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Selective Integrin Ligands Promote Cell Internalization of the Antineoplastic Agent Fluorouracil.
Baiula, Monica; Cirillo, Martina; Martelli, Giulia; Giraldi, Valentina; Gasparini, Elisa; Anelli, Alessandro Claudio; Spampinato, Santi Mario; Giacomini, Daria.
Afiliación
  • Baiula M; Department of Pharmacy and Biotechnology, University of Bologna, Via Irnerio, 48, 40126, Bologna, Italy.
  • Cirillo M; Department of Chemistry "G. Ciamician", University of Bologna, Via Selmi 2, 40126 Bologna, Italy.
  • Martelli G; Department of Chemistry "G. Ciamician", University of Bologna, Via Selmi 2, 40126 Bologna, Italy.
  • Giraldi V; Department of Pharmacy and Biotechnology, University of Bologna, Via Irnerio, 48, 40126, Bologna, Italy.
  • Gasparini E; Department of Chemistry "G. Ciamician", University of Bologna, Via Selmi 2, 40126 Bologna, Italy.
  • Anelli AC; Department of Chemistry "G. Ciamician", University of Bologna, Via Selmi 2, 40126 Bologna, Italy.
  • Spampinato SM; Department of Chemistry "G. Ciamician", University of Bologna, Via Selmi 2, 40126 Bologna, Italy.
  • Giacomini D; Department of Pharmacy and Biotechnology, University of Bologna, Via Irnerio, 48, 40126, Bologna, Italy.
ACS Pharmacol Transl Sci ; 4(5): 1528-1542, 2021 Oct 08.
Article en En | MEDLINE | ID: mdl-34661072
Drug conjugates consisting of an antineoplastic drug and a targeting receptor ligand could be effective to overcome the heavy side effects of unselective anticancer agents. To address this need, we report here the results of a project aimed to study agonist and antagonist integrin ligands as targeting head of molecular cargoes for the selective delivery of 5-fluorouracil (5-FU) to cancer or noncancer cells. Initially, two fluorescent ß-lactam-based integrin ligands were synthesized and tested for an effective and selective internalization mediated by α4ß1 or α5ß1 integrins in Jurkat and K562 cells, respectively. No cellular uptake was observed for both fluorescent compounds in HEK293 noncancerous control cells. Afterward, three conjugates composed of the ß-lactam-based integrin ligand, suitable linkers, and 5-FU were realized. The best compound E, acting as α5ß1 integrin agonist, is able to selectively deliver 5-FU into tumor cells, successfully leading to cancer cell death.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Pharmacol Transl Sci Año: 2021 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Estados Unidos
Texto completo
Añadir a Mi BVS
Imprimir
XML
PubMed Links
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Idioma: En Revista: ACS Pharmacol Transl Sci Año: 2021 Tipo del documento: Article País de afiliación: Italia Pais de publicación: Estados Unidos