Nanomolar inhibitors of the peptidyl prolyl cis/trans isomerase Pin1 from combinatorial peptide libraries.

@article{Wildemann2006NanomolarIO,
  title={Nanomolar inhibitors of the peptidyl prolyl cis/trans isomerase Pin1 from combinatorial peptide libraries.},
  author={Dirk Wildemann and Frank Erdmann and Birte Hernandez Alvarez and Gerlind Stoller and Xiao Zhen Zhou and Joerg Fanghaenel and Mike Schutkowski and Kun Lu and Gunter Fischer},
  journal={Journal of medicinal chemistry},
  year={2006},
  volume={49 7},
  pages={2147-50}
}
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 Pin1 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… CONTINUE READING
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