Sucralose Promotes Benzo(a)Pyrene-Induced Renal Toxicity in Mice by Regulating P-glycoprotein. [PDF]
Hu J +7 more
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Enhanced plasma and brain concentrations and medulloblastoma cytotoxicity of asciminib and nilotinib by P-glycoprotein inhibition with tariquidar. [PDF]
Thompson EM, Cheng L, Spasojevic I.
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Autotaxin regulates the expression and the activity of P-glycoprotein in lipopolysaccharide -activated microglial cells. [PDF]
Fayyad-Kazan M +4 more
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P-Glycoprotein Drives Glioblastoma Survival and Chemotherapy Resistance: Potential as a Promising Liquid Biopsy Biomarker. [PDF]
Pilotto Heming C +6 more
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Multidrug resistance (MDR) is defined by the simultaneous acquisition of cellular resistance to a broad range of cytotoxic compounds bearing little or no structural and functional homologies [1–5]. MDR is caused in cultured cells in vitro [6–9] and in tumor cells in vivo [10–12] by the overexpression of P-glycoprotein (Pgp) (reviewed in [13]).
E, Buschman, P, Lepage, P, Gros
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Functional intracellular P‐glycoprotein
International Journal of Cancer, 1998Efflux of chemotherapy drugs by P-glycoprotein (P-gp) at the plasma membrane is thought to be a major cause of cancer multidrug resistance. In this report, we show by flow cytometry that P-gp also concentrates large amounts of 2 different drugs, Hoechst 33342 and daunorubicin, within a cytoplasmic compartment of multidrug resistant CHRC5 cells.
A B, Shapiro +4 more
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Original Vinca Derivatives: From P-Glycoprotein Substrates to P-Glycoprotein Inhibitors
Journal of Medicinal Chemistry, 2016The first example of vinca derivatives 16-18 able to modulate P-glycoprotein (Pgp) efflux activity is reported. They were elaborated in two steps from vinorelbine 3 (VLN) by a modification of the velbenamine moiety. These compounds were able to decrease efficiently Pgp mediated influx and efflux of rhodamine-123 (Rho) and to restore the cytotoxicity of
Olga, Gherbovet +3 more
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P-glycoprotein and multidrug resistance
Current Opinion in Genetics & Development, 1996Although the phenomenon of simultaneous resistance to multiple cytotoxic drugs (multidrug resistance) in cancer cells has been discussed for more than two decades, and the human and mouse genes encoding an energy-dependent transporter (the multidrug transporter or P-glycoprotein) responsible for multidrug resistance were cloned 10 years ago, there is ...
M M, Gottesman, I, Pastan, S V, Ambudkar
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Photoaffinity substrates for P-glycoprotein
Biochemical Pharmacology, 1992A variety of compounds can inhibit the function of P-glycoprotein (Pgp) by binding to it and preventing the efflux of anticancer drug substrates. While the molecular architecture of the drug binding site(s) in Pgp is not known, it is clear that modulators in general appear to conform to some general physical-chemical rules.
W T, Beck, X D, Qian
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The P-glycoprotein multidrug transporter
General Pharmacology: The Vascular System, 19961. P-glycoprotein (P-gp) is a transmembrane protein involved in ATP-dependent efflux of various structurally unrelated anticancer drugs. Its overexpression in cancer cells decreases intracellular drug concentrations and, thus, confers a multidrug resistance phenotype. 2.
O, Fardel, V, Lecureur, A, Guillouzo
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