Probing the potential of platinum(II) complexes for the inhibition of thiol-dependent enzymatic activity

Publication

Probing the potential of platinum(II) complexes for the inhibition of thiol-dependent enzymatic activity

Journal Paper/Review - Jun 1, 2005

van Zutphen Steven, Kraus Marianne, Driessen Christoph, van der Marel Gijs A, Overkleeft Herman S, Reedijk Jan

Citation

van Zutphen S, Kraus M, Driessen C, van der Marel G, Overkleeft H, Reedijk J. Probing the potential of platinum(II) complexes for the inhibition of thiol-dependent enzymatic activity. Journal of inorganic biochemistry 2005; 99:1384-9.

Type

Journal Paper/Review (English)

Journal

Journal of inorganic biochemistry 2005; 99

Publication Date

Jun 1, 2005

Issn Print

0162-0134

Pages

1384-9

Brief description/objective

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.