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Publications à Abstracts |
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Development
of dual-acting prodrugs for circumventing multidrug
resistance Khalid
Abu Ajaj, Felix Kratz Bioorganic Medicinal Chemistry Letters, 2009, 19 (3), 995–1000 Keywords:
multidrug resistance; albumin-binding prodrug;
doxorubicin Abstract: We have developed a novel dual-acting maleimide-bearing prodrug that
incorporates the anticancer agent doxorubicin and an inhibitor of the
P-glycoprotein efflux pump that is over-expressed in multidrug resistant
tumor cells. Additionally, the prodrug contains a 1,6-self-immolative spacer coupled to the dipeptide Phe-Lys that acts as
a substrate for cathepsin B. The prodrug, once bound through its maleimide
moiety to the cysteine-34 group of human serum albumin, was cleaved by cathepsin B and in tumor homogenates demonstrating a
release of the anticancer agent doxorubicin and the inhibitor. |
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