Pharmacological inhibition of syntenin PDZ2 domain impairs breast cancer cell activities and exosome loadifing with syndecan and EpCAM cargo.
Leblanc, R., Kashyap, R., Barral, K., Egea-Jimenez, A.L., Kovalskyy, D., Feracci, M., Garcia, M., Derviaux, C., Betzi, S., Ghossoub, R., Platonov, M., Roche, P., Morelli, X., Hoffer, L., Zimmermann, P.(2020) J Extracell Vesicles 10: e12039-e12039
- PubMed: 33343836 
- DOI: https://doi.org/10.1002/jev2.12039
- Primary Citation of Related Structures:  
6R9H, 6RLC - PubMed Abstract: 
Exosomes support cell-to-cell communication in physiology and disease, including cancer. We currently lack tools, such as small chemicals, capable of modifying exosome composition and activity in a specific manner. Building on our previous understanding of how syntenin, and its PDZ partner syndecan (SDC), impact on exosome composition we optimized a small chemical compound targeting the PDZ2 domain of syntenin. In vitro , in tests on MCF-7 breast carcinoma cells, this compound is non-toxic and impairs cell proliferation, migration and primary sphere formation. It does not affect the size or the number of secreted particles, yet it decreases the amounts of exosomal syntenin, ALIX and SDC4 while leaving other exosomal markers unaffected. Interestingly, it also blocks the sorting of EpCAM, a bona fide target used for carcinoma exosome immunocapture. Our study highlights the first characterization of a small pharmacological inhibitor of the syntenin-exosomal pathway, of potential interest for exosome research and oncology.
Organizational Affiliation: 
Equipe labellisée Ligue 2018 Centre de Recherche en Cancérologie de Marseille (CRCM) Aix-Marseille Université, Inserm, CNRS, Institut Paoli-Calmettes Marseille France.