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Researchers use new molecular inhibitors to successfully hit difficult cancer target
Date:2/5/2013

in theory block cancer-fueling proteins without causing unwanted toxicity to healthy cells.

The challenge is to design a chemical structure that can attach to appropriate binding sites on a given target enzyme. Usually, only proteins with sufficiently deep hydrophobic pockets are considered "druggable." In their paper, Zheng and his colleagues said this "significantly limits the scope of the drug discovery effort." The surface area of many G-proteins, including RhoA, is mostly spherical and lacks obvious binding pockets.

Using computer drug design and high-throughput molecular screening, Zheng and his colleagues looked for molecular structures capable of blocking G-protein Rho GEFs. They came up with a structure that in computer-based tests appeared to work. The result was Y16 and derivatives that bind to a critical junction site of an enzyme called LARG (which stands for leukemia-associated Rho guanine nucleotide exchange factor). The compound prevents the LARG enzyme from activating RhoA.

Computer tests showed that by blocking LARG, Y16 suppressed the activation of the RhoA cell signaling and downstream molecular events that fuel cancer growth. These computer tests were subsequently verified by laboratory experiments. The degree of suppression was based on the dosage used by researchers.

This suppression was amplified significantly when Y16 was used with Rhosin/G04, which the investigators previously have shown also targets RhoA. Used independently, Y16 and Rhosin/G04 reduced RhoA cell signaling activity by about 50 percent. Used together, the compounds could work synergistically to inhibit RhoA activity and proliferative potential in breast cancer cells, where RhoA signaling is often hyperactive, the researchers said.

When tested on healthy mammary cells not undergoing cancerous transformation, Y16 and Rhosin/G04 did not affect cell function.

The researchers cautioned that an extensive amount of additional r
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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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