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New candidate drug stops cancer cells, regenerates nerve cells
Date:6/21/2012

CINCINNATI Scientists have developed a small-molecule-inhibiting drug that in early laboratory cell tests stopped breast cancer cells from spreading and also promoted the growth of early nerve cells called neurites.

Researchers from Cincinnati Children's Hospital Medical Center report their findings online June 21 in Chemistry & Biology. The scientists named their lead drug candidate "Rhosin" and hope future testing shows it to be promising for the treatment of various cancers or nervous system damage.

The inhibitor overcomes a number of previous scientific challenges by precisely targeting a single component of a cell signaling protein complex called Rho GTPases. This complex regulates cell movement and growth throughout the body. Miscues in Rho GTPase processes are also widely implicated in human diseases, including various cancers and neurologic disorders.

"Although still years from clinical development, in principle Rhosin could be useful in therapy for many kinds of cancer or possibly neuron and spinal cord regeneration," said Yi Zheng, PhD, lead investigator and director of Experimental Hematology and Cancer Biology at Cincinnati Children's. "We've performed in silica (computerized) rational drug design, pharmacological characterization and cell tests in the laboratory, and we are now starting to work with mouse models."

Because the role of Rho GTPases in cellular processes and cancer formation is well established, researchers have spent years trying to identify safe and effective therapeutic targets for specific parts of the protein complex. In particular, scientists have focused on the center protein in the complex called RhoA, which is essential for the signaling function of the complex. In breast cancer for example, increased RhoA activity makes the cancer cells more invasive and causes them to spread, while a deficiency of RhoA suppresses cancer growth and progression.

Despite this knowledge, past
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Contact: Nick Miller
nicholas.miller@cchmc.org
513-803-6035
Cincinnati Children's Hospital Medical Center
Source:Eurekalert

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