Abstract
Cathepsin B (CtsB) is a lysosomal cysteine proteinase that is specifically translocated to the extracellular milieu during cancer progression. The development of a lipidated CtsB inhibitor incorporated into the envelope of a liposomal nanocarrier (LNC-NS-629) is described. Ex vivo and in vivo studies confirmed selective targeting and internalization of LNC-NS-629 by tumor and stromal cells, thus validating CtsB targeting as a highly promising approach to cancer diagnosis and treatment.
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Mikhaylov, G., Klimpel, D., Schaschke, N., Mikac, U., Vizovisek, M., Fonovic, M., … Vasiljeva, O. (2014). Selective targeting of tumor and stromal cells by a nanocarrier system displaying lipidated cathepsin b inhibitor. Angewandte Chemie - International Edition, 53(38), 10077–10081. https://doi.org/10.1002/anie.201402305
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