ArticleProceedings of the National Academy of Sciences of the United States of America2007
Antiinflammatory glucocorticoid receptor ligand with reduced side effects exhibits an altered protein-protein interaction profile.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers, 1 of them a synthesis that pooled it.
What it found
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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.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
22 citing papers in PubMed, 1 synthesis or guideline pooled it, 67 citations in OpenAlex.
- Efficacy and safety of selective glucocorticoid receptor modulators in comparison to glucocorticoids in arthritis, a systematic review.PloS one · 2017Pooled it
- Selective Modulation of the Human Glucocorticoid Receptor Compromises GR Chromatin Occupancy and Recruitment of p300/CBP and the Mediator Complex.Molecular & cellular proteomics : MCP · 2024Article
- Improved Glucocorticoid Receptor Ligands: Fantastic Beasts, but How to Find Them?Frontiers in endocrinology · 2020Review
- A General Introduction to Glucocorticoid Biology.Frontiers in immunology · 2019Review
- A screening assay for Selective Dimerizing Glucocorticoid Receptor Agonists and Modulators (SEDIGRAM) that are effective against acute inflammation.Scientific reports · 2018Article
- Molecular mechanisms of glucocorticoids on skeleton and bone regeneration after fracture.Journal of molecular endocrinology · 2018Review
- An Approach to Greater Specificity for Glucocorticoids.Frontiers in endocrinology · 2018Review
- Understanding how long-acting βBritish journal of pharmacology · 2016Review
- Glucocorticoid-independent modulation of GR activity: Implications for immunotherapy.Pharmacology & therapeutics · 2016Review
- Ginsenoside Rh1 potentiates dexamethasone's anti-inflammatory effects for chronic inflammatory disease by reversing dexamethasone-induced resistance.Arthritis research & therapy · 2014Article
- Article
- The possible separation of 12-O-tetradecanoylphorbol-13-acetate-induced skin inflammation and hyperplasia by compound A.Molecular carcinogenesis · 2013Article
- Nuclear receptors and their selective pharmacologic modulators.Pharmacological reviews · 2013Review
- The multiple facets of glucocorticoid action in rheumatoid arthritis.Nature reviews. Rheumatology · 2012Review
- Anti-inflammatory effects of selective glucocorticoid receptor modulators are partially dependent on up-regulation of dual specificity phosphatase 1.British journal of pharmacology · 2012Article
- Assessing the metabolic effects of prednisolone in healthy volunteers using urine metabolic profiling.Genome medicine · 2012Article
- Article
- Crosstalk in inflammation: the interplay of glucocorticoid receptor-based mechanisms and kinases and phosphatases.Endocrine reviews · 2009Review
- Design and x-ray crystal structures of high-potency nonsteroidal glucocorticoid agonists exploiting a novel binding site on the receptor.Proceedings of the National Academy of Sciences of the United States of America · 2009Article
- Inhaled corticosteroids as combination therapy with beta-adrenergic agonists in airways disease: present and future.European journal of clinical pharmacology · 2009Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Glucocorticoids are commonly used antiinflammatory agents whose use is limited by side effects. We have developed a series of glucocorticoid receptor (GR) ligands that retain the strong antiinflammatory activity of conventional glucocorticoids with reduced side effects. We present a compound, LGD5552, that binds the receptor efficiently and strongly represses inflammatory gene expression. LGD5552 bound to GR activates gene expression somewhat differently than glucocorticoids. It activates some genes with an efficacy similar to that of the glucocorticoids. However, other glucocorticoid-activated genes are not regulated by LGD5552. These differences may be because of the more efficient binding of corepressor in the presence of LGD5552, compared with glucocorticoid agonists. This class of nonsteroidal, GR-dependent antiinflammatory drugs may offer a safer alternative to steroidal glucocorticoids in the treatment of inflammatory disease.
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Registered trials
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.