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Publications à Abstracts |
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Development of protein-binding bifunctional
linkers for a new generation of dual-acting prodrugs Khalid
Abu Ajaj, Martin Biniossek, Felix Kratz Bioconjugate Chemistry, 2009, 20 (2), 390–396 Keywords:
combination chemotherapy; albumin-binding prodrug;
albumin; cathepsin B; 1,6-self-immolative spacer;
doxorubicin; paclitaxel Abstract: The aim of this work was to develop a new bifunctional maleimide linker
for the development of dual-acting prodrugs
that incorporate two different pharmaceutically anticancer agents
independently bound by enzymatically cleavable
substrates. The linker consists of a carboxyl group in one arm and an
activated 1,6-self-immolative para-aminobenzyloxycarbonyl
spacer together with a cathepsin B cleavable dipeptide Phe-Lys in the other.
Aided with this linker, we have prepared a thiol-binding
prodrug that contains the anticancer drugs
doxorubicin and paclitaxel. Bound to the
cysteine-34 position of albumin, it was cleaved efficiently by cathepsin B releasing the free drugs. |
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