PRECLINICAL REPORTSHA-1077 inhibits cell migration/invasion of oral squamous cell carcinomaMoreira Carboni, Simone de Sales Costaa; Rodrigues Lima, Nathália Alvesa; Pinheiro, Nanci Mendesa; Tavares-Murta, Beatriz Martinsb; Crema, Virgínia OliveiraaAuthor Information Departments of aStructural Biology bPharmacology, Institute of Natural and Biological Sciences, Federal University of Triângulo Mineiro, Uberaba, MG, Brazil Correspondence to Virgínia Oliveira Crema, Department of Structural Biology, Institute of Natural and Biological Sciences, Federal University of Triângulo Mineiro, Praça Manoel Terra 330, Uberaba, MG, CEP 38025-050, Brazil Tel: +55 34 3318 5463; fax: +55 34 3318 5462; e-mail: [email protected] Received May 19, 2015 Accepted June 19, 2015 Anti-Cancer Drugs: October 2015 - Volume 26 - Issue 9 - p 923-930 doi: 10.1097/CAD.0000000000000267 Buy Metrics Abstract Oral squamous cell carcinoma (OSCC) is the most malignant lesion occurring in the head and neck. The Rho-kinases (ROCKs), effectors of Rho proteins, are involved in actin cytoskeletal organization, cell migration, and maintenance cortex. The HA-1077 inhibits the ROCKs. This study aimed to evaluate the effect of treatment with HA-1077 on cell motility in SCC-4 cells, a cell line originating from human OSCC. F-actin of SCC-4 cells treated or not with HA-1077 (1, 50 and 100 μmol/l), and also HA-1077 50 μmol/l and/or inhibitors Y-27632 30 μmol/l was stained with rhodamine-conjugated phalloidin and analyzed by confocal microscopy. Approximately 1×105 cells/well, control and treated with HA-1077 (25, 50, and 100 μmol/l) were added to the migration plate assay. In addition, 1×105 cells/well, control and treated with HA-1077 50 μmol/l, were tested by invasion assays (plate coated with Matrigel). The inhibition of ROCKs with HA-1077 and/or Y-27632 leads to morphological changes, affecting the organization of the actin. The inhibitory effect of HA-1077 (P<0.0001) was dose dependent as the number of cells migrated at 100 μmol/l was statistically different: 25 μmol/l (P<0.0001) and 50 μmol/l (P<0.01). The number of cells treated with HA-1077 50 μmol/l decreased compared with control cells that invaded through Matrigel (P<0.0001). This study shows an inhibitory effect of HA-1077 on cell migration and invasion, suggesting that the use of HA-1077 can be a potential therapy for OSCC. Copyright © 2015 Wolters Kluwer Health, Inc. All rights reserved.