A self-immolative dendritic glucuronide prodrug of doxorubicin
2011; Royal Society of Chemistry; Volume: 3; Issue: 1 Linguagem: Inglês
10.1039/c1md00193k
ISSN2040-2511
AutoresMarion Grinda, Jonathan Clarhaut, Brigitte Renoux, Isabelle Tranoy‐Opalinski, Sébastien Papot,
Tópico(s)Glycosylation and Glycoproteins Research
ResumoThe first self-immolative dendritic glucuronide prodrug of doxorubicin was studied with the aim to target β-glucuronidase overexpressed in the microenvironment of numerous tumors. This compound includes a chemical amplifier programmed to release two molecules of doxorubicin after a single enzymatic activation step. Upon β-glucuronidase activation, the dendritic prodrug was twice more toxic than its monomeric counterpart against H661 lung cancer cells.
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