ArticleActa pharmacologica Sinica2022
Discovery of a novel nonsteroidal selective glucocorticoid receptor modulator by virtual screening and bioassays.
Article in Acta pharmacologica Sinica, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 22 citations in OpenAlex.
- Corticosteroids in ARDS: old controversies, new insights, and future directions.Intensive care medicine · 2026Review
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- M3S-GRPred: a novel ensemble learning approach for the interpretable prediction of glucocorticoid receptor antagonists using a multi-step stacking strategy.BMC bioinformatics · 2025Article
- Association between stroke and fracture and the mediating role of depression: a cross-sectional study from NHANES 2017 to 2020.Frontiers in neurology · 2025Article
- Merging Natural Product Structures with Pharmaceutical Leads: Unnatural Enantiomers of Estranes as Glucocorticoid Receptor Modulators That Suppress TNF-α and IL-6 Release.Journal of medicinal chemistry · 2024Article
- Chemical Evolution and Biological Evaluation of Natural Products for Efficient Therapy of Acute Lung Injury.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2024Article
- Computationally guided discovery of novel non-steroidal AR-GR dual antagonists demonstrating potency against antiandrogen resistance.Acta pharmacologica Sinica · 2023Article
- Immunological evaluation of herbal extracts commonly used for treatment of mental diseases during pregnancy.Scientific reports · 2023Article
- Intein-Mediated Protein Engineering for Cell-Based Biosensors.Biosensors · 2022Review
- Biology of cyclooxygenase-2: An application in depression therapeutics.Frontiers in psychiatry · 2022Review
Corrections and comments
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Authors and funding
15 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Synthetic glucocorticoids (GCs) have been widely used in the treatment of a broad range of inflammatory diseases, but their clinic use is limited by undesired side effects such as metabolic disorders, osteoporosis, skin and muscle atrophies, mood disorders and hypothalamic-pituitary-adrenal (HPA) axis suppression. Selective glucocorticoid receptor modulators (SGRMs) are expected to have promising anti-inflammatory efficacy but with fewer side effects caused by GCs. Here, we reported HT-15, a prospective SGRM discovered by structure-based virtual screening (VS) and bioassays. HT-15 can selectively act on the NF-κB/AP1-mediated transrepression function of glucocorticoid receptor (GR) and repress the expression of pro-inflammation cytokines (i.e., IL-1β, IL-6, COX-2, and CCL-2) as effectively as dexamethasone (Dex). Compared with Dex, HT-15 shows less transactivation potency that is associated with the main adverse effects of synthetic GCs, and no cross activities with other nuclear receptors. Furthermore, HT-15 exhibits very weak inhibition on the ratio of OPG/RANKL. Therefore, it may reduce the side effects induced by normal GCs. The bioactive compound HT-15 can serve as a starting point for the development of novel therapeutics for high dose or long-term anti-inflammatory treatment.
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