Document Report Card

ID: ALA1146085

Journal: J Med Chem

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

Authors: Wildemann D, Erdmann F, Alvarez BH, Stoller G, Zhou XZ, Fanghänel J, Schutkowski M, Lu KP, Fischer G.

Abstract: 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 progression in HeLa cells in a dose-dependent manner.

CiteXplore: 16570909

DOI: 10.1021/jm060036n