Biased regulation of glucocorticoid receptors signaling.

Receptors, Glucocorticoid / metabolism Glucocorticoids / pharmacology Anti-Inflammatory Agents / pharmacology Signal Transduction Protein Binding
AL438 (PubChem CID: 9906282) AZD9567 (PubChem CID: 121248172) BI653048 (PubChem CID: 44543970) Biased regulation C108297 (PubChem CID: 25110774) CpdA (PubChem CID: 9838148) Fosdagrocorat (PubChem CID: 24872952) GSK866 (PubChem CID: 25058139) GW870086 (PubChem CID: 11376392) Glucocorticoid receptor LEO 134310 (PubChem CID: 126714060) ORG 214007–0 (PubChem CID: 154659439) RU24782 (PubChem CID: 385448896) RU24858 (PubChem CID: 223258861) Selective glucocorticoid receptor agonists Selective glucocorticoid receptor modulators ZK216348 (PubChem CID: 9805004) ZK245186 (PubChem CID: 24795088)

Journal

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie
ISSN: 1950-6007
Titre abrégé: Biomed Pharmacother
Pays: France
ID NLM: 8213295

Informations de publication

Date de publication:
Sep 2023
Historique:
received: 11 05 2023
revised: 03 07 2023
accepted: 07 07 2023
medline: 17 8 2023
pubmed: 17 7 2023
entrez: 16 7 2023
Statut: ppublish

Résumé

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.

Identifiants

DOI: 10.1016/j.biopha.2023.115145 PMID: 37454592
pubmed: 37454592
pii: S0753-3322(23)00936-8
doi: 10.1016/j.biopha.2023.115145
pii:
doi:

Substances chimiques

Receptors, Glucocorticoid 0
Glucocorticoids 0
Anti-Inflammatory Agents 0

Types de publication

Journal Article Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

115145

Informations de copyright

Copyright © 2023 The Authors. Published by Elsevier Masson SAS.. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest I declare that this article does not involve any conflict of interest.

Auteurs

Lijuan Mao (L)

Institute of Clinical Pharmacology, Anhui Medical University, Key Laboratory of Anti-inflammatory and Immune Medicine of Education Ministry, Anhui Cooperative Innovation Center for Anti-inflammatory Immune Drugs, Center of Rheumatoid Arthritis of Anhui Medical University, Hefei 230032, China.

Wei Wei (W)

Institute of Clinical Pharmacology, Anhui Medical University, Key Laboratory of Anti-inflammatory and Immune Medicine of Education Ministry, Anhui Cooperative Innovation Center for Anti-inflammatory Immune Drugs, Center of Rheumatoid Arthritis of Anhui Medical University, Hefei 230032, China. Electronic address: wwei@ahmu.edu.cn.

Jingyu Chen (J)

Institute of Clinical Pharmacology, Anhui Medical University, Key Laboratory of Anti-inflammatory and Immune Medicine of Education Ministry, Anhui Cooperative Innovation Center for Anti-inflammatory Immune Drugs, Center of Rheumatoid Arthritis of Anhui Medical University, Hefei 230032, China. Electronic address: cjyanyi@126.com.

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Classifications MeSH

questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Récepteurs cytoplasmiques et nucléaires › Récepteurs aux glucocorticoïdes › Biased regulation of glucocorticoid receptors...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Effets physiologiques des médicaments › Hormones, substituts d'hormones et antagonistes d'hormones › Hormones › Glucocorticoïdes › Biased regulation of glucocorticoid receptors...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-inflammatoires › Biased regulation of glucocorticoid receptors...
questionsmedicales.fr › Phénomènes physiologiques cellulaires › Transduction du signal › Biased regulation of glucocorticoid receptors...
questionsmedicales.fr › Métabolisme › Liaison aux protéines › Biased regulation of glucocorticoid receptors...