A team of scientists has used a novel approach to identify protein degraders that target Pin1, a protein involved in pancreatic cancer development.
In drug discovery, targeted protein degradation is a method that selectively eliminates disease-causing proteins. A University of California, Riverside team of scientists has used a novel approach to identify protein degraders that target Pin1, a protein involved in pancreatic cancer development.that it has designed agents that not only bind tightly to Pin1 but are designed to cause its destabilization and cellular degradation -- a finding that could pave the way for new cancer therapies.
The researchers' interest in studying Pin1 was two-fold. They wanted to identify potent molecules that could degrade Pin1. They also wanted to study the role of Pin1 in the crosstalk between pancreatic cancer cells and the tumor microenvironment -- macrophages and cancer-associated fibroblasts -- where Pin 1 is also expressed. Macrophages are a type of white blood cell. Cancer-associated fibroblasts are cells that play a key role in the development and progression of tumors.
Pellecchia explained that if his team can kill cancer-associated fibroblasts through Pin1 inhibition, then it is possible that pancreatic cancer cells will be more susceptible to anticancer agents. The difficulty until now, Pellecchia said, has been how to obtain potent and selective Pin1 inhibitors that can penetrate cancer-associated fibroblasts and/or cancer cells and, at the same time, block the function of Pin1, possibly eliminating Pin1 altogether by inducing its degradation.
"Our collaboration would like to see if we can administer these agents to pancreatic cancer patients or other patients that develop peritoneal metastasis, which is often associated with cancer-associated fibroblast activity," Pellecchia said."Ultimately, we hope to develop our agents into novel cancer therapeutics in this collaboration."
Pellecchia was joined in the research by Giulia Alboreggia, the first author of the paper, and Parima Udompholkul, who work in his laboratory; and Isaac Rodriguez and Gregor Blaha. Rodriguez works in Blaha's laboratory.Fighting cancer effectively often involves stopping cancer cells from multiplying, which requires understanding proteins that the cells rely on to survive. Protein profiling plays a critical role in ...
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