Titel
The Aquaporin-3-Inhibiting Potential of Polyoxotungstates
Autor*in
Catarina Pimpão
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa
Inês V. da Silva
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa
Andreia F. Mósca
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa
... show all
Abstract
Polyoxometalates (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.
Stichwort
Physical and Theoretical ChemistryInorganic ChemistryOrganic ChemistrySpectroscopyMolecular BiologyCatalysisGeneral MedicineComputer Science Applications
Objekt-Typ
Sprache
Englisch [eng]
Persistent identifier
phaidra.univie.ac.at/o:1224734
Erschienen in
Titel
International Journal of Molecular Sciences
Band
21
Ausgabe
7
ISSN
1422-0067
Erscheinungsdatum
2020
Publication
MDPI AG
Fördergeber
Austrian Science Fund (FWF) — P27534
Austrian Science Fund (FWF) — M2203
Erscheinungsdatum
2020
Zugänglichkeit
Rechte
Rechteangabe
© 2020 by the authors
Universität Wien | Universitätsring 1 | 1010 Wien | T
+43-1-4277-0