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  • Title: Crystallization of the human glucocorticoid receptor ligand binding domain: a step towards selective glucocorticoids.
    Author: Necela BM, Cidlowski JA.
    Journal: Trends Pharmacol Sci; 2003 Feb; 24(2):58-61. PubMed ID: 12559765.
    Abstract:
    The crystal structure of the glucocorticoid receptor (GR) ligand binding domain in a ternary complex with dexamethasone and a TIF2 coactivator peptide has been determined recently. The structure reveals several distinct features not found in other nuclear receptors, such as a novel dimerization interface and a second charge clamp that might be important in determining coactivator binding selectivity. The GR ligand binding domain also has a steroid binding pocket that is distinct from other nuclear receptors and might explain its selectivity for glucocorticoids and its diversity of responses.
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