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 viewthat proteasome inhibitionmay play amajor – yet not exclusive – role in the cytotoxic actions of gold based anticancer agents.
Selected Cytotoxic Gold Compounds cause Significant Inhibition of 20S Proteasome Catalytic Activities / Nicola Micale;Tanja Schirmeister; Roberta Ettari; Maria A. Cinellu; Laura Maiore; Maria Serratrice; Chiara Gabbiani; Lara Massai; Luigi Messori.. - In: JOURNAL OF INORGANIC BIOCHEMISTRY. - ISSN 0162-0134. - STAMPA. - 141:(2014), pp. 79-82. [10.1016/j.jinorgbio.2014.08.001]
Selected Cytotoxic Gold Compounds cause Significant Inhibition of 20S Proteasome Catalytic Activities
GABBIANI, CHIARA;MASSAI, LARA;MESSORI, LUIGI
2014
Abstract
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 viewthat proteasome inhibitionmay play amajor – yet not exclusive – role in the cytotoxic actions of gold based anticancer agents.
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