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Molecules 2017, 22(4), 600; doi:10.3390/molecules22040600

Cellular Models and In Vitro Assays for the Screening of modulators of P-gp, MRP1 and BCRP

UCIBIO/REQUIMTE, Laboratório de Toxicologia, Departamento de Ciências Biológicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal
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Authors to whom correspondence should be addressed.
Academic Editor: Diego Muñoz-Torrero
Received: 30 January 2017 / Revised: 24 March 2017 / Accepted: 28 March 2017 / Published: 8 April 2017
(This article belongs to the Special Issue Can Membrane Transporters Contribute to Drug Discovery?)
View Full-Text   |   Download PDF [3051 KB, uploaded 11 April 2017]   |  

Abstract

Adenosine triphosphate (ATP)-binding cassette (ABC) transporters are highly expressed in tumor cells, as well as in organs involved in absorption and secretion processes, mediating the ATP-dependent efflux of compounds, both endogenous substances and xenobiotics, including drugs. Their expression and activity levels are modulated by the presence of inhibitors, inducers and/or activators. In vitro, ex vivo and in vivo studies with both known and newly synthesized P-glycoprotein (P-gp) inducers and/or activators have shown the usefulness of these transport mechanisms in reducing the systemic exposure and specific tissue access of potentially harmful compounds. This article focuses on the main ABC transporters involved in multidrug resistance [P-gp, multidrug resistance-associated protein 1 (MRP1) and breast cancer resistance protein (BCRP)] expressed in tissues of toxicological relevance, such as the blood-brain barrier, cardiovascular system, liver, kidney and intestine. Moreover, it provides a review of the available cellular models, in vitro and ex vivo assays for the screening and selection of safe and specific inducers and activators of these membrane transporters. The available cellular models and in vitro assays have been proposed as high throughput and low-cost alternatives to excessive animal testing, allowing the evaluation of a large number of compounds. View Full-Text
Keywords: inducers; activators; ATP-binding cassette transporters; cellular models; membrane assays; cell-based assays; in vitro assays; P-glycoprotein; multidrug resistance-associated protein 1; breast cancer resistance protein inducers; activators; ATP-binding cassette transporters; cellular models; membrane assays; cell-based assays; in vitro assays; P-glycoprotein; multidrug resistance-associated protein 1; breast cancer resistance protein
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Gameiro, M.; Silva, R.; Rocha-Pereira, C.; Carmo, H.; Carvalho, F.; Bastos, M.L.; Remião, F. Cellular Models and In Vitro Assays for the Screening of modulators of P-gp, MRP1 and BCRP. Molecules 2017, 22, 600.

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