Avtor/Urednik | Meier, Samuel M.; Kreutz, Dominique; Winter, Lilli; Klose, Matthias H. M.; Cseh, Klaudia; Weiss, Tamara; Bileck, Andrea; Alte, Beatrix; Mader, Johanna C.; Wiche, Gerhard | |
Naslov | An organoruthenium anticancer agent shows unexpected target selectivity for plectin | |
Tip | članek | |
Vol. in št. | Letnik 56, št. 28 | |
Leto izdaje | 2017 | |
Obseg | str. 8267-8271 | |
ISSN | 1433-7851 - Angewandte Chemie (International ed. in English) | |
Jezik | eng | |
Abstrakt | 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. | |
Proste vsebinske oznake | plectin anticancer agents colon plektin sredstva proti raku debelo črevo |