ArticleBritish journal of pharmacology2002
Pharmacological profile of PKF242-484 and PKF241-466, novel dual inhibitors of TNF-alpha converting enzyme and matrix metalloproteinases, in models of airway inflammation.
Article in British journal of pharmacology, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 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
16 citing papers in PubMed, 87 citations in OpenAlex.
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- Exposure to lipopolysaccharide (LPS) reduces contractile response of small airways from GSTCD-/- mice.PloS one · 2019Article
- Inhibition of hepatocellular carcinoma cell proliferation, migration, and invasion by a disintegrin and metalloproteinase-17 inhibitor TNF484.Journal of research in medical sciences : the official journal of Isfahan University of Medical Sciences · 2019Article
- Diagnosis, monitoring and prevention of exposure-related non-communicable diseases in the living and working environment: DiMoPEx-project is designed to determine the impacts of environmental exposure on human health.Journal of occupational medicine and toxicology (London, England) · 2018Review
- Inflammatory and Oxidative Stress Markers in Experimental Allergic Asthma.Inflammation · 2017Article
- Activation of Proinflammatory Responses in Cells of the Airway Mucosa by Particulate Matter: Oxidant- and Non-Oxidant-Mediated Triggering Mechanisms.Biomolecules · 2015Review
- Article
- The effectiveness of fish oil supplementation in asthmatic rats is limited by an inefficient action on ASM function.Lipids · 2013Article
- ADAM17-mediated processing of TNF-α expressed by antiviral effector CD8+ T cells is required for severe T-cell-mediated lung injury.PloS one · 2013Article
- p38 MAPK inhibitors, IKK2 inhibitors, and TNFα inhibitors in COPD.Current opinion in pharmacology · 2012Review
- Lung endothelial ADAM17 regulates the acute inflammatory response to lipopolysaccharide.EMBO molecular medicine · 2012Article
- Suppression of TNF receptor-1 signaling in an in vitro model of epileptic tolerance.International journal of physiology, pathophysiology and pharmacology · 2011Article
- Formation of a ternary complex among NHERF1, beta-arrestin, and parathyroid hormone receptor.The Journal of biological chemistry · 2010Article
- ADAM-17: the enzyme that does it all.Critical reviews in biochemistry and molecular biology · 2010Review
- Agonist-regulated cleavage of the extracellular domain of parathyroid hormone receptor type 1.The Journal of biological chemistry · 2010Article
- Transmembrane proteases in cell growth and invasion: new contributors to angiogenesis?Oncogene · 2004Review
Corrections and comments
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Authors and funding
5 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. TNF-alpha converting enzyme (TACE) and matrix metalloproteinases (MMPs) are believed to play a role in various airway inflammatory disorders. Therefore we have tested the effect of two new inhibitors of TACE/MMPs (PKF242-484, PKF241-466) in models of airway inflammation. 2. PKF242-484 and PKF241-466 inhibited purified MMP-1, -2, -3, -9, -13 and rat collagenase at low nanomolar range. Both compounds inhibited the TNF-alpha release from activated human peripheral blood mononuclear cells with IC(50) values of 56+/-28 and 141+/-100 nM, respectively and had no significant effect on the activation of other human leukocytes, as neither neutrophils and eosinophils oxidative burst nor proliferation or cytokines production by T cells were inhibited in vitro. 3. PKF242-484 and PKF241-466 had beneficial effects in two different murine models of acute lung inflammation in vivo. The influx of neutrophils and lymphocytes into the airways was reduced 3 and 24 h after intranasal LPS challenge. This was accompanied by reduced levels of myeloperoxidase and elastase activities in the bronchoalveolar lavage. Furthermore, a complete inhibition of TNF-alpha release into the airways was observed. In addition, PKF242-484 effectively reduced the influx of neutrophils, eosinophils and lymphocytes in a model of acute allergic lung inflammation. 4. PKF242-484 and PKF241-466 are two novel and potent dual inhibitors of TACE and MMPs, which show activity in in vivo models of lung inflammation. Such compounds could have beneficial effects in airway inflammatory conditions such as asthma and chronic obstructive pulmonary disease.
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