Nature Communications (Jun 2017)
A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action
- Elena Campaner,
- Alessandra Rustighi,
- Alessandro Zannini,
- Alberto Cristiani,
- Silvano Piazza,
- Yari Ciani,
- Ori Kalid,
- Gali Golan,
- Erkan Baloglu,
- Sharon Shacham,
- Barbara Valsasina,
- Ulisse Cucchi,
- Agnese Chiara Pippione,
- Marco Lucio Lolli,
- Barbara Giabbai,
- Paola Storici,
- Paolo Carloni,
- Giulia Rossetti,
- Federica Benvenuti,
- Ezia Bello,
- Maurizio D’Incalci,
- Elisa Cappuzzello,
- Antonio Rosato,
- Giannino Del Sal
Affiliations
- Elena Campaner
- National Laboratory CIB (LNCIB), Area Science Park Padriciano
- Alessandra Rustighi
- National Laboratory CIB (LNCIB), Area Science Park Padriciano
- Alessandro Zannini
- National Laboratory CIB (LNCIB), Area Science Park Padriciano
- Alberto Cristiani
- National Laboratory CIB (LNCIB), Area Science Park Padriciano
- Silvano Piazza
- National Laboratory CIB (LNCIB), Area Science Park Padriciano
- Yari Ciani
- National Laboratory CIB (LNCIB), Area Science Park Padriciano
- Ori Kalid
- Karyopharm Therapeutics
- Gali Golan
- Karyopharm Therapeutics
- Erkan Baloglu
- Karyopharm Therapeutics
- Sharon Shacham
- Karyopharm Therapeutics
- Barbara Valsasina
- Nerviano Medical Sciences Srl
- Ulisse Cucchi
- Nerviano Medical Sciences Srl
- Agnese Chiara Pippione
- Department of Science and Drug Technology, University of Torino
- Marco Lucio Lolli
- Department of Science and Drug Technology, University of Torino
- Barbara Giabbai
- Elettra Sincrotrone Trieste S.C.p.A., Area Science Park Basovizza
- Paola Storici
- Elettra Sincrotrone Trieste S.C.p.A., Area Science Park Basovizza
- Paolo Carloni
- Computational Biomedicine, Institute for Advanced Simulation (IAS-5) and Institute of Neuroscience and Medicine (INM-9), Forschungszentrum Jülich
- Giulia Rossetti
- Computational Biomedicine, Institute for Advanced Simulation (IAS-5) and Institute of Neuroscience and Medicine (INM-9), Forschungszentrum Jülich
- Federica Benvenuti
- International Centre for Genetic Engineering and Biotechnology (ICGEB), Area Science Park Padriciano
- Ezia Bello
- IRCCS-Mario Negri Institute for Pharmacological Research
- Maurizio D’Incalci
- IRCCS-Mario Negri Institute for Pharmacological Research
- Elisa Cappuzzello
- Department of Surgery, Oncology and Gastroenterology, Oncology and Immunology Section, University of Padova
- Antonio Rosato
- Department of Surgery, Oncology and Gastroenterology, Oncology and Immunology Section, University of Padova
- Giannino Del Sal
- National Laboratory CIB (LNCIB), Area Science Park Padriciano
- DOI
- https://doi.org/10.1038/ncomms15772
- Journal volume & issue
-
Vol. 8,
no. 1
pp. 1 – 15
Abstract
PIN1 is a promising therapeutic target for cancer treatment. In this study, the authors identify a covalent inhibitor of PIN1 with anti-tumour and anti-metastatic properties thanks to PIN1 inactivation and to the release, after binding to PIN1, of a quinone-mimicking compound that elicits reactive oxygen generation and causes DNA damage.
