Publikation
Probing the potential of platinum(II) complexes for the inhibition of thiol-dependent enzymatic activity
Wissenschaftlicher Artikel/Review - 01.06.2005
van Zutphen Steven, Kraus Marianne, Driessen Christoph, van der Marel Gijs A, Overkleeft Herman S, Reedijk Jan
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The synthesis and biological evaluation of platinum(II) amine complexes designed to act as inhibitors of the human cysteine protease cathepsin B, a thiol-dependent enzyme, is described. The complexes, composed of a cathepsin targeting ligand and a platinum(II) moiety with varying degrees of reactivity towards nucleophiles were characterized by physical-analytical methods and a proof of principle was illustrated in a model reaction. In biological tests for inhibitory activity against cathepsin B the presented compounds did not show significant inhibitory activity.