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Please use this identifier to cite or link to this item: http://hdl.handle.net/10277/814

Authors: Bodero Padilla, Lizeth Alicia
Title: Synthesis of novel conjugates based on a functionalized cyclo[DKP-isoDGR] integrin ligand and potent cytotoxic agents
Abstract: Targeted drug delivery is a growing-interest field in cancer therapy as a strategy for overcoming the systemic cytotoxicity associated to traditional chemotherapy. One important approach in this research area is represented by the small molecule-drug conjugates (SMDCs), where the drug-targeting is performed by a low molecular weight ligand (peptide, vitamin or peptidomimetic) connected to a potent warhead through a stable linker. This PhD thesis describes the synthesis and biological evaluation of novel SMDCs containing the functionalized cyclo[DKP-isoDGR] integrin ligand developed by our research group and potent cytotoxic drugs (α-amanitin, MMAE and MMAF) combined via different linkers and spacers. The conjugates were evaluated for their binding affinity to the isolated αvβ3 receptor and for their antiproliferative activity on cancer cell lines with different levels of αVβ3 expression in order to study the efficacy of the cyclo[DKP-isoDGR] integrin ligand as a vector for tumor drug-delivery.
Keywords: cancer, drug delivery, integrins, peptidomimetics, isoDGR, SMDC
Issue Date: 2018
Language: eng
Doctoral course: Scienze chimiche e ambientali
Academic cycle: 30
Publisher: Università degli Studi dell'Insubria
Other information: The work herein described was performed at the Insubria University at the Department of Science and Hight Technology – Laboratory of Organic Chemistry in the period from July 2015 to June 2018 under the supervision of Prof. Umberto Piarulli. This project has received funding from the European Union’s Horizon 2020 research and innovation program under the Marie Sklodowska-Curie grant agreement No 642004.
Citation: Bodero Padilla, L.A.Synthesis of novel conjugates based on a functionalized cyclo[DKP-isoDGR] integrin ligand and potent cytotoxic agents (Doctoral Thesis, Università degli Studi dell'Insubria, 2018).

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