Targeting PIN1

The peptidyl-prolyl cis-trans isomerase PIN-1 is an important regulator of cellular processes. It is known for its unique ability to specifically identify and catalyze the isomerization of the phosphorylated serine/threonine-proline motif (pSer/Thr-Pro) in proteins, which affects the target protein's function. Due to its multibiological functions in vivo, Pin1 is extensively studied as a promising drug target for various human diseases, especially cancer. Starting from the structure of one of the most potent PIN1 inhibitors KPT-6566, we aim to identify new hits for developing novel and efficient PIN1 inhibitors, to reach the preclinical studies.

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Collaborations

  • Prof. Giannino Del Sal, International Centre of Genetic Engineering and Biotechnology (ICGEB), Area Science Park-Padriciano, Trieste (IT) and IFOM ETS, the AIRC Institute of Molecular Oncology, Milano (IT)
  • Dr. Alessandra Rustighi, Dep. of Life Sciences, University of Trieste (IT)
  • Dr. Rosa Maria Vitale, Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Pozzuoli, Napoli (IT)
  • Dr. Pietro Amodeo, Institute of Biomolecular Chemistry, National Research Council (ICB-CNR), Pozzuoli, Napoli (IT)

Representative pubblications & Projects

  • E. Campaner, A. Rustighi, A. Zannini, A. Cristiani, S. Piazza, Y. Ciani, o. Kalid, G. Golan, E. Baloglu, S. Shacham, B. Valsasina, U. Cucchi, A. C. Pippione, M. L. Lolli, B. Giabbai, P. Storici, P. Carloni, G. Rossetti, F. Benvenuti, E. Bello, M. D’Incalci, E. Cappuzzello, A. Rosato, G. Del Sal. A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action. Nature Communications, 2017, (8), 15772.  https://doi.org/10.1038/ncomms15772


  •  “PRIN-UNO - Prolyl isomerase PIN1 inhibitors: a drug design strategy against aggressive tumors” funded by the Italian Ministry of University and Research, program “Projects of relevant national interest (PRIN)”, call 2022 PNRR (National Recovery and Resilience Plan). The fund is active rom 12/1/2023 to 11/30/2025.