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Open AccessArticle

Evaluation of the Anti-Tumor Activity of Small Molecules Targeting Eph/Ephrins in APC min/J Mice

1
Food and Drug Department, University of Parma, Viale delle Scienze 27/a, 43124 Parma, Italy
2
Department of Sociology and Social Research, University of Milano-Bicocca, Via Bicocca degli Arcimboldi 8, 20126 Milan, Italy
3
Department of Veterinary Science, University of Parma, Strada del Taglio 10, 43126 Parma, Italy
*
Author to whom correspondence should be addressed.
Pharmaceuticals 2020, 13(4), 69; https://doi.org/10.3390/ph13040069
Received: 31 March 2020 / Revised: 12 April 2020 / Accepted: 14 April 2020 / Published: 16 April 2020
(This article belongs to the Special Issue Targeting the Eph–ephrin System)
The Eph receptors are the largest receptors tyrosine kinases (RTKs) family in humans and together with ephrin ligands constitute a complex cellular communication system often dysregulated in many tumors. The role of the Eph-ephrin system in colorectal cancer (CRC) has been investigated and different expression of Eph receptors have been associated with tumor development and progression. In light of this evidence, we investigated if a pharmacological approach aimed at inhibiting Eph/ephrin interaction through small molecules could prevent tumor growth in APC min/J mice. The 8-week treatment with the Eph-ephrin antagonist UniPR129 significantly reduced the number of adenomas in the ileum and decreased the diameter of adenomas in the same region. Overall our data suggested as UniPR129 could be able to slow down the tumor development in APC min/J mice. These results further confirm literature data about Eph kinases as a new valuable target in the intestinal cancer and for the first time showed the feasibility of the Eph-ephrin inhibition as a useful pharmacological approach against the intestinal tumorigenesis. In conclusion this work paves the way for further studies with Eph-ephrin inhibitors in order to confirm the Eph antagonism as innovative pharmacological approach with preventive benefit in the intestinal tumor development. View Full-Text
Keywords: Eph-ephrin system; EphA receptors; EphB receptors; Eph antagonist; UniPR129; APC min/J mice; colorectal cancer (CRC); Familial adenomatous polyposis (FAP) Eph-ephrin system; EphA receptors; EphB receptors; Eph antagonist; UniPR129; APC min/J mice; colorectal cancer (CRC); Familial adenomatous polyposis (FAP)
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Corrado, M.; Giorgio, C.; Barocelli, E.; Marzetti, G.V.; Cantoni, A.M.; Di Lecce, R.; Incerti, M.; Castelli, R.; Lodola, A.; Tognolini, M. Evaluation of the Anti-Tumor Activity of Small Molecules Targeting Eph/Ephrins in APC min/J Mice. Pharmaceuticals 2020, 13, 69.

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