Can a fungal compound discovered more than 50 years ago have the potential to treat brain cancer? A group of chemists from the Massachusetts Institute of Technology (MIT) might have cracked the code.
“We have a much better appreciation for how those subtle structural changes can significantly increase the synthetic challenge. Now we have the technology where we can not only access them for the first time, more than 50 years after they were isolated, but also we can make many designed variants, which can enable further detailed studies," says Mohammad Movassaghi, an MIT professor of chemistry.
The fungal compound in discussion, verticillin A, has a complex structure, which made it more difficult for experts to synthesise than related compounds, even though they say it differed by only a couple of atoms.
Researchers at MIT mentioned that the derivative of verticillin A showed promising results as an anticancer agent against a type of pediatric brain cancer called diffuse midline glioma (DMG) that has few treatment options.
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The researchers found that the DMG cell lines most susceptible to these compounds were those that have high levels of a protein called EZHIP. This protein, which plays a role in the methylation of DNA, has been previously identified as a potential drug target for DMG. The verticillin derivatives appear to interact with EZHIP in a way that increases DNA methylation, which induces the cancer cells to undergo programmed cell death, informed MIT.
However, experts stress that more tests will be needed to evaluate its potential for clinical use.