Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 49, Issue 7, Pages 2147-2150Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm060036n
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Funding
- NIGMS NIH HHS [R01 GM 058556] Funding Source: Medline
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The peptidyl prolyl cis/trans isomerase Pin1 has been implicated in the development of cancer, Alzheimer's disease and asthma, but highly specific and potent Pint inhibitors remain to be identified. Here, by screening a combinatorial peptide library, we identified a series of nanomolar peptidic inhibitors. Nonproteinogenic amino acids, incorporated into 5-mer to 8-mer oligopeptides containing a D-phosphothreonine as a central template, yielded selective inhibitors that blocked cell cycle progression in HeLa cells in a dose-dependent manner.
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