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The aquaporin-3-inhibiting potential of polyoxotungstates

2020Journal article Open access
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dc.contributor.authorPimpão, Catarina
dc.contributor.authorda Silva, Inês V.
dc.contributor.authorMósca, Andreia F.
dc.contributor.authorPinho, Jacinta O.
dc.contributor.authorGaspar, Maria Manuela
dc.contributor.authorGumerova, Nadiia I.
dc.contributor.authorRompel, Annette
dc.contributor.authorAureliano, Manuel
dc.contributor.authorSoveral, Graça
dc.date.accessioned2020-06-15T15:29:07Z
dc.date.available2020-06-15T15:29:07Z
dc.date.issued2020
dc.description.abstractPolyoxometalates (POMs) are of increasing interest due to their proven anticancer activities. Aquaporins (AQPs) were found to be overexpressed in tumors bringing particular attention to their inhibitors as anticancer drugs. Herein, we report for the first time the ability of polyoxotungstates (POTs), such as of Wells-Dawson P2W18, P2W12, and P2W15, and Preyssler P5W30 structures, to affect aquaporin-3 (AQP3) activity and impair melanoma cell migration. The tested POTs were revealed to inhibit AQP3 function with different effects, with P2W18, P2W12, and P5W30 being the most potent (50% inhibitory concentration (IC50) = 0.8, 2.8, and 3.2 µM), and P2W15 being the weakest (IC50 > 100 µM). The selectivity of P2W18 toward AQP3 was confirmed in yeast cells transformed with human aquaglyceroporins. The effect of P2W12 and P2W18 on melanoma cells that highly express AQP3 revealed an impairment of cell migration between 55% and 65% after 24 h, indicating that the anticancer properties of these compounds may in part be due to the blockage of AQP3-mediated permeability. Altogether, our data revealed that P2W18 strongly affects AQP3 activity and cancer cell growth, unveiling its potential as an anticancer drug against tumors where AQP3 is highly expressed.pt_PT
dc.description.sponsorshipFundação para a Ciência e a Tecnologia (FCT) (PTDC/BTM-SAL/28977/2017, PTDC/MED-QUI/31721/2017, UID/DTP/04138/2019, UIDB/04326/2020, SFRH/BD/117586/2016. Austrian Science Fund (FWF) P27534, M2203pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.doi10.3390/ijms21072467pt_PT
dc.identifier.issn1661-6596
dc.identifier.urihttp://hdl.handle.net/10400.1/14013
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherMDPIpt_PT
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/pt_PT
dc.subjectAquaporinpt_PT
dc.subjectAquaglyceroporinpt_PT
dc.subjectInhibitorspt_PT
dc.subjectGlycerolpt_PT
dc.subjectCancerpt_PT
dc.subjectPolyoxotungstatespt_PT
dc.subjectMelanomapt_PT
dc.titleThe aquaporin-3-inhibiting potential of polyoxotungstatespt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.issue7pt_PT
oaire.citation.startPage2467pt_PT
oaire.citation.titleInternational Journal of Molecular Sciencespt_PT
oaire.citation.volume21pt_PT
person.familyNameAureliano
person.givenNameManuel
person.identifier584146
person.identifier.ciencia-idAA14-3490-DC5E
person.identifier.orcid0000-0003-4858-3201
person.identifier.ridI-3283-2012
person.identifier.scopus-author-id6603412860
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublicationbb413661-7edd-4b57-8338-33889cfd05db
relation.isAuthorOfPublication.latestForDiscoverybb413661-7edd-4b57-8338-33889cfd05db

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