Active participation of membrane lipids in inhibition of multidrug transporter P-glycoprotein

نویسندگان

چکیده

Lipid invasion of P-glycoprotein, enhanced by binding an inhibitor.

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منابع مشابه

The P-glycoprotein multidrug transporter: interactions with membrane lipids, and their modulation of activity.

Gounaris, K., Mannock, D. A., Sen, A., Brain, A. P. R., Williams, W. P. and Quinn, P. J. (1983) Biochim. Biophys. Acta 732,229-242 Quinn, P. J. and Williams, W. P. (1983) Biochim. Biophys. Acta 737, 223-266 Sen, A., Mannock, D. A., Collins, D. J., Quinn, P. J. and Williams, W. P. (1983) Proc. R. SOC. London Ser. B 218, 349-364 Gounaris, K., Brain, A. P. R., Quinn, P. J. and Williams, W. P. (198...

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The P-glycoprotein multidrug transporter.

Pgp (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 affects the uptake and distribution of man...

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The reliability of molecular dynamics simulations of the multidrug transporter P-glycoprotein in a membrane environment

Despite decades of research, the mechanism of action of the ABC multidrug transporter P-glycoprotein (P-gp) remains elusive. Due to experimental limitations, many researchers have turned to molecular dynamics simulation studies in order to investigate different aspects of P-gp function. However, such studies are challenging and caution is required when interpreting the results. P-gp is highly f...

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Bivalent probes of the human multidrug transporter P-glycoprotein.

A small library of bivalent agents was designed to probe the substrate binding sites of the human multidrug transporter P-glycoprotein (P-gp). The bivalent agents were composed of two copies of the P-gp substrate emetine, linked by tethers of varied composition. An optimum distance between the emetine molecules of approximately 10 A was found to be necessary for blocking transport of the known ...

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Characterization of two pharmacophores on the multidrug transporter P-glycoprotein.

The multidrug transporter P-glycoprotein is a plasma membrane protein involved in cell and tissue detoxification and the multidrug resistance (MDR) phenotype. It actively expels from cells a number of cytotoxic molecules, all amphiphilic but chemically unrelated. We investigated the molecular characteristics involved in the binding selectivity of P-glycoprotein by means of a molecular modeling ...

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ژورنال

عنوان ژورنال: Chemical Science

سال: 2021

ISSN: ['2041-6520', '2041-6539']

DOI: https://doi.org/10.1039/d0sc06288j