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A groundbreaking discovery in cancer drug development - A groundbreaking discovery in cancer drug development

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An incurable disease -

Despite decades of research, there is currently no cure for any type of cancer.

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Cancer cases set to rise -

The latest report from the World Health Organization (WHO) predicts that there will be over 35 million new cases of cancer in 2050.

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A grim prediction -

That grim prediction marks a significant rise from the approximate 20 million cancer cases that occurred in 2022 and translates as a forecasted 77% increase over a 28-year period.

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New methods of treatment needed -

With numbers growing and no cure in sight, scientists continue to explore new methods to both prevent and treat cancer.

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Breakthrough -

But now, recent insight into a specific protein could pave the way for new cancer treatments.

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A culprit is identified -

Researchers from the University of California, Riverside (UCR) have identified a new way to change the physical properties of a specific protein known to be the culprit in about 75% of all human cancer cases.

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A specific protein -

Central to this groundbreaking study is a specific protein called MYC.

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What is MYC? -

MYC is a transcription factor, which means it helps regulate the rate of copying genetic information from DNA to messenger RNA into healthy cells.

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What does MYC do? -

In other words, this gene is a proto-oncogene and encodes a nuclear phosphoprotein that plays a significant role in cell cycle progression, apoptosis (the death of cells which occurs as a normal and controlled part of an organism's growth or development), and cellular transformation.

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Rogue reaction -

But here's the kicker: while MYC is part of healthy cell activity, with cancer cells MYC becomes hyperactive and ultimately helps cancer tumors grow.

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The genesis of many cancers -

In fact, the MYC oncogene contributes to the genesis of many human cancers.

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Potential treatment target -

MYC's association with cancer has been identified in previous studies, with the protein examined as a potential treatment target.

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Reining in MYC -

Now, however, scientists believe they have found a way of stopping MYC going outside of its normal, carefully controlled role and promoting the spread of cancer.

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How cancer cells multiply -

"Cancer cells are hyperactive, and they replicate themselves without supervision. You can think of them as a mass-production pipeline of biomolecules," outlined senior study author Min Xue, a biochemist at UCR.

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The role of DNA -

"All these production processes are based on some blueprint, which is DNA. MYC facilitates access to that blueprint information, enabling a constant supply of building blocks for uncontrolled growth," added Xue, speaking to Medical News Today.

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Difficult to identify -

MYC is by and large a shapeless protein. It doesn't have a structure that can be targeted. This makes it difficult for drugs to effectively identify MYC and keep it behaving normally.

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A challenging task -

The challenge therefore facing Xue and his team was to develop a peptide compound that could bind or interact with MYC and help get it back under control.

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What is a peptide? -

A peptide is a molecule that contains two or more amino acids (the molecules that join together to form proteins). Peptides act as structural components of cells and tissues, hormones, toxins, antibiotics, and enzymes.

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Exploring new methods -

The UCR scientists explored a new peptide capable of creating a strong bond directly to MYC. "We designed a 'bicyclic peptide,' which has a 3D binding surface and can be considered as a miniature version of a protein," Xue explained.

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NT-B2R -

This peptide, called NT-B2R, proved particularly adept at disabling MYC.

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Changing the rules -

As detailed by ScienceAlert, in tests using a culture made from human brain cancer cells, NT-B2R was shown to successfully bind to MYC, changing the way cells regulated many of its genes and ultimately decreasing the metabolism and proliferation of the cancer cells.

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The binding process -

"Peptides can assume a variety of forms, shapes, and positions. Once you bend and connect them to form rings, they cannot adopt other possible forms, so they then have a low level of randomness. This helps with the binding," elaborated Xue.

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An effective inhibitor -

"[Peptides] can bind to MYC and change MYC's physical properties, preventing it from accessing the information in the DNA. ... [And] because MYC is essential in fueling a wide collection of cancers, an effective MYC inhibitor may help us treat those cancers," he continued.

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Creating cancer therapeutics -

"An added bonus is that these cancer cells are more addicted to the high level of MYC activities, way above the normal cells, and this property can help create cancer therapeutics with fewer side effects."

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Method of delivery -

Researchers delivered the peptide through small spheres of fatty molecules called lipid nanoparticles. However, they plan to examine other options. This method is not very convenient for a drug, Xue conceded. "We are exploring other ways to make the peptide enter the cells autonomously."

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Improvements needed -

"We are also working on improving the potency of the peptide," added Xue. "The current version is not strong enough for a drug. But I think we are off to a very good start."

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No "silver bullet" -

While early results of the study undertaken by the team at UCR look promising, Xue warned that there is no "silver bullet" for all cancers.

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A deadly collection -

"Cancer is not 'a disease'—it's a collection of diseases. Each cancer has its own characteristics, and even the same type of cancer can manifest differently among patients."

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The next step -

There's still a lot of work to be done, admitted Xue, "and the next step will be to carry out rigorous tests in human subjects."

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Stopping the spread of cancer -

"But we just might have found a method for stopping one of the ways in which cancer hijacks healthy biological processes in order to survive."

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The "holy grail" of cancer drug development -

"MYC represents chaos, basically, because it lacks structure," Xue reiterated. "That, and its direct impact on so many types of cancer make it one of the holy grails of cancer drug development. We are very excited that it is now within our grasp."

Sources: (Medical News Today) (WHO) (National Center for Biotechnology Information) (ScienceAlert) (Journal of the American Chemical Society)

See also: Skin cancer: everything you should know

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