2. Academic Validation
  3. Exploring the Implication of DDX3X in DENV Infection: Discovery of the First-in-Class DDX3X Fluorescent Inhibitor

Exploring the Implication of DDX3X in DENV Infection: Discovery of the First-in-Class DDX3X Fluorescent Inhibitor

  • ACS Med Chem Lett. 2020 Apr 9;11(5):956-962. doi: 10.1021/acsmedchemlett.9b00681.
Annalaura Brai 1,  Adele Boccuto 2,  Martina Monti 3,  Serena Marchi 3,  Ilaria Vicenti 2,  Francesco Saladini 2,  Claudia Immacolata Trivisani 1,  Alessandro Pollutri 1,  Claudia Maria Trombetta 3,  Emanuele Montomoli 3 4,  Valentina Riva 5,  Anna Garbelli 5,  Emanuele Maria Nola 5,  Maurizio Zazzi 2,  Giovanni Maga 5,  Elena Dreassi 1,  Maurizio Botta 1 6
Affiliations

Affiliations

  • 1 Dipartimento Farmaco Chimico Tecnologico, Università degli Studi di Siena, via Aldo Moro 2, 53100 Siena, Italy.
  • 2 Dipartimento di Biotecnologie Mediche, Università degli Studi di Siena, 53100 Siena, Italy.
  • 3 Dipartimento di Medicina Molecolare e dello Sviluppo, Università degli Studi di Siena, 53100 Siena, Italy.
  • 4 VisMederi Srl, Strada del Petriccio e Belriguardo 35, 53100 Siena, Italy.
  • 5 Institute of Molecular Genetics IGM-CNR "Luigi Luca Cavalli-Sforza", via Abbiategrasso 207, 27100 Pavia, Italy.
  • 6 Sbarro Institute for Cancer Research and Molecular Medicine, Center for Biotechnology, College of Science and Technology, Temple University, BioLife Science Building, Suite 333, 1900 N 12th Street, Philadelphia, Pennsylvania 19122, United States.
PMID: 32435411 DOI: 10.1021/acsmedchemlett.9b00681
Abstract

In the absence of effective drugs or vaccines for the treatment of the five Dengue virus serotypes, the search for novel Antiviral drugs is of primary importance for the scientific community. In this context, drug repurposing represents the most used strategy; however, the study of host targets is now attracting attention since it allows identification of broad-spectrum drugs endowed with high genetic barrier. In the last ten years our research group identified several small molecules DDX3X inhibitors and proved their efficacy against different viruses including novel emerging ones. Herein, starting from a screening of our compounds, we designed and synthesized novel derivatives with potent activity and high selectivity. Finally, we synthesized a fluorescent inhibitor that allowed us to study DDX3X cellular localization during DENV Infection in vitro. Immunofluorescence analysis showed that our inhibitor colocalized with DDX3X, promoting the reduction of infected cells and recovering the number of viable cells.

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