Journal
MACROMOLECULAR BIOSCIENCE
Volume 12, Issue 1, Pages 93-103Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/mabi.201100277
Keywords
dendrimers; drug delivery systems; kidney; platinum linkers; sunitinib
Funding
- European Framework program FP6 [LSHB-CT-2007-036644]
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The development of a macromolecular conjugate of a multitargeted tyrosine kinase inhibitor is described that can be used for renal-specific delivery into proximal tubular cells. A novel sunitinib analogue, that is, 17864, is conjugated to a NH2-PAMAM-G3 dendrimer via the platinum (II)-based Universal Linkage System (ULS (TM)). The activity of 17864 is retained after coordination to the ULS linker alone or when coupled to NH2-PAMAM-G3. 17864-UlS-NH2-PAMAM-G3 is non-toxic to proximal tubular cells in vitro. After intravenous administration to mice, 17864-UlS-NH2-PAMAM-G3 rapidly and efficiently accumulates in the kidneys. These results are encouraging for future studies focusing on the development of novel therapeutics for the treatment of renal diseases.
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