Lessons learnt from structural studies of the oestrogen receptor

Over the last 10 years, structural studies of the ligand-binding domains of nuclear hormone receptors have provided a wealth of information on the nature of ligand-binding and its role in receptor activation. This review examines the insights that studies on oestrogen receptor subtypes ERα and ERβ have provided in terms of (1) basis of receptor activation; (2) recruitment of coregulators; (3) hormone recognition; and (4) subtype-selective ligands. It also highlights the implications for the binding of endocrine disruptors.

Key words: receptor agonist, antagonist, protein structure, selective oestrogen receptor modulator, SERM, activation function 2, ligand-binding domain