Title : Understanding the accumulation of P-glycoprotein substrates within cells: The effect of cholesterol on membrane partitioning.

Pub. Date : 2016 Apr

PMID : 26724201






6 Functional Relationships(s)
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1 Understanding the accumulation of P-glycoprotein substrates within cells: The effect of cholesterol on membrane partitioning. Cholesterol ATP binding cassette subfamily B member 1 Homo sapiens
2 The apparent activity of the multidrug transporter P-glycoprotein (P-gp) is enhanced by the presence of cholesterol. Cholesterol ATP binding cassette subfamily B member 1 Homo sapiens
3 The apparent activity of the multidrug transporter P-glycoprotein (P-gp) is enhanced by the presence of cholesterol. Cholesterol ATP binding cassette subfamily B member 1 Homo sapiens
4 Whether this is due to the direct effect of cholesterol on the activity of P-gp, its effect on the local concentration of substrate in the membrane, or its effect on the rate of entry of the drug into the cell, is unknown. Cholesterol ATP binding cassette subfamily B member 1 Homo sapiens
5 In this study, molecular dynamics simulation techniques coupled with potential of mean force calculations have been used to investigate the role of cholesterol in the movement of four P-gp substrates across a POPC bilayer in the presence or absence of 10% cholesterol. Cholesterol ATP binding cassette subfamily B member 1 Homo sapiens
6 These findings suggest that P-gp substrates may preferentially accumulate in cholesterol-rich regions of the membrane, which may explain its enhanced transport activity. Cholesterol ATP binding cassette subfamily B member 1 Homo sapiens