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Selected gold compounds cause pronounced inhibition of Falcipain 2 and effectively block P. falciparum growth in vitro

Micale, Nicola and Cinellu, Maria Agostina and Maiore, Laura and Sannella, Anna Rosa and Severini, Carlo and Schirmeister, Tanja and Gabbiani, Chiara and Messori, Luigi (2011) Selected gold compounds cause pronounced inhibition of Falcipain 2 and effectively block P. falciparum growth in vitro. Journal of Inorganic Biochemistry, Vol. 105 (12), p. 1576-1579. eISSN 1873-3344. Article.

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DOI: 10.1016/j.jinorgbio.2011.09.006

Abstract

A number of structurally diverse gold compounds were evaluated as possible inhibitors of Falcipain 2 (Fp2), a cysteine protease from P. falciparum that is a validated target for the development of novel antimalarial drugs. Remarkably, most tested compounds caused pronounced but reversible inhibition of Fp2 with Ki values falling in the micromolar range. Enzyme inhibition is basically ascribed to gold binding to catalytic active site cysteine. The same gold compounds were then tested for their ability to inhibit P. falciparum growth in vitro; important parasite growth inhibition was indeed observed. However, careful analysis of the two sets of data failed to establish any direct correlation between enzyme inhibition and reduction of P. falciparum growth suggesting that Fp2 inhibition represents just one of the various mechanisms through which gold compounds effectively antagonize P. falciparum replication.

Item Type:Article
ID Code:7275
Status:Published
Refereed:Yes
Uncontrolled Keywords:Gold compounds, metallodrugs, malaria, Falcipain 2
Subjects:Area 03 - Scienze chimiche > CHIM/03 Chimica generale e inorganica
Divisions:001 Università di Sassari > 01 Dipartimenti > Chimica
Publisher:Elsevier Science
eISSN:1873-3344
Deposited On:21 Mar 2012 17:14

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