Results 261 to 270 of about 507,211 (287)
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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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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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P-glycoprotein in breast cancer
1989Resistance to cytotoxic chemotherapy is a major impediment to the successful treatment of breast cancer. Adjuvant chemotherapy, though given under theoretically optimal conditions of low tumor bulk [1], often fails to eradicate micrometastasis.
D E, Merkel, S A, Fuqua, W L, McGuire
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Cytokine Regulation of P-Glycoprotein
Drug Metabolism Reviews, 2003P-glycoprotein (Pgp) is a membrane bound transporter involved in the disposition of many endogenous compounds and xenobiotics. Alterations in Pgp expression and activity can significantly affect the disposition of Pgp substrates. Infection and inflammatory stimuli have also been shown to alter drug disposition.
Mary Peace, McRae +2 more
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Photoaffinity Labeling of P-Glycoprotein
Mini-Reviews in Medicinal Chemistry, 2005The aim of the present review is to summarize recent progress in identifying substrate binding domains of P-glycoprotein by photoaffinity labeling. Preferred substrate binding regions have been identified using a number of photoaffinity ligands, including anthracyclines, the quinazoline iodoarylazidoprazosine (IAAP), dihydropyridines, taxanes and ...
Michael, Peer +4 more
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P-glycoprotein in autoimmune diseases
Autoimmunity Reviews, 2004Multidrug resistance-1 (MDR-1) is characterized by overfunction of P-glycoprotein (P-gp), a pump molecule that decreases intracellular drug concentration by effluxing them from the intracellular space. Broad ranges of structurally unrelated compounds are transported by P-gp, including antineoplastic agents, HIV protease inhibitors, prednisone, gold ...
Yvonne, Richaud-Patin +3 more
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