Author/Editor     Meier, Samuel M.; Kreutz, Dominique; Winter, Lilli; Klose, Matthias H. M.; Cseh, Klaudia; Weiss, Tamara; Bileck, Andrea; Alte, Beatrix; Mader, Johanna C.; Wiche, Gerhard
Title     An organoruthenium anticancer agent shows unexpected target selectivity for plectin
Type     članek
Vol. and No.     Letnik 56, št. 28
Publication year     2017
Volume     str. 8267-8271
ISSN     1433-7851 - Angewandte Chemie (International ed. in English)
Language     eng
Abstract     Organometallic metal(arene) anticancer agents require ligand exchange for their anticancer activity and this is generally believed to confer low selectivity for potential cellular targets. However, using an integrated proteomics-based target-response profiling approach as a potent hypothesisgenerating procedure, we found an unexpected target selectivity of a ruthenium(arene) pyridinecarbothioamide (plecstatin) for plectin, a scaffold protein and cytolinker, which was validated in a plectin knock-out model in vitro. Plectin targeting shows potential as a strategy to inhibit tumor invasiveness as shown in cultured tumor spheroids while oral administration of plecstatin- 1 to mice reduces tumor growth more efficiently in the invasive B16 melanoma than in the CT26 colon tumor model.
Keywords     plectin
anticancer agents
colon
plektin
sredstva proti raku
debelo črevo