Structural and molecular characterization of lopinavir and ivermectin as breast cancer resistance protein (BCRP/ABCG2) inhibitors
Abstract: A current clinical challenge in cancer is multidrug resistance (MDR) mediated by ABC transporters. Breast cancer resistance protein (BCRP) or ABCG2 transporter is one of the most important ABC transporters implicated in MDR and the use of inhibitors is a promising approach to overcome the resistance in cancer. This study aimed to characterize the molecular mechanism of ABCG2 inhibitors identified by a repurposing drug strategy using antiviral, anti-inflammatory and antiparasitic agents. Lopinavir and ivermectin can be considered as pan-inhibitors of ABC transporters, since both compounds inhibited ABCG2, P-glycoprotein and MRP1. They inhibited ABCG2 activity showing IC50 values of 25.5 and 23.4 µM, respectively. These drugs were highly cytotoxic and not transported by ABCG2. Additionally, these drugs increased the 5D3 antibody binding and did not affect the mRNA and protein expression levels. Cell-based analysis of the type of inhibition suggested a non-competitive inhibition, whic.... https://www.excli.de/excli/article/view/6427
- Location
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Deutsche Nationalbibliothek Frankfurt am Main
- Extent
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Online-Ressource
- Language
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Englisch
- Bibliographic citation
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Structural and molecular characterization of lopinavir and ivermectin as breast cancer resistance protein (BCRP/ABCG2) inhibitors ; volume:22 ; year:2023
EXCLI journal ; 22 (2023)
- Creator
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Dutra, Julia de Paula
Scheiffer, Gustavo
Kronenberger, Thales
Gomes, Lucas Julian Cruz
Zanzarini, Isadora
dos Santos, Kelly Karoline
Tonduru, Arun K.
Poso, Antti
Rego, Fabiane Gomes de Moraes
Picheth, Geraldo
Valdameri, Glaucio
Rotuno Moure, Vivian
- DOI
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10.17179/excli2023-6427
- URN
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urn:nbn:de:101:1-2502171611431.885218569366
- Rights
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Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Last update
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15.08.2025, 7:22 AM CEST
Data provider
Deutsche Nationalbibliothek. If you have any questions about the object, please contact the data provider.
Associated
- Dutra, Julia de Paula
- Scheiffer, Gustavo
- Kronenberger, Thales
- Gomes, Lucas Julian Cruz
- Zanzarini, Isadora
- dos Santos, Kelly Karoline
- Tonduru, Arun K.
- Poso, Antti
- Rego, Fabiane Gomes de Moraes
- Picheth, Geraldo
- Valdameri, Glaucio
- Rotuno Moure, Vivian
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