Journal
BEST PRACTICE & RESEARCH CLINICAL ENDOCRINOLOGY & METABOLISM
Volume 20, Issue 1, Pages 1-14Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.beem.2005.09.002
Keywords
receptor agonist; antagonist; protein structure; selective oestrogen receptor modulator; SERM; activation function 2; ligand-binding domain
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Funding
- Wellcome Trust [064803] Funding Source: Medline
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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 ER alpha. and ER beta 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.
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