2. Academic Validation
  3. Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents

Drug Design and Synthesis of First in Class PDZ1 Targeting NHERF1 Inhibitors as Anticancer Agents

  • ACS Med Chem Lett. 2019 Jan 14;10(4):499-503. doi: 10.1021/acsmedchemlett.8b00532.
Antonio Coluccia 1,  Giuseppe La Regina 1,  Valentina Naccarato 1,  Marianna Nalli 1,  Viviana Orlando 2,  Stefano Biagioni 2,  Maria Laura De Angelis 3,  Marta Baiocchi 3,  Candice Gautier 4,  Stefano Gianni 4,  Fiorella Di Pastena 5,  Laura Di Magno 6,  Gianluca Canettieri 5,  Addolorata Maria Luce Coluccia 7,  Romano Silvestri 1
Affiliations

Affiliations

  • 1 Department of Drug Chemistry and Technologies, Sapienza University of Rome, Laboratory affiliated to Istituto Pasteur Italia - Fondazione Cenci Bolognetti, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
  • 2 Department of Biology and Biotechnologies "Charles Darwin", Sapienza University of Rome, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
  • 3 Department of Oncology and Molecular Medicine, Istituto Superiore di Sanità, Viale Regina Elena, 299, 00161 Rome, Italy.
  • 4 Department of Biochemistry, Sapienza University of Rome, Laboratory affiliated to Istituto Pasteur Italia - Fondazione Cenci Bolognetti, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
  • 5 Department of Molecular Medicine, Sapienza University of Rome, Laboratory affiliated to Istituto Pasteur Italia - Fondazione Cenci Bolognetti, Viale Regina Elena, 291, I-00161 Roma, Italy.
  • 6 Center for Life Nano Science@Sapienza, Istituto Italiano di Tecnologia, 00161 Rome, Italy.
  • 7 Department of Biological and Environmental Sciences and Technologies, University of Salento, I-73100 Lecce, Italy.
PMID: 30996786 DOI: 10.1021/acsmedchemlett.8b00532
Abstract

Targeted approaches aiming at modulating NHERF1 activity, rather than its overall expression, would be preferred to preserve the normal functions of this versatile protein. We focused our attention on the NHERF1/PDZ1 domain that governs its membrane recruitment/displacement through a transient phosphorylation switch. We herein report the design and synthesis of novel NHERF1 PDZ1 domain inhibitors. These compounds have potential therapeutic value when used in combination with antagonists of β-catenin to augment apoptotic death of colorectal Cancer cells refractory to currently available Wnt/β-catenin-targeted agents.

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