Work

The “specific” P-glycoprotein inhibitor zosuquidar (LY335979) also weakly inhibits human organic cation transporters

Year: 2024

Type: article

Abstract: Zosuquidar (LY335979) is a widely used experimental P-glycoprotein (P-gp) inhibitor, which is commended as very potent but also as very specific for P-gp. In this in vitro and in silico study, we demonstrated for the first time that zosuquidar also inhibits organic cation transporters (OCT) 1-3, albeit less potently than P-gp. This still has to be kept in mind when zosuquidar is used to inhibit cellular efflux of P-gp substrates that are concurrently transported into the cells by OCTs. To avoid interference in these assays, zosuquidar concentrations should be kept below 1 µM.

Source: Naunyn-Schmiedeberg s Archives of Pharmacology

DOI: 10.1007/s00210-024-03743-y

Authors: Gzona Bajraktari-Sylejmani, Rajamanikkam Kamaraj, Dirk Theile, Petr Pávek, Johanna Weiss

Institutions: Heidelberg University, University Hospital Heidelberg, Charles University

Language: English

Topic: Drug Transport and Resistance Mechanisms

Subfield: Oncology

Field: Medicine

Domain: Health Sciences

SDG: Good health and well-being

Open Access status: hybrid

Estimated APC paid: $4,590