Scientific ReportsCancer BiologyPeer-reviewed journal article
Discovery of Z1362873773: A Novel Fascin Inhibitor from a Large Chemical Library for Colorectal Cancer
Alejandro Rodríguez MartíneziD, Lucía Giraldo-Ruiz, María C. RamosiD, Irene LuqueiD, Diogo Ribeiro, Fátima Postigo-CorralesiD, Begoña Alburquerque-GonzáleziD, Silvia Montoro‐GarcíaiD, Ana Belén Arroyo-Rodríguez, Pablo Conesa‐ZamoraiD, Ana María HurtadoiD, Ginés Luengo‐GiliD, Horacio Pérez‐SáncheziD
Abstract
Metastasis 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 ({approx}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 O_FIG O_LINKSMALLFIG WIDTH=200 HEIGHT=123 SRC="FIGDIR/small/606007v1_ufig1.gif" ALT="Figure 1"> View larger version (34K): org.highwire.dtl.DTLVardef@10ddb2borg.highwire.dtl.DTLVardef@afe8b1org.highwire.dtl.DTLVardef@d5f436org.highwire.dtl.DTLVardef@940ddc_HPS_FORMAT_FIGEXP M_FIG C_FIG
- Citations
- 5
- FWCI
- 1.54
- Field percentile
- top 18%
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