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.

Selected cytotoxic gold compounds cause significant inhibition of 20S proteasome catalytic activities

GABBIANI, CHIARA;
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 view that proteasome inhibition may play a major - yet not exclusive - role in the cytotoxic actions of gold based anticancer agents.
Micale, N.; Schirmeister, T.; Ettari, R.; Cinellu, M. A.; Maiore, L.; Serratrice, M.; Gabbiani, Chiara; Massai, L.; Messori, L.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11568/559467
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