Cancers, Vol. 11, Pages 531: Efficacy of a Selective Binder of αVβ3 Integrin Linked to the Tyrosine Kinase Inhibitor Sunitinib in Ovarian Carcinoma Preclinical Models
Cancers, Vol. 11, Pages 531: Efficacy of a Selective Binder of αVβ3 Integrin Linked to the Tyrosine Kinase Inhibitor Sunitinib in Ovarian Carcinoma Preclinical Models
Cancers doi: 10.3390/cancers11040531
Authors:
Andrea Sartori
Cristina Corno
Michelandrea De Cesare
Eugenio Scanziani
Lucia Minoli
Lucia Battistini
Franca Zanardi
Paola Perego
Ovarian carcinoma, the most lethal gynecological cancer, is characterized by late diagnosis, with drug resistance limiting the efficacy of platinum-based therapy. Since some integrins are upregulated in cancer, including ovarian carcinoma, they represent a potential target for drug delivery. Receptor tyrosine kinases are also deregulated in cancer and their expression has been associated with drug resistance. Here, the antitumor effects of three conjugates possessing a selective binder of the extracellular portion of integrin αVβ3 covalently linked to the tyrosine kinase inhibitor sunitinib were investigated in cisplatin-sensitive and -resistant ovarian carcinoma cells expressing both tyrosine kinase VEGFR2 and αVβ3 at different levels. We found that one of the three compounds was active in inhibiting the growth of both drug-sensitive and -resistant cells in the micromolar range with a slightly increased potency in resistant cells as compared to sunitinib. The same compound markedly impaired cell migratory and invasive abilities and reduced paxillin phosphorylatio...
Source: Cancers - Category: Cancer & Oncology Authors: Andrea Sartori Cristina Corno Michelandrea De Cesare Eugenio Scanziani Lucia Minoli Lucia Battistini Franca Zanardi Paola Perego Tags: Article Source Type: research