Imatinib-ULS-lysozyme: a proximal tubular cell-targeted conjugate of imatinib for the treatment of renal diseases.

@article{Dolman2012ImatinibULSlysozymeAP,
  title={Imatinib-ULS-lysozyme: a proximal tubular cell-targeted conjugate of imatinib for the treatment of renal diseases.},
  author={M. Emmy M. Dolman and K. M. A. van Dorenmalen and Ebel H. E. Pieters and Marie Lacombe and J{\'a}nos Pat{\'o} and Gert Storm and Wim E Hennink and Robbert Jan Kok},
  journal={Journal of controlled release : official journal of the Controlled Release Society},
  year={2012},
  volume={157 3},
  pages={461-8}
}
The anticancer drug imatinib is an inhibitor of the platelet-derived growth factor receptor (PDGFR) kinases, which are involved in the pathogenesis of fibrotic diseases. In the current study we investigated the delivery of imatinib to the proximal tubular cells of the kidneys and evaluated the potential antifibrotic effects of imatinib in tubulointerstitial fibrosis. Coupling of imatinib to the low molecular weight protein lysozyme via the platinum (II)-based linker ULS yielded a 0.8:1 drug… CONTINUE READING

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