (C) 2000 Elsevier Science Ltd. All rights reserved.