ArticleThe Journal of biological chemistry2012
Anti-inflammatory effects of mapracorat, a novel selective glucocorticoid receptor agonist, is partially mediated by MAP kinase phosphatase-1 (MKP-1).
Article in The Journal of biological chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 45 citations in OpenAlex.
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- VDAC1 Intervention Alleviates Bisphenol AF-Induced Succinate Metabolism Dysregulation and Inflammatory Responses.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Targeting ALOX5 ameliorates renal tubular injury in ischemia-reperfusion-induced acute kidney injury via inhibition of ferroptosis.Communications biology · 2025Article
- Metallaphotocatalytic triple couplings for modular synthesis of elaborate N-trifluoroalkyl anilines.Nature communications · 2024Article
- Housing conditions affect enterocyte death mode and turnover rate in mouse small intestine.Scientific reports · 2023Article
- Recent Approaches to Targeting Canonical NFJournal of the American Society of Nephrology : JASN · 2021Review
- Pleiotropic Effects of Glucocorticoids on the Immune System in Circadian Rhythm and Stress.Frontiers in immunology · 2021Review
- A Novel Approach to Safer Glucocorticoid Receptor-Targeted Anti-lymphoma Therapy via REDD1 (Regulated in Development and DNA Damage 1) Inhibition.Molecular cancer therapeutics · 2020Article
- Antiviral immune mechanism of Toll-like receptor 4-mediated human alveolar epithelial cells type Ⅱ.Experimental and therapeutic medicine · 2020Article
- MAP kinase phosphatase-1, a gatekeeper of the acute innate immune response.Life sciences · 2020Review
- Improved Glucocorticoid Receptor Ligands: Fantastic Beasts, but How to Find Them?Frontiers in endocrinology · 2020Review
- A screening assay for Selective Dimerizing Glucocorticoid Receptor Agonists and Modulators (SEDIGRAM) that are effective against acute inflammation.Scientific reports · 2018Article
- HMGB1-TLR4 signaling participates in renal ischemia reperfusion injury and could be attenuated by dexamethasone-mediated inhibition of the ERK/NF-κB pathway.American journal of translational research · 2016Article
- DUSP1 phosphatase regulates the proinflammatory milieu in head and neck squamous cell carcinoma.Cancer research · 2014Article
- FOXO1-dependent up-regulation of MAP kinase phosphatase 3 (MKP-3) mediates glucocorticoid-induced hepatic lipid accumulation in mice.Molecular and cellular endocrinology · 2014Article
- Roles for the mitogen-activated protein kinase (MAPK) phosphatase, DUSP1, in feedback control of inflammatory gene expression and repression by dexamethasone.The Journal of biological chemistry · 2014Article
- Ginsenoside Rh1 potentiates dexamethasone's anti-inflammatory effects for chronic inflammatory disease by reversing dexamethasone-induced resistance.Arthritis research & therapy · 2014Article
- Repression of transcription by the glucocorticoid receptor: A parsimonious model for the genomics era.The Journal of biological chemistryReview
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Mapracorat is a novel selective glucocorticoid receptor agonist (SEGRA), structurally distinct from corticosteroids. In preclinical studies, mapracorat potently inhibits the production of a variety of inflammatory mediators including cytokines and prostaglandin E2 (PGE(2)), with limited side effects associated with traditional corticosteroids. The objective of this study was to delineate the mechanisms underlying the anti-inflammatory properties of mapracorat. We found that mapracorat potently inhibited the production of GM-CSF and TNF-α in LPS-stimulated Raw 264.7 macrophages. Mapracorat also substantially attenuated the expression of COX-2 and the production of PGE(2). The inhibition of mapracorat on the inflammatory response was dose-dependent, and substantially inhibitory effects were observed at concentrations in the 10-100 nm range. Examination of the activation kinetics of p38 and its downstream target MAPK-activated protein kinase-2 (MK-2) revealed a shortened activation course after LPS stimulation in cells pretreated with mapracorat. Supporting the notion that mapracorat augments a feedback control mechanism restraining the p38 pathway, we found that mapracorat enhanced the expression of MAPK phosphatase-1 (MKP-1), a critical negative regulator of MAPKs that drive the production of cytokines and other inflammatory mediators. While mapracorat alone did not stimulate MKP-1 expression, it markedly enhanced the expression of MKP-1 in cells stimulated by LPS, in a similar manner and potency to the augmenting effect of dexamethasone. Blocking MKP-1 expression by triptolide also abolished the accelerating effects of mapracorat on p38 and MK-2 deactivation, further supporting a role of MKP-1 in the anti-inflammatory mechanism of mapracorat. Taken together, these results indicate that mapracorat exerts its anti-inflammatory effects, at least in part, by augmenting MKP-1 expression.
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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.