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Case Western Reserve researcher discovers new 'anti-pathogenic' drugs to treat MRSA
Date:9/16/2010

hroughout the body.

The screening for AgrA inhibitors was initially carried out in a computer by docking a library of 90,000 compounds and finding out which compounds would fit best into the activation site on AgrA. Subsequently, about one hundred of the best scoring compounds were acquired and tested in the laboratory for inhibition of the production of a toxin that ruptures red blood cells.

Seven of these compounds were found to be active. Testing compounds bearing chemical similarity to the original compounds lead to the discovery of additional and more potent compounds.

More than a dozen active compounds have been discovered by this method. The best drug candidate reduces red blood cell rupture to 12% of the value without the drug at a concentration of 10 g/mL, without affecting bacterial growth..

"It is possible to inhibit virulence of MRSA without killing the bacteria," continued Dr. Shoham. "Such anti-pathogenic drugs may be used for prophylaxis or therapy by themselves or in combination with an antibiotic."

This research was carried out in the laboratory of Dr. Menachem Shoham in the Department of Biochemistry at the Case Western Reserve University School of Medicine in Cleveland, Ohio. Funding was provided by grants from the Steris Corporation and from the American Heart Association.

The results were presented at the 50th Interscience Conference on Antimicrobial Agents and Chemotherapy, Boston Conference Center earlier this week.


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Contact: Christina DeAngelis
christina.deangelis@case.edu
216-368-3635
Case Western Reserve University
Source:Eurekalert

Page: 1 2

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