Discovery of Z1362873773: A Novel Fascin Inhibitor from a Large Chemical Library for Colorectal Cancer

Author:

Rodríguez-Martínez AlejandroORCID,Giraldo-Ruiz Lucía,Ramos Maria C.,Luque Irene,Ribeiro Diogo,Postigo-Corrales Fátima,Alburquerque-González Begoña,Montoro-García Silvia,Arroyo-Rodríguez Ana Belén,Conesa-Zamora Pablo,Hurtado Ana María,Luengo-Gil Ginés,Pérez-Sánchez Horacio

Abstract

AbstractMetastasis is one of the leading causes of cancer-related death worldwide. Fascin is involved in this process by bundling actin filaments and producing protrusions in cancer cells, which facilitate their migration. It has been shown that the overexpression of this protein is related to the appearance of different types of cancer, such as colorectal cancer. In this study, we conducted an in silico screening against the enamine library, a compound library with a broad chemical space (≈1.4M compounds), followed by further validation with physicochemical assays and cellular migration and cytotoxicity tests, thereby obtaining a molecule with considerable fascin inhibitory and migration-arresting capacity similar to other inhibitors already known in the literature.Graphical Abstract

Publisher

Cold Spring Harbor Laboratory

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