Scientists control key cancer protein for better treatment

University of California-Riverside researchers have discovered a way to control the MYC protein, which worsens most human cancer cases. Usually helping cell processes, MYC becomes hyperactive in cancer cells, promoting rapid growth. The team developed a molecule that binds to MYC, inhibiting its cancer-promoting function. By dampening MYC’s hyperactivity, they aim to create a window for controlling cancer, offering hope for new treatments.

Xue said, “It’s basically a glob of randomness. Conventional drug discovery pipelines rely on well-defined structures, and this does not exist for MYC.”

A recent Journal of the American Chemical Society paper, led by Xue, unveils a peptide compound inhibiting MYC activity. The researchers found that altering a peptide’s rigidity and shape enhances its interaction with structureless proteins like MYC. By forming rings, peptides become more specific in binding. The team created a peptide with strong, specific interaction—approaching the strength of an antibody. This discovery marks a potential advancement in controlling MYC and treating cancer.

Xue mentioned, “We enhanced the peptide’s binding by a hundred times, moving us closer to drug development goals.” The team now uses lipid nanoparticles to deliver the peptide into cells, though they aim for better delivery methods. Once inside the cell, the peptide binds to MYC, altering its properties and stopping its transcription activities. This progress holds promise for future cancer treatments.

Funding from the U.S. Department of Defense and the National Institutes of Health supports Xue’s work at UC Riverside. His lab focuses on developing molecular tools for understanding biology and drug discovery. 

Intrigued by chaotic processes, Xue is tackling the challenge of controlling MYC, a protein linked to various cancers. MYC’s lack of structure makes it a complex target, but Xue is excited about progress, considering it a potential breakthrough in cancer drug development.

In conclusion, the breakthrough in taming the chaotic protein MYC offers a promising avenue for treating 75% of cancers. Developing a molecule inhibiting MYC’s cancer-promoting function and exploring a peptide compound highlight significant strides in cancer research.

Journal reference:

1. Zhonghan Li, Yi Huang, et al., MYC-Targeting Inhibitors Generated from a Stereodiversified Bicyclic Peptide Library. Journal of the American Chemical Society. DOI: 10.1021/jacs.3c09615.