Biased regulation of glucocorticoid receptors signaling.

Lijuan Mao, Wei Wei, Jingyu Chen

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie 2023 Sep

filter terms:

Glucocorticoids (GCs), steroid hormones that depend on glucocorticoid receptor (GR) binding for their action, are essential for regulating numerous homeostatic functions in the body.GR signals are biased, that is, GR signals are various in different tissue cells, disease states and ligands. This biased regulation of GR signaling appears to depend on ligand-induced metameric regulation, protein post-translational modifications, assembly at response elements, context-specific assembly (recruitment of co-regulators) and intercellular differences. Based on the bias regulation of GR, selective GR agonists and modulators (SEGRAMs) were developed to bias therapeutic outcomes toward expected outcomes (e.g., anti-inflammation and immunoregulation) by influencing GR-mediated gene expression. This paper provides a review of the bias regulation and mechanism of GR and the research progress of drugs. Copyright © 2023 The Authors. Published by Elsevier Masson SAS.. All rights reserved.

Citation

Lijuan Mao, Wei Wei, Jingyu Chen. Biased regulation of glucocorticoid receptors signaling. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2023 Sep;165:115145