ArticleBritish journal of pharmacology2000
Geldanamycin, an inhibitor of heat shock protein 90 (Hsp90) mediated signal transduction has anti-inflammatory effects and interacts with glucocorticoid receptor in vivo.
Article in British journal of pharmacology, 2000. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers, 1 of them a synthesis that pooled it.
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Who cites it
24 citing papers in PubMed, 1 synthesis or guideline pooled it, 68 citations in OpenAlex.
- Viral Induced Oxidative and Inflammatory Response in Alzheimer's Disease Pathogenesis with Identification of Potential Drug Candidates: A Systematic Review using Systems Biology Approach.Current neuropharmacology · 2019Pooled it
- Geldanamycin treatment does not result in anti-cancer activity in a preclinical model of orthotopic mesothelioma.PloS one · 2023Article
- Peripheral Nerve Regeneration: Opportunities and Challenges.Journal of spine research and surgery · 2023Article
- The Keap1 signaling in the regulation of HSP90 pathway.Cell stress & chaperones · 2022Article
- Targeting HSP90 Inhibits Proliferation and Induces Apoptosis Through AKT1/ERK Pathway in Lung Cancer.Frontiers in pharmacology · 2021Article
- Identification of key genes and pathways for peri-implantitis through the analysis of gene expression data.Experimental and therapeutic medicine · 2017Article
- Activation of Epidermal Growth Factor Receptor in Macrophages Mediates Feedback Inhibition of M2 Polarization and Gastrointestinal Tumor Cell Growth.The Journal of biological chemistry · 2016Article
- Parathyroid hormone regulation of hypoxia-inducible factor signaling in osteoblastic cells.Bone · 2015Article
- Nitric oxide suppresses LPS-induced inflammation in a mouse asthma model by attenuating the interaction of IKK and Hsp90.Experimental biology and medicine (Maywood, N.J.) · 2015Article
- Effect of gedunin on acute articular inflammation and hypernociception in mice.Molecules (Basel, Switzerland) · 2015Article
- Article
- Activation of epidermal growth factor receptor mediates mucin production stimulated by p40, a Lactobacillus rhamnosus GG-derived protein.The Journal of biological chemistry · 2014Article
- Antifungal activity of geldanamycin alone or in combination with fluconazole against Candida species.Mycopathologia · 2013Article
- Berberine inhibits proliferation and down-regulates epidermal growth factor receptor through activation of Cbl in colon tumor cells.PloS one · 2013Article
- A highly selective Hsp90 affinity chromatography resin with a cleavable linker.Bioorganic & medicinal chemistry · 2012Article
- HSP90 inhibition by 17-DMAG reduces inflammation in J774 macrophages through suppression of Akt and nuclear factor-κB pathways.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2012Article
- Hsp90 regulates NADPH oxidase activity and is necessary for superoxide but not hydrogen peroxide production.Antioxidants & redox signaling · 2011Article
- Akt1 is critical for acute inflammation and histamine-mediated vascular leakage.Proceedings of the National Academy of Sciences of the United States of America · 2009Article
- Asymmetric dimethylarginine inhibits HSP90 activity in pulmonary arterial endothelial cells: role of mitochondrial dysfunction.American journal of physiology. Cell physiology · 2008Article
- Evolutionary constraints on chaperone-mediated folding provide an antiviral approach refractory to development of drug resistance.Genes & development · 2007Article
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
Histamine, vascular endothelial growth factor, acetylcholine, oestrogen as well as fluid shear stress activates a mechanism that recruits heat shock protein 90 to the endothelial nitric oxide synthase. The interaction between Hsp90 and eNOS enhances the activation of the enzyme in cells and in intact blood vessels leading to NO production. Intraplantar administration of carrageenan (50 microl paw(-1)) to mice causes an oedema lasting 72 h. Geldanamycin (0.1, 0.3, 1 mg kg(-1)), a specific inhibitor of Hsp-90, that inhibits endothelium-dependent relaxations of the rat aorta, mesentery and middle artery inhibits carrageenan-induced mouse paw oedema in a dose dependent manner. Co-administration to mice of dexamethasone (1 mg kg(-1)) with geldanamycin (0.3 mg kg(-1)) at anti-inflammatory dose causes a loss of the total anti-inflammatory effect of each agent alone. RU 486 (10 mg kg(-1)), a well known glucocorticoid receptorial antagonist, does not inhibit oedema formation but prevents the anti-inflammatory action of dexamethasone (1 mg kg(-1)). Similarly, RU 486 prevents the anti-inflammatory action of geldanamycin (0.3 mg kg(-1)). In conclusion we have described for the first time that geldanamycin, an inhibitor of Hsp90 dependent signal transduction, is anti-inflammatory in vivo implying that Hsp90 is critical for pathways involved in carrageenan-induced paw oedema. In addition the ability of GA to block NO release and reduce oedema formation suggests a therapeutic rationale for specific inhibitors of Hsp90 as potential anti-inflammatory drugs.
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Registered trials
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