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1994
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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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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P-Glycoprotein and Multidrug Resistance
New England Journal of Medicine, 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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Parasitology Today, 1994
The P-glycoprotein (Pgp), a member of a group of integral membrane proteins that contain the ATP-binding cassette, is widely represented in the animal kingdom. A family of Pgp homologues has recently been described in nematodes. Pgps have been implicated in drug resistance in Plasmodium and in other parasitic protozoa, so the interest of ...
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The P-glycoprotein (Pgp), a member of a group of integral membrane proteins that contain the ATP-binding cassette, is widely represented in the animal kingdom. A family of Pgp homologues has recently been described in nematodes. Pgps have been implicated in drug resistance in Plasmodium and in other parasitic protozoa, so the interest of ...
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Dimerization of the P-glycoprotein in membranes
Biochimica et Biophysica Acta (BBA) - Biomembranes, 1990Plasma membranes from a CHO cell line, CHRC5, which exhibits multidrug resistance was studied using radiation inactivation analysis. The P-glycoprotein content of the membrane was determined by Western blots. Irradiation resulted in the loss of P-glycoprotein.
D, Boscoboinik +5 more
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P-glycoprotein function in the elderly
European Journal of Clinical Pharmacology, 2004The MDR1-encoded P-glycoprotein (Pgp) represents the best-studied membraneous efflux pump defending the body against xenobiotics. Various polymorphisms (single nucleotide polymorphisms; SNPs) in the MDR1 gene have been identified, and a silent mutation in exon 26 (C3435T) has been correlated with duodenal expression of Pgp, which might affect the ...
Stefanie S, Brenner, Ulrich, Klotz
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The Structure and Functions of P-Glycoprotein
Current Medicinal Chemistry, 2010P-glycoprotein (P-gp) is an ATP-driven transmembrane transporter capable of effluxing a wide variety of structurally diverse and functionally unrelated hydrophobic compounds out of the cell. Multidrug resistance (MDR), often associated with the over-expression of P-gp, has been implicated as a major obstacle to effective chemotherapy for cancer ...
Y, Li +5 more
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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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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
Essays in Biochemistry, 2011Pgp (P-glycoprotein) (ABCB1) is an ATP-powered efflux pump which can transport hundreds of structurally unrelated hydrophobic amphipathic compounds, including therapeutic drugs, peptides and lipid-like compounds. This 170 kDa polypeptide plays a crucial physiological role in protecting tissues from toxic xenobiotics and endogenous metabolites, and also
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Expression of P-glycoprotein in the chicken
Comparative Biochemistry and Physiology Part A: Molecular & Integrative Physiology, 2001The multidrug resistance gene product, P-glycoprotein, may act as a defense mechanism against natural and man-made environmental toxins. Like mammals, chickens show high levels of P-glycoprotein expression in the liver, small intestine, and kidney. Expression of P-glycoprotein rapidly increased with age in the liver and kidney reaching a plateau by 2 ...
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