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The Ca2+-ATPase inhibition potential of gold (I, III) compounds

2020Journal article Open access
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dc.contributor.authorFonseca, Custódia
dc.contributor.authorFraqueza, Gil
dc.contributor.authorCarabineiro, Sónia A.
dc.contributor.authorAureliano, Manuel
dc.date.accessioned2020-11-03T10:58:42Z
dc.date.available2020-11-03T10:58:42Z
dc.date.issued2020
dc.description.abstractThe therapeutic applications of gold are well-known for many centuries. The most used gold compounds contain Au(I). Herein, we report, for the first time, the ability of four Au(I) and Au(III) complexes, namely dichloro (2-pyridinecarboxylate) Au(III) (abbreviated as1), chlorotrimethylphosphine Au(I) (2), 1,3-bis(2,6-diisopropylphenyl) imidazole-2-ylidene Au(I) chloride (3), and chlorotriphenylphosphine Au(I) (4), to affect the sarcoplasmic reticulum (SR) Ca2+-ATPase activity. The tested gold compounds strongly inhibit the Ca2+-ATPase activity with different effects, being Au(I) compounds2and4the strongest, with half maximal inhibitory concentration (IC50) values of 0.8 and 0.9 mu M, respectively. For Au(III) compound1and Au(I) compound3, higher IC(50)values are found (4.5 mu M and 16.3 mu M, respectively). The type of enzymatic inhibition is also different, with gold compounds1and2showing a non-competitive inhibition regarding the native substrate MgATP, whereas for Au compounds3and4, a mixed type of inhibition is observed. Our data reveal, for the first time, Au(I) compounds with powerful inhibitory capacity towards SR Ca(2+)ATPase function. These results also show, unprecedently, that Au (III) and Au(I) compounds can act as P-type ATPase inhibitors, unveiling a potential application of these complexes.pt_PT
dc.description.sponsorshipFCT: UIDB/04326/2020/ UIDB/50006/2020pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.doi10.3390/inorganics8090049pt_PT
dc.identifier.urihttp://hdl.handle.net/10400.1/14806
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectGold(I, III) compoundspt_PT
dc.subjectCa2+-ATPasept_PT
dc.subjectAnticancerpt_PT
dc.subjectP-type ATPases inhibitorspt_PT
dc.titleThe Ca2+-ATPase inhibition potential of gold (I, III) compoundspt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.issue9pt_PT
oaire.citation.startPage49pt_PT
oaire.citation.titleInorganicspt_PT
oaire.citation.volume8pt_PT
person.familyNameFonseca
person.familyNameFraqueza
person.familyNameAureliano
person.givenNameCustódia
person.givenNameGil
person.givenNameManuel
person.identifier1179689
person.identifier584146
person.identifier.ciencia-id601F-8F41-D5E4
person.identifier.ciencia-id1317-C7C9-5BDA
person.identifier.ciencia-idAA14-3490-DC5E
person.identifier.orcid0000-0002-2480-3364
person.identifier.orcid0000-0003-2969-9292
person.identifier.orcid0000-0003-4858-3201
person.identifier.ridA-3552-2013
person.identifier.ridI-3283-2012
person.identifier.scopus-author-id54683851800
person.identifier.scopus-author-id6603412860
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublication30b7964c-964a-4ed0-bb05-594361e50df7
relation.isAuthorOfPublication9e7ef53d-b79c-4446-9093-0611980e6ecd
relation.isAuthorOfPublicationbb413661-7edd-4b57-8338-33889cfd05db
relation.isAuthorOfPublication.latestForDiscoverybb413661-7edd-4b57-8338-33889cfd05db

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