Biased regulation of glucocorticoid receptors signaling

被引：16

作者：

Mao, Lijuan ^{[1
]}

Wei, Wei ^{[1
]}

Chen, Jingyu ^{[1
]}

机构：

[1] Anhui Med Univ, Ctr Rheumatoid Arthrit, Anhui Cooperat Innovat Ctr Antiinflammatory Immune, Inst Clin Pharmacol,Educ Minist,Key Lab Antiinflam, Hefei 230032, Peoples R China

来源：

BIOMEDICINE & PHARMACOTHERAPY | 2023年 / 165卷

基金：

中国国家自然科学基金;

关键词：

Glucocorticoid receptor; Biased regulation; Selective glucocorticoid receptor modulators; Selective glucocorticoid receptor agonists; LIGAND-BINDING DOMAIN; TRANSCRIPTIONAL COACTIVATORS; TRANSLATIONAL ISOFORMS; GENE-EXPRESSION; PHOSPHORYLATION; MECHANISMS; HORMONE; SUMOYLATION; PLASTICITY; BETA;

D O I：

10.1016/j.biopha.2023.115145

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

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.

引用

页数：12

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