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Lysine‐specific demethylase 5A (KDM5A) has recently become a promising target for epigenetic therapy. In this study, we designed and synthesized metal complexes bearing ligands with reported demethylase and p27 modulating activities. The Rh(III) complex 1 was identified as a direct, selective and potent inhibitor of KDM5A that directly abrogate KDM5A demethylase activity via antagonizing the KDM5A‐tri‐/di‐methylated...
Ein Rhodium(III)‐basierter Inhibitor von Lysin‐spezifischer Demethylase‐5A wurde entwickelt. In ihrer Zuschrift auf S. 13275 berichten V. K. W. Wong, D. L. Ma, C.‐H. Leung et al. über diesen Rhodium(III)‐Komplex, der Antitumoraktivität in einem Mausmodell von tripel‐negativem Brustkrebs zeigt, einer besonders schwierig zu behandelnden Brustkrebsform. Der Komplex könnte als neuartiges Strukturgerüst...
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