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Updated: Mar 25, 2026

Biochemical Reconstitution of Steroid Receptor•Hsp90 Protein Complexes and Reactivation of Ligand Binding
Published on: September 21, 2011
Biased signalling from the glucocorticoid receptor: Renewed opportunity for tailoring glucocorticoid activity
Christine R Keenan1, Michael J Lew1, Alastair G Stewart1
1Department of Pharmacology and Therapeutics, The University of Melbourne, Parkville, Victoria 3010, Australia.
Abstract:
Recent landmark studies applying analytical pharmacology approaches to the glucocorticoid receptor (GR) have demonstrated that different ligands can cause differential activation of distinct GR-regulated genes. Drawing on concepts of signalling bias from the field of G protein-coupled receptor (GPCR) biology, we speculate that ligand-dependent differences in GR signalling can be considered analogous to GPCR biased signalling, and thus can be quantitatively analysed in a similar way. This type of approach opens up the possibility of using rational structure-based drug optimisation strategies to improve the therapeutic selectivity of glucocorticoid drugs to maximise their efficacy and minimise adverse effects.
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