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Issue 2, 2015
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PEGylation enhances the tumor selectivity of melanoma-targeted conjugates

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Abstract

In the development of our melanoma-selective delivery approach, three preselected conjugates of 5-iodo-2′-deoxyuridine (IUdR) to the ICF01012 melanoma-carrier were radiolabelled with iodine-125, and their in vivo distribution profile was determined. A radioiodination method for the conjugate 1a and its PEGylated derivatives 1b–c was developed via electrophilic iododestannylation in good radiochemical yield with excellent radiochemical purity (>99%). When administered to melanoma-bearing mice, the PEGylated conjugates exhibited an increased tumour uptake with a prolonged residence time. PEGylation also resulted in enhanced tumour selectivity compared with the non-PEGylated parent. These characteristics support further development of this model to achieve maximal concentration of anticancer therapeutics at the local site of action and minimize distribution to non-targeted sites.

Graphical abstract: PEGylation enhances the tumor selectivity of melanoma-targeted conjugates

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Supplementary files

Article information


Submitted
15 Aug 2014
Accepted
27 Oct 2014
First published
03 Nov 2014

Org. Biomol. Chem., 2015,13, 388-397
Article type
Paper
Author version available

PEGylation enhances the tumor selectivity of melanoma-targeted conjugates

M. André, S. Besse, J. Chezal and E. Mounetou, Org. Biomol. Chem., 2015, 13, 388
DOI: 10.1039/C4OB01751J

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