Three University of North Florida (UNF) researchers have been awarded a U.S. patent for a targeted cancer-fighting compound, or peptoid, that the team has discovered targets certain breast, colon and lung cancers and stops them from progressing. This promising discovery could lead to significantly better patient outcomes for difficult to treat cancers.
UNF is among the very first studies to explore the use of peptoids for early cancer diagnosis and potential treatment and is the only known university conducting this type of study.
The research is focused on a group of proteins called protein arginine methyltransferases (PRMT) to understand why they become overproduced and highly activated, causing them to bind with more proteins in the body. When this happens, it creates a chemical mark on proteins called methylation, which subsequently causes cancer genes that were previously suppressed to become active -; it turns cancer on.
The UNF faculty team includes lead researcher Dr. Bryan Knuckley, Department of Chemistry and Biochemistry chair and professor, Dr. Corey Causey, chemistry and biochemistry associate professor, and Dr. Fatima Rehman, biology associate lecturer.
We're still early on in the process, but this is an exciting development, and the research shows promising intervention for the treatment of some aggressive cancers."
Dr. Bryan Knuckley, Department of Chemistry and Biochemistry chair and professor
Knuckley first began this research soon after joining UNF's faculty in 2012. He spearheaded the project by identifying and developing new peptoid compounds and conducting biochemical studies to validate their targeting of PRMT proteins. Causey created the essential building blocks needed for the synthesis of these innovative peptoids. Rehman played a crucial role in testing the efficacy and specificity of these novel compounds in human cancer and normal cells, assessing their potential as a targeted cancer therapy. Several undergraduate students have also been involved in the research since 2019.
The team is currently examining the exact mechanism of action through which these peptoids kill cancer cells specifically along with further testing of individual peptoids designed during the study, while waiting for a second related patent they hope to be awarded within the year. The first patent is focused on the treatment of cancers using peptoids targeting PRMTs, while the second patent awaiting approval is for the specific peptoid compounds.
"This is a lifetime project to contribute to ending cancer," said Knuckley. "We want to continue our research and testing to better understand how these proteins work and how we can improve upon the inhibitor to develop new therapies or pharmaceuticals."
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Journal reference:
DuBose, M. B., et al. (2022). A peptoid-based inhibitor of protein arginine methyltransferase 1 (PRMT1) induces apoptosis and autophagy in cancer cells. Journal of Biological Chemistry. doi.org/10.1016/j.jbc.2022.102205.