Modulation of P-glycoprotein efflux pump: induction and activation as a therapeutic strategy

R Silva, V Vilas-Boas, H Carmo… - Pharmacology & …, 2015‏ - Elsevier
Abstract P-glycoprotein (P-gp) is an ATP-dependent efflux pump encoded by the MDR1
gene in humans, known to mediate multidrug resistance of neoplastic cells to cancer …

[HTML][HTML] Cellular models and in vitro assays for the screening of modulators of P-gp, MRP1 and BCRP

M Gameiro, R Silva, C Rocha-Pereira, H Carmo… - Molecules, 2017‏ - mdpi.com
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 …

[HTML][HTML] Study models of drug–drug interactions involving p-glycoprotein: the potential benefit of p-glycoprotein modulation at the kidney and intestinal levels

J Veiga-Matos, AI Morales, M Prieto, F Remião, R Silva - Molecules, 2023‏ - mdpi.com
P-glycoprotein (P-gp) is a crucial membrane transporter situated on the cell's apical surface,
being responsible for eliminating xenobiotics and endobiotics. P-gp modulators are …

Interactions of pesticides with membrane drug transporters: implications for toxicokinetics and toxicity

L Chedik, A Bruyere, A Bacle, S Potin… - Expert opinion on …, 2018‏ - Taylor & Francis
Introduction: Drug transporters are now recognized as major actors of pharmacokinetics.
They are also likely implicated in toxicokinetics and toxicology of environmental pollutants …

P-glycoprotein induction in Caco-2 cells by newly synthetized thioxanthones prevents paraquat cytotoxicity

R Silva, A Palmeira, H Carmo, DJ Barbosa… - Archives of …, 2015‏ - Springer
The induction of P-glycoprotein (P-gp), an ATP-dependent efflux pump, has been proposed
as a strategy against the toxicity induced by P-gp substrates such as the herbicide paraquat …

Rifampin regulation of drug transporters gene expression and the association of microRNAs in human hepatocytes

EA Benson, MT Eadon, Z Desta, Y Liu, H Lin… - Frontiers in …, 2016‏ - frontiersin.org
Membrane drug transporters contribute to the disposition of many drugs. In human liver,
drug transport is controlled by two main superfamilies of transporters, the solute carrier …

Xanthones as P-glycoprotein modulators and their impact on drug bioavailability

V Silva, E Gil-Martins, B Silva… - Expert Opinion on …, 2021‏ - Taylor & Francis
ABSTRACT Introduction: P-glycoprotein (P-gp) is an important efflux pump responsible for
the extruding of many endogenous and exogenous substances out of the cells. P-gp can be …

Induction and activation of P-glycoprotein by dihydroxylated xanthones protect against the cytotoxicity of the P-glycoprotein substrate paraquat

R Silva, E Sousa, H Carmo, A Palmeira… - Archives of …, 2014‏ - Springer
Xanthones are a family of compounds with several known biological activities and
therapeutic potential for which information on their interaction with membrane transporters is …

Organic anion-transporting polypeptide genes are not induced by the pregnane X receptor activator rifampin: studies in hepatocytes in vitro and in monkeys in vivo

C Niu, Y Wang, X Zhao, S Tep, E Murakami… - Drug Metabolism and …, 2019‏ - Elsevier
Induction potentials of the pregnane X receptor (PXR) activator rifampin (RIF) on transporter
genes [eg, organic anion-transporting polypeptides (OATPs)] are still in its infancy or remain …

[HTML][HTML] Cardiac PET imaging of ATP binding cassette (ABC) transporters: opportunities and challenges

W Liu, P Mossel, V Schwach, RHJA Slart, G Luurtsema - Pharmaceuticals, 2023‏ - mdpi.com
Adenosine triphosphate binding cassette (ABC) transporters are a broad family of
membrane protein complexes that use energy to transport molecules across cells and/or …