AI Article Synopsis
- Recent studies show that various ligands can activate different genes regulated by the glucocorticoid receptor (GR) in distinct ways.
- This suggests that GR signaling differences, similar to biased signaling seen in G protein-coupled receptors (GPCRs), can be analyzed quantitatively.
- Using these insights could allow for better drug design strategies that enhance the effectiveness of glucocorticoid drugs while reducing side effects.
Article 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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| http://dx.doi.org/10.1016/j.bcp.2016.02.008 | DOI Listing |
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