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New Combinatorial Chemistry Study Findings Have Been Reported from MSKCC (A 1536-Well Fluorescence Polarization Assay to Screen for Modulators of the...

August 20, 2014



New Combinatorial Chemistry Study Findings Have Been Reported from MSKCC (A 1536-Well Fluorescence Polarization Assay to Screen for Modulators of the MUSASHI Family of RNA-Binding Proteins)

By a News Reporter-Staff News Editor at Biotech Week -- Data detailed on Combinatorial Chemistry have been presented. According to news reporting from New York City, New York, by NewsRx journalists, research stated, "RNA-binding proteins (RBPs) can act as stem cell modulators and oncogenic drivers, but have been largely ignored by the pharmaceutical industry as potential therapeutic targets for cancer. The MUSASHI (MSI) family has recently been demonstrated to be an attractive clinical target in the most aggressive cancers."

The news correspondents obtained a quote from the research from MSKCC, "Therefore, the discovery and development of small molecule inhibitors could provide a novel therapeutic strategy. In order to find novel compounds with MSI RNA binding inhibitory activity, we have developed a fluorescence polarization (FP) assay and optimized it for high throughput screening (HTS) in a 1536-well microtiter plate format. Using a chemical library of 6,208 compounds, we performed pilot screens, against both MSI1 and MSI2, leading to the identification of 7 molecules for MSI1, 15 for MSI2 and 5 that inhibited both. A secondary FP dose-response screen validated 3 MSI inhibitors with IC50 below 10 mu M. Out of the 25 compounds retested in the secondary screen only 8 demonstrated optical interference due to high fluorescence. Utilizing a SYBR-based RNA electrophoresis mobility shift assay (EMSA), we further verified MSI inhibition of the top 3 compounds. Surprisingly, even though several aminoglycosides were present in the library, they failed to demonstrate MSI inhibitor activity challenging the concept that these compounds are pan-active against RBPs."

According to the news reporters, the research concluded: "In summary, we have developed an in vitro strategy to identify MSI specific inhibitors using an FP HTS platform, which will facilitate novel drug discovery for this class of RBPs."

For more information on this research see: A 1536-Well Fluorescence Polarization Assay to Screen for Modulators of the MUSASHI Family of RNA-Binding Proteins. Combinatorial Chemistry & High Throughput Screening, 2014;17(7):596-609. Combinatorial Chemistry & High Throughput Screening can be contacted at: Bentham Science Publ Ltd, Executive Ste Y-2, PO Box 7917, Saif Zone, 1200 Br Sharjah, U Arab Emirates. (Bentham Science Publishers - www.benthamscience.com; Combinatorial Chemistry & High Throughput Screening - www.benthamscience.com/cchts/index.htm)

Our news journalists report that additional information may be obtained by contacting G. Minuesa, MSKCC, HTS Core Facil, New York, NY, United States. Additional authors for this research include C. Antczak, D. Shum, C. Radu, B. Bhinder, Y.M. Li, H. Djaballah and M.G. Kharas (see also Combinatorial Chemistry).

Keywords for this news article include: New York City, United States, Combinatorial Chemistry, North and Central America

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2014, NewsRx LLC


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Source: Biotech Week


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