my.chemeurope.com
With an accout for my.chemeurope.com you can always see everything at a glance – and you can configure your own website and individual newsletter.
Sphingomyelinases are a group of hydrolases that cleave sphingomyelin, a common component of plasma membranes, to form ceramide and phosphocholine. Ceramide is a second messenger that is present in virtually all cell types and regulates a variety of cellular functions such as proliferation, differentiation, apoptosis, and inflammation response. Inhibition of sphingomyelinase activity to reduce ceramide concentrations has recently emerged as a potential therapeutic approach for several diseases including atherosclerosis, pathogen infections, inflammation, diabetes, and obesity. To effectively screen compound collections for the identification of new sphingomyelinase inhibitors, we have developed a high-throughput assay utilizing the natural substrate sphingomyelin in 1,536-well plate format. The assay has a signal-to-basal ratio of 6.1-fold in pH 5.0 buffer and 4.3-fold in pH 6.5 buffer, indicating a robust assay for compound library screening. A screen of ~300,000 compounds using this assay led to the identification of eight compounds as sphingomyelinase inhibitors (IC50s = 1.7 to 38.2 μM) that exhibited different activities between the natural substrate assay and profluorescence substrate assay. The results demonstrate the robustness and effectiveness of the natural substrate sphingomyelinase assay for screening sphingomyelinase inhibitors.
| Authors: | Miao Xu, Ke Liu, Noel Southall, Juan J. Marugan, Alan T. Remaley, Wei Zheng | |
| Journal: | Analytical and Bioanalytical Chemistry | |
| Year: | 2012 | |
| DOI: | 10.1007/s00216-012-6174-5 | |
| Publication date: | 19-06-2012 |
Watchlist
This is where you can add this publication to your personal favourites.
Additional Information
Nematicidal activity of essential oils: a review
Plant parasitic nematodes are the most destructive group of plant pathogens worldwide and their control is extremely challenging. Plant Essential oils (EOs) and their constituents have a great potential in nematode control since they can be developed for use as nematicides themselves or can ... more
For over a century, ulcer has been a major cause of morbidity and mortality. Its treatment has progressed from vagotomy to proton pump inhibitors. However, the drugs used produce many adverse effects and are less effective than they ought to be. Therefore, there is a growing interest in alt ... more
Endophytic fungi from medicinal plants: a treasure hunt for bioactive metabolites
Endophytic fungi are ubiquitous organisms found in the plants, residing intercellular or intracellular, at least for a portion of their lives without causing apparent symptoms of infection. Almost all plants are known to harbor endophytes. The choice of the plant to be used for exploring en ... more
Cocktail achieves superconducting boost
Physicists describe how they have synthesized a new material that belongs to the iron-selenide class of superconductors, called LixFe2Se2(NH3)y, in a paper about to be published in EPJ B. The work was carried out by Ernst-Wilhelm Scheidt from the University of Augsburg and colleagues. This ... more
US underestimates costs of carbon pollution and climate change
The U.S. federal government is significantly underestimating the costs of carbon pollution because it is using a faulty analytical model, according to a new study published in the Journal of Environmental Studies and Sciences. A more appropriate accounting of costs would pave the way to cle ... more
Vladimir V. Dmitriev awarded prestigious prize in low temperature physics
Springer advisory board member Vladimir V. Dmitriev, along with fellow scientists Yuriy M. Bunkov and Igor A. Fomin, have been named winners of the 2008 Fritz London Memorial Prize for their discovery and understanding of the "Phase Coherent Spin Precession and Spin Superfluidity of 3He-B." ... more
Über CHEMIE.DE
CHEMIE.DE Information Service GmbH runs specialist scientific internet portals. The secret to our success? We are familiar with what we publish.
Advertising at CHEMIE.DE
Our advertising formats support you in getting your message across to a clearly defined target audience.
© 1997-2013 CHEMIE.DE Information Service GmbH, All rights reserved
Netmeeting
