Peptidyl prolyl isomerase Pin1-inhibitory activity of d -glutamic and d -aspartic acid derivatives bearing a cyclic aliphatic amine moiety

The Peptidyl-Prolyl Isomerase Pin1 Regulates

The peptidyl-prolyl isomerase Pin1 regulates cytokinesis through Cep55.

Failure of cytokinesis results in tetraploidy and can increase the genomic instability frequently observed in cancer. The peptidyl-prolyl isomerase Pin1, which is deregulated in many tumors, regulates several processes, including cell cycle progression. Here, we show a novel role for Pin1 in cytokinesis. Pin1 knockout mouse embryonic fibroblasts show a cytokinesis delay, and depletion of Pin1 f...

Generation of a cell-permeable cycloheptapeptidyl inhibitor against the peptidyl-prolyl isomerase Pin1.

Cyclic peptides are capable of binding and modulating challenging drug targets including protein-protein interactions. However, their lack of membrane permeability prevents their application against intracellular targets. In this study, we show that it is possible to design a cell-permeable and biologically active cycloheptapeptide inhibitor against the intracellular enzyme peptidyl-prolyl isom...

Expression of peptidyl-prolyl isomerase PIN1 and its role in the pathogenesis of extrahepatic cholangiocarcinoma

The phosphorylation of proteins on serine/threonine residues that immediately precede proline (pSer/Thr-Pro) is a key signaling mechanism by which cell cycle regulation and cell differentiation and proliferation occur. The peptidyl-prolyl isomerase PIN1-catalyzed conformational changes of the pSer/Thr-Pro motifs may have profound effects on the function of numerous oncogenic and cell signaling ...

Exploring the Structure and Biochemistry of Oxidation-Mediated Inhibitation of the Peptidyl-Prolyl Isomerase PIN1

.................................................................................................................. ii Co-Authorship Statement....................................................................................... iii Acknowledgments.................................................................................................. iv Table of