“This protein makes 3 in 4 cancer cases worse”: scientists are on track to stop it | Science & Planet

The MYC protein helps regulate the growth and division of our cells. But in many cancers this protein is ‘overactive’ and contributes to uncontrolled cell division and therefore tumor growth. Because MYC has no fixed structure, it has been very difficult to develop a drug for it until now. An American research team is now on track to curb the MYC protein. “This is one of the holy grails of cancer drug development”

The MYC protein plays a role in the conversion of genetic information for cell growth and cell division. “In healthy cells, the activity of MYC is strictly controlled, but in cancer cells the protein becomes hyperactive,” say Professor Min Xue from the University of California. This overactivation of the MYC protein can cause or accelerate tumor growth. “MYC is like a steroid that makes tumors grow faster,” said Xue. “It is involved in 75% of all cancer cases.”

Xue and his team have been looking for a way to curb the activity of the MYC protein for years, but it is not that simple. Unlike most proteins, MYC does not have a fixed structure. This makes it difficult to develop molecules that can block the protein.

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The protein (orange) binds to MYC (gray) to stop overactive DNA interactions. © Min Xue/UCR

In Previous research using a special approach, the team has already managed to find a small molecule that targets MYC. It involved a short protein fragment in the shape of a double loop. This structure makes the molecule small yet sturdy at the same time. The researchers now used these insights to make a whole range of similar molecules and to see whether there are any that succeed in binding well with MYC. This turns out to be effectively the case, they report now in the journal of the American Chemical Society. “One of the new molecules binds significantly better to MYC, compared to the previous version,” says Xue. “This brings us a lot closer to what we want to achieve for drug development.”

The first lab experiments with NT-B2R, the name the researchers have given the new structure, suggest that it can also effectively curb the activity of the MYC protein. The researchers tested whether the metabolism and growth of cancer cells could be slowed down in petri dishes. More research is needed to know whether NT-B2R is really suitable for drug development. First of all, the researchers are working on a way to efficiently get it into our cells. For the time being, they use nanoparticles as a transport medium for their experiments with cell lines, but this is not ideal for a real therapy.


This makes it one of the holy grails of cancer drug development

Apart from the method for getting NT-B2R into the right cells, the team also wants to further refine the molecule itself. “We believe that further chemical modifications to NT-B2R itself and the search for similar types of molecules could yield even better MYC blockers that we would like to study further,” the researchers write.

The team’s work once again underlines that the search for a medicine is very complicated and that it requires different forms of expertise. For these scientists it is already a fantastic and very motivating challenge: “The MYC protein actually represents chaos, because it has no structure. That, and its direct impact on so many types of cancer, make it one of the holy grails of cancer drug development,” said Xue, who is very excited to be one step closer to that ultimate goal.

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