期刊
BIOCHEMICAL PHARMACOLOGY
卷 112, 期 -, 页码 6-12出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bcp.2016.02.008
关键词
Corticosteroids; Pharmacodynamics; G protein-coupled receptors; Steroid resistance; Systems biology; Inflammation
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. (C) 2016 Elsevier Inc. All rights reserved.
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