Micale, Nicola and Schirmeister, Tanja and Ettari, Roberta and Cinellu, Maria Agostina and Maiore, Laura and Serratrice, Maria and Gabbiani, Chiara and Massai, Lara and Messori, Luigi (2014) Selected cytotoxic gold compounds cause significant inhibition of 20S proteasome catalytic activities. Journal of Inorganic Biochemistry, Vol. 141 , p. 79-82. ISSN 0162-0134. Article.
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Six structurally diverse cytotoxic gold compounds are reported to cause profound and differential inhibition of the three main catalytic activities of purified 20S proteasome whilst auranofin, an established gold(I) drug in clinical use, is nearly ineffective. In particular, the gold(I) complex [(pbiH)Au(PPh3)]PF6, turns out to be the most potent inhibitor of all three enzyme activities with sub-micromolar IC50 values. The present results further support the view that proteasome inhibition may play a major – yet not exclusive – role in the cytotoxic actions of gold based anticancer agents.
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