ArticlePharmaceutical research2007
P-glycoprotein in proteoliposomes with low residual detergent: the effects of cholesterol.
Article in Pharmaceutical research, 2007. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
What it found
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Who cites it
13 citing papers in PubMed, 29 citations in OpenAlex.
- Exploring lipid diversity and minimalism to define membrane requirements for synthetic cells.FEBS letters · 2025Review
- Association between residual cholesterol and vulnerable non-culprit lesions progressing to major adverse cardiovascular events.Frontiers in endocrinology · 2025Observational
- Ligand's Partition to the Lipid Bilayer Should Be Accounted for When Estimating Their Affinity to Proteins.Molecules (Basel, Switzerland) · 2023Article
- Interaction of a Homologous Series of Amphiphiles with P-glycoprotein in a Membrane Environment-Contributions of Polar and Non-Polar Interactions.Pharmaceutics · 2023Article
- Lipid environment determines the drug-stimulated ATPase activity of P-glycoprotein.Frontiers in molecular biosciences · 2023Article
- Characterization of the Lipidome and Biophysical Properties of Membranes from High Five Insect Cells Expressing Mouse P-Glycoprotein.Biomolecules · 2021Article
- Arbuscular Mycorrhizal Fungi Alter Plant and Soil C:N:P Stoichiometries Under Warming and Nitrogen Input in a Semiarid Meadow of China.International journal of environmental research and public health · 2019Article
- Hydrogel-assisted functional reconstitution of human P-glycoprotein (ABCB1) in giant liposomes.Biochimica et biophysica acta · 2015Article
- Complex Interplay between the P-Glycoprotein Multidrug Efflux Pump and the Membrane: Its Role in Modulating Protein Function.Frontiers in oncology · 2014Review
- Biophysics of cell membrane lipids in cancer drug resistance: Implications for drug transport and drug delivery with nanoparticles.Advanced drug delivery reviews · 2013Review
- Conformational analysis of human ATP-binding cassette transporter ABCB1 in lipid nanodiscs and inhibition by the antibodies MRK16 and UIC2.The Journal of biological chemistry · 2011Article
- Chapter 11 - Reconstitution of membrane proteins in phospholipid bilayer nanodiscs.Methods in enzymology · 2009Article
- Comparative analysis of CK2 expression and function in tumor cell lines displaying sensitivity vs. resistance to chemical induced apoptosis.Molecular and cellular biochemistry · 2008Article
Corrections and comments
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeThere is evidence that cholesterol affects the ATPase and transport functions of P-glycoprotein (P-gp). To study the influence of cholesterol on P-gp in a well defined lipid environment, we reconstituted P-gp in egg phosphatidylcholine (PhC) and PhC/cholesterol proteoliposomes with negligible residual amounts of detergents. MATERIALS AND
methodsP-gp proteoliposomes were prepared by continuous dialysis from micelles consisting of P-gp, lipids, sodium dodecyl sulfate and cholate. Basal and modulator-induced ATPase activities were studied in an established enzyme assay. Modulator affinities to P-gp and to the lipid bilayers were determined by equilibrium dialysis.
resultsIn the absence of cholesterol the basal ATPase activity was six fold lower than in the presence of 20 or 40% cholesterol, and no P-gp binding and ATPase induction was detected for the tested modulators verapamil and progesterone. In proteoliposomes containing 20 and 40% cholesterol, respectively, the modulators showed significant P-gp binding and ATPase activation. The concentration of the modulators for half maximal activation of the ATPase was higher with 40% than with 20% cholesterol.
conclusionsCholesterol influences P-gp in three ways: (a) it enhances its basal ATPase activity, (b) it renders P-gp sensitive towards the modulators verapamil and progesterone and (c) it affects the modulator concentration at half maximal ATPase activation.
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