Pre-clinical evaluation of a potent and effective Pin1-degrading agent in pancreatic cancer.

ABSTRACT: The peptidyl-prolyl isomerase protein Pin1 has been shown to contribute to cancer onset, development, and progression by regulating the function and stability of oncogenes and tumor suppressors, both in cancer cells and surrounding stromal cells. Hence, it has long been sought as a possible therapeutic target in oncology. However, further validation of Pin1 as a suitable target for novel therapeutic strategies requires the development of potent and effective pharmacological inhibitors, which are currently scarce. Very recently, we reported novel covalent Pin1 inhibitors that, acting as molecular crowbars, destabilize the protein in vitro, causing its degradation in cells. Here, we advanced those agents by improving their plasma stability. We further characterized their mode of actio

SUBMITTER: Alboreggia G 

PROVIDER: S-EPMC12657321 | biostudies-literature | 2025 Dec

REPOSITORIES: biostudies-literature