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

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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DOI: 10.1016/j.jinorgbio.2014.08.001

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.

Item Type:Article
ID Code:10516
Status:Published
Refereed:Yes
Uncontrolled Keywords:Proteasome, gold compounds, anticancer drugs, enzyme inhibition
Subjects:Area 03 - Scienze chimiche > CHIM/03 Chimica generale e inorganica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Elsevier Science
ISSN:0162-0134
Deposited On:03 Dec 2014 13:35

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