Effect of steroid hormones on the template activity of DNA and glucocorticoid-receptor interaction

1982 ◽  
Vol 12 (5) ◽  
pp. 385-388
Author(s):  
P. P. Golikov ◽  
A. S. Bobkova
Keyword(s):  
Glucocorticoid Receptor ◽  
Steroid Hormones ◽  
Receptor Interaction ◽  
Template Activity

scholarly journals Glucocorticoid resistance conferring mutation in the C-terminus of GR alters the receptor conformational dynamics

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Anna Kaziales ◽  
Florian Rührnößl ◽  
Klaus Richter
Keyword(s):  
Glucocorticoid Receptor ◽  
Steroid Hormones ◽  
In Silico ◽  
Conformational Dynamics ◽  
Glucocorticoid Resistance ◽  
Physiological Processes ◽  
C Terminus ◽  
Hsp90 Chaperone ◽  
In Silico Methods

AbstractThe glucocorticoid receptor is a key regulator of essential physiological processes, which under the control of the Hsp90 chaperone machinery, binds to steroid hormones and steroid-like molecules and in a rather complicated and elusive response, regulates a set of glucocorticoid responsive genes. We here examine a human glucocorticoid receptor variant, harboring a point mutation in the last C-terminal residues, L773P, that was associated to Primary Generalized Glucocorticoid Resistance, a condition originating from decreased affinity to hormone, impairing one or multiple aspects of GR action. Using in vitro and in silico methods, we assign the conformational consequences of this mutation to particular GR elements and report on the altered receptor properties regarding its binding to dexamethasone, a NCOA-2 coactivator-derived peptide, DNA, and importantly, its interaction with the chaperone machinery of Hsp90.

scholarly journals Acquired Glucocorticoid Resistance Due to Homologous Glucocorticoid Receptor Downregulation: A Modern Look at an Age-Old Problem

Cells ◽  
2021 ◽  
Vol 10 (10) ◽  
pp. 2529
Author(s):  
Lee-Maine L. Spies ◽  
Nicolette J. D. Verhoog ◽  
Ann Louw
Keyword(s):  
Transcription Factor ◽  
Side Effects ◽  
Pharmaceutical Industry ◽  
Glucocorticoid Receptor ◽  
Steroid Hormones ◽  
Molecular Mechanisms ◽  
Protein Levels ◽  
Current Review ◽  
Role Players ◽  
Receptor Conformation

For over 70 years, the unique anti-inflammatory properties of glucocorticoids (GCs), which mediate their effects via the ligand-activated transcription factor, the glucocorticoid receptor alpha (GRα), have allowed for the use of these steroid hormones in the treatment of various autoimmune and inflammatory-linked diseases. However, aside from the onset of severe side-effects, chronic GC therapy often leads to the ligand-mediated downregulation of the GRα which, in turn, leads to a decrease in GC sensitivity, and effectively, the development of acquired GC resistance. Although the ligand-mediated downregulation of GRα is well documented, the precise factors which influence this process are not well understood and, thus, the development of an acquired GC resistance presents an ever-increasing challenge to the pharmaceutical industry. Recently, however, studies have correlated the dimerization status of the GRα with its ligand-mediated downregulation. Therefore, the current review will be discussing the major role-players in the homologous downregulation of the GRα pool, with a specific focus on previously reported GC-mediated reductions in GRα mRNA and protein levels, the molecular mechanisms through which the GRα functional pool is maintained and the possible impact of receptor conformation on GC-mediated GRα downregulation.

scholarly journals Steroid hormones differentially regulate expression of complement receptors immunoglobulin in human macrophages, involving the glucocorticoid receptor

2019 ◽  
Vol 2 (1) ◽  
Author(s):  
Nateelak Kooltheat ◽  
Pachuen Potup ◽  
Yordhathai Thongsri ◽  
Antonio Ferrante ◽  
Kanchana Usuwanthim
Keyword(s):  
Glucocorticoid Receptor ◽  
Steroid Hormones ◽  
Complement Receptors ◽  
Human Macrophages

scholarly journals A metal-linked gapped zipper model is proposed for theh sp90-glucocorticoid receptor interaction

FEBS Letters ◽  
1993 ◽  
Vol 315 (2) ◽  
pp. 109-113 ◽  
Author(s):  
J.A. Schwartz ◽  
H. Mizukami ◽  
D.F. Skafar
Keyword(s):  
Glucocorticoid Receptor ◽  
Receptor Interaction

The glucocorticoid receptor binds to a sequence overlapping the TATA box of the human osteocalcin promoter: a potential mechanism for negative regulation

1991 ◽  
Vol 11 (6) ◽  
pp. 3379-3383
Author(s):  
P E Strömstedt ◽  
L Poellinger ◽  
J A Gustafsson ◽  
J Carlstedt-Duke
Keyword(s):  
Glucocorticoid Receptor ◽  
Specific Binding ◽  
Tata Box ◽  
Receptor Interaction ◽  
Receptor Binding Site ◽  
Osteocalcin Gene ◽  
Close Proximity ◽  
Human Osteocalcin

Expression of the human osteocalcin promoter is negatively regulated by glucocorticoids in vivo. In vitro DNase I and exonuclease III footprinting analysis showed binding of purified glucocorticoid receptor in close proximity to and overlapping with the TATA box of the osteocalcin gene. These results imply competition or interference with binding of the TATA box-binding transcription factor IID as a mechanism of repression of this gene by glucocorticoids. In support of this notion, point mutation analysis of the receptor binding site indicated that flanking nucleotides and not the TATA box motif per se were important for receptor interaction. Moreover, DNA binding competition assays showed specific binding of the receptor only to the TATA box region of the osteocalcin gene and not to the corresponding region of an immunoglobulin heavy-chain promoter.

scholarly journals A Model of Glucocorticoid Receptor Interaction With Coregulators Predicts Transcriptional Regulation of Target Genes

2019 ◽  
Vol 10 ◽  
Author(s):  
Federico Monczor ◽  
Antonia Chatzopoulou ◽  
Carlos Daniel Zappia ◽  
René Houtman ◽  
Onno C. Meijer ◽  
...  
Keyword(s):  
Transcriptional Regulation ◽  
Glucocorticoid Receptor ◽  
Target Genes ◽  
Receptor Interaction

scholarly journals Glucocorticoid Receptor Interaction with 14-3-3 and Raf-1, a Proposed Mechanism for Cross-talk of Two Signal Transduction Pathways

2000 ◽  
Vol 275 (50) ◽  
pp. 39296-39301 ◽  
Author(s):  
Christina Widén ◽  
Johanna Zilliacus ◽  
Jan-Åke Gustafsson ◽  
Ann-Charlotte Wikström
Keyword(s):  
Signal Transduction ◽  
Glucocorticoid Receptor ◽  
Cross Talk ◽  
Receptor Interaction ◽  
Signal Transduction Pathways

scholarly journals Glucocorticoid receptor in the rat epididymis: Expression, cellular distribution and regulation by steroid hormones

2010 ◽  
Vol 325 (1-2) ◽  
pp. 64-77 ◽  
Author(s):  
Erick J.R. Silva ◽  
Daniel B.C. Queiróz ◽  
Luciana Honda ◽  
Maria Christina W. Avellar
Keyword(s):  
Glucocorticoid Receptor ◽  
Steroid Hormones ◽  
Cellular Distribution ◽  
Rat Epididymis
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