The Biologist’s Guide to the Glucocorticoid Receptor’s Structure

Author:

Deploey Nick123,Van Moortel Laura123,Rogatsky Inez45,Peelman Frank12,De Bosscher Karolien123ORCID

Affiliation:

1. VIB Center for Medical Biotechnology, VIB, 9052 Ghent, Belgium

2. Department of Biomolecular Medicine, Ghent University, 9000 Ghent, Belgium

3. Translational Nuclear Receptor Research (TNRR) Laboratory, VIB, 9052 Ghent, Belgium

4. Hospital for Special Surgery Research Institute, The David Z. Rosensweig Genomics Center, New York, NY 10021, USA

5. Graduate Program in Immunology and Microbial Pathogenesis, Weill Cornell Graduate School of Medical Sciences, New York, NY 10065, USA

Abstract

The glucocorticoid receptor α (GRα) is a member of the nuclear receptor superfamily and functions as a glucocorticoid (GC)-responsive transcription factor. GR can halt inflammation and kill off cancer cells, thus explaining the widespread use of glucocorticoids in the clinic. However, side effects and therapy resistance limit GR’s therapeutic potential, emphasizing the importance of resolving all of GR’s context-specific action mechanisms. Fortunately, the understanding of GR structure, conformation, and stoichiometry in the different GR-controlled biological pathways is now gradually increasing. This information will be crucial to close knowledge gaps on GR function. In this review, we focus on the various domains and mechanisms of action of GR, all from a structural perspective.

Funder

Research Foundation Flanders

VIB and Ghent University institutional funding

NIH

The Hospital for Special Surgery David Z. Rosensweig Genomics Center

Publisher

MDPI AG

Subject

General Medicine

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