Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10748299 | Biochemical and Biophysical Research Communications | 2016 | 6 Pages |
Abstract
Peptidyl prolyl cis/trans isomerization by Pin1 regulates various oncogenic signals during cancer progression, and its inhibition through multiple approaches has established Pin1 as a therapeutic target. However, lack of simplified screening systems has limited the discovery of potent Pin1 inhibitors. We utilized phosphorylation-dependent binding of Pin1 to its specific substrate to develop a screening system for Pin1 inhibitors. Using this system, we screened a chemical library, and identified a novel selenium derivative as Pin1 inhibitor. Based on structure-activity guided chemical synthesis, we developed more potent Pin1 inhibitors that inhibited cancer cell proliferation.
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Authors
Amit Subedi, Takeshi Shimizu, Akihide Ryo, Emiko Sanada, Nobumoto Watanabe, Hiroyuki Osada,