P-Glycoprotein: One Mechanism, Many Tasks and the Consequences for Pharmacotherapy of Cancers

Seelig, Anna. (2020) P-Glycoprotein: One Mechanism, Many Tasks and the Consequences for Pharmacotherapy of Cancers. Frontiers in Oncology, 10. p. 576559.

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P-glycoprotein or multidrug resistance protein (MDR1) is an adenosine triphosphate (ATP)binding cassette transporter (ABCB1) intensely investigated because it is an obstacle tosuccessful pharmacotherapy of cancers. P-glycoprotein prevents cellular uptake of alarge number of structurally and functionally diverse compounds, including most cancertherapeutics and in this way causes multidrug resistance (MDR). To overcome MDR,and thus improve cancer treatment, an understanding of P-glycoprotein inhibition at themolecular level is required. With this goal in mind, we propose rules that predict whether acompound is a modulator, substrate, inhibitor, or inducer of P-glycoprotein. This new setof rules is derived from a quantitative analysis of the drug binding and transport propertiesof P-glycoprotein. We further discuss the role of P-glycoprotein in immune surveillanceand cell metabolism. Finally, the predictive power of the proposed rules is demonstratedwith a set of FDA approved drugs which have been repurposed for cancer therapy.
Faculties and Departments:05 Faculty of Science > Departement Biozentrum > Former Organization Units Biozentrum > Biophysical Chemistry (Seelig A)
UniBasel Contributors:Seelig-Löffler, Anna
Item Type:Article, refereed
Article Subtype:Research Article
Publisher:Frontiers Media
Note:Publication type according to Uni Basel Research Database: Journal article
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Last Modified:17 Nov 2020 11:18
Deposited On:17 Nov 2020 11:18

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