ArticleBritish journal of pharmacology2015
An analysis of glucocorticoid receptor-mediated gene expression in BEAS-2B human airway epithelial cells identifies distinct, ligand-directed, transcription profiles with implications for asthma therapeutics.
Article in British journal of pharmacology, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
17 citing papers in PubMed, 29 citations in OpenAlex.
- Article
- Differential RELA and GR recruitment to the BIRC3/BIRC2 locus: Molecular insight as to combinatorial regulation by proinflammatory cytokines and glucocorticoid.Molecular pharmacology · 2025Article
- Differential regulation of BIRC2 and BIRC3 expression by inflammatory cytokines and glucocorticoids in pulmonary epithelial cells.PloS one · 2023Article
- Comparative efficacy of glucocorticoid receptor agonists on Th2 cell function and attenuation by progesterone.BMC immunology · 2020Article
- GR Dimerization and the Impact of GR Dimerization on GR Protein Stability and Half-Life.Frontiers in immunology · 2019Review
- Long-ActingMolecular pharmacology · 2018Article
- Identification of a tumor-promoter cholesterol metabolite in human breast cancers acting through the glucocorticoid receptor.Proceedings of the National Academy of Sciences of the United States of America · 2017Article
- Glucocorticoid resistance of migration and gene expression in a daughter MDA-MB-231 breast tumour cell line selected for high metastatic potential.Scientific reports · 2017Article
- Scientific rationale for the possible inhaled corticosteroid intraclass difference in the risk of pneumonia in COPD.International journal of chronic obstructive pulmonary disease · 2017Review
- Understanding how long-acting βBritish journal of pharmacology · 2016Review
- Impaired anti-inflammatory action of glucocorticoid in neutrophil from patients with steroid-resistant asthma.Respiratory research · 2016Article
- Budesonide and fluticasone propionate differentially affect the airway epithelial barrier.Respiratory research · 2016Article
- Gene Expression Control by Glucocorticoid Receptors during Innate Immune Responses.Frontiers in endocrinology · 2016Review
- Basal protein phosphatase 2A activity restrains cytokine expression: role for MAPKs and tristetraprolin.Scientific reports · 2015Article
- The long-acting β2 -adrenoceptor agonist, indacaterol, enhances glucocorticoid receptor-mediated transcription in human airway epithelial cells in a gene- and agonist-dependent manner.British journal of pharmacology · 2015Article
- Potential mechanisms to explain how LABAs and PDE4 inhibitors enhance the clinical efficacy of glucocorticoids in inflammatory lung diseases.F1000prime reports · 2015Review
- Genomic determinants implicated in the glucocorticoid-mediated induction of KLF9 in pulmonary epithelial cells.The Journal of biological chemistryArticle
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
Abstract
background and purposeInternational asthma guidelines recommend that inhaled glucocorticoids be used as a monotherapy in all patients with mild to moderate disease because of their ability to suppress airways inflammation. Current evidence suggests that the therapeutic benefit of glucocorticoids is due to the transactivation and transrepression of anti-inflammatory and pro-inflammatory genes respectively. However, the extent to which clinically relevant glucocorticoids are equivalent in their ability to modulate gene expression is unclear. EXPERIMENTAL APPROACH: A pharmacodynamics investigation of glucocorticoid receptor (GR)-mediated gene transactivation in BEAS-2B human airway epithelial cells was performed using a glucocorticoid response element luciferase reporter coupled with an analysis of glucocorticoid-inducible genes encoding proteins with anti-inflammatory and adverse-effect potential. KEY
resultsUsing transactivation as a functionally relevant output, a given glucocorticoid displayed a unique, gene expression 'fingerprint' where intrinsic efficacy and GR density were essential determinants. We showed that depending on the gene selected for analysis, a given glucocorticoid can behave as an antagonist, partial agonist, full agonist or even 'super agonist'. In the likely event that different, tissue-dependent gene expression profiles are reproduced in vivo, then the anti-inflammatory and adverse-effect potential of many glucocorticoids currently available as asthma therapeutics may not be equivalent. CONCLUSIONS AND IMPLICATIONS: The generation of gene expression 'fingerprints' in target and off-target human tissues could assist the rational design of GR agonists with improved therapeutic ratios. This approach could identify compounds that are useful in the management of severe asthma and other inflammatory disorders where systemic exposure is desirable.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.