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

Publikationstyp:
Zeitschriftenaufsatz
Metadaten:
Autoren
  • Nicola Micale
  • Maria Agostina Cinellu
  • Laura Maiore
  • Anna Rosa Sannella
  • Carlo Severini
  • Tanja Schirmeister
  • Chiara Gabbiani
  • Luigi Messori
Autoren-URL
https://www.webofscience.com/api/gateway?GWVersion=2&SrcApp=fis-test-1&SrcAuth=WosAPI&KeyUT=WOS:000297904900007&DestLinkType=FullRecord&DestApp=WOS_CPL
DOI
10.1016/j.jinorgbio.2011.09.006
eISSN
1873-3344
Externe Identifier
  • Clarivate Analytics Document Solution ID: 859VW
  • PubMed Identifier: 22071081
ISSN
0162-0134
Ausgabe der Veröffentlichung
12
Zeitschrift
JOURNAL OF INORGANIC BIOCHEMISTRY
Schlüsselwörter
  • Gold compounds
  • Metallodrugs
  • Malaria
  • Falcipain 2
Paginierung
1576 - 1579
Datum der Veröffentlichung
2011
Status
Published
Titel
Selected gold compounds cause pronounced inhibition of Falcipain 2 and effectively block <i>P</i>. <i>falciparum</i> growth <i>in vitro</i>
Sub types
  • Article
Ausgabe der Zeitschrift
105

Datenquelle: Web of Science (Lite)

Andere Metadatenquellen:
Autoren
  • Nicola Micale
  • Maria Agostina Cinellu
  • Laura Maiore
  • Anna Rosa Sannella
  • Carlo Severini
  • Tanja Schirmeister
  • Chiara Gabbiani
  • Luigi Messori
DOI
10.1016/j.jinorgbio.2011.09.006
ISSN
0162-0134
Ausgabe der Veröffentlichung
12
Zeitschrift
Journal of Inorganic Biochemistry
Sprache
en
Paginierung
1576 - 1579
Datum der Veröffentlichung
2011
Status
Published
Herausgeber
Elsevier BV
Herausgeber URL
http://dx.doi.org/10.1016/j.jinorgbio.2011.09.006
Datum der Datenerfassung
2021
Titel
Selected gold compounds cause pronounced inhibition of Falcipain 2 and effectively block P. falciparum growth in vitro
Ausgabe der Zeitschrift
105

Datenquelle: Crossref

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 K(i) 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.
Addresses
  • Department of Medicinal Chemistry, University of Messina, Messina, Italy. nmicale@unime.it
Autoren
  • Nicola Micale
  • Maria Agostina Cinellu
  • Laura Maiore
  • Anna Rosa Sannella
  • Carlo Severini
  • Tanja Schirmeister
  • Chiara Gabbiani
  • Luigi Messori
DOI
10.1016/j.jinorgbio.2011.09.006
eISSN
1873-3344
Externe Identifier
  • PubMed Identifier: 22071081
Funding acknowledgements
  • Regione Autonoma della Sardegna:
  • Università degli Studi di Sassari:
  • Beneficentia Stiftung:
  • Fondazione Banco di Sardegna:
Open access
false
ISSN
0162-0134
Ausgabe der Veröffentlichung
12
Zeitschrift
Journal of inorganic biochemistry
Schlüsselwörter
  • Plasmodium falciparum
  • Gold
  • Cysteine Endopeptidases
  • Cysteine Proteinase Inhibitors
  • Antimalarials
  • Culture Techniques
  • Inhibitory Concentration 50
  • Coordination Complexes
Sprache
eng
Medium
Print-Electronic
Online publication date
2011
Paginierung
1576 - 1579
Datum der Veröffentlichung
2011
Status
Published
Datum der Datenerfassung
2011
Titel
Selected gold compounds cause pronounced inhibition of Falcipain 2 and effectively block P. falciparum growth in vitro.
Sub types
  • Research Support, Non-U.S. Gov't
  • Journal Article
Ausgabe der Zeitschrift
105

Datenquelle: Europe PubMed Central

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 K(i) 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.
Date of acceptance
2011
Autoren
  • Nicola Micale
  • Maria Agostina Cinellu
  • Laura Maiore
  • Anna Rosa Sannella
  • Carlo Severini
  • Tanja Schirmeister
  • Chiara Gabbiani
  • Luigi Messori
Autoren-URL
https://www.ncbi.nlm.nih.gov/pubmed/22071081
DOI
10.1016/j.jinorgbio.2011.09.006
eISSN
1873-3344
Ausgabe der Veröffentlichung
12
Zeitschrift
J Inorg Biochem
Schlüsselwörter
  • Antimalarials
  • Coordination Complexes
  • Culture Techniques
  • Cysteine Endopeptidases
  • Cysteine Proteinase Inhibitors
  • Gold
  • Inhibitory Concentration 50
  • Plasmodium falciparum
Sprache
eng
Country
United States
Paginierung
1576 - 1579
PII
S0162-0134(11)00249-2
Datum der Veröffentlichung
2011
Status
Published
Datum, an dem der Datensatz öffentlich gemacht wurde
2012
Titel
Selected gold compounds cause pronounced inhibition of Falcipain 2 and effectively block P. falciparum growth in vitro.
Sub types
  • Journal Article
  • Research Support, Non-U.S. Gov't
Ausgabe der Zeitschrift
105

Datenquelle: PubMed

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