P-glycoprotein in proteoliposomes with low residual detergent: the effects of cholesterol.

P-glycoprotein in proteoliposomes with low residual detergent: the effects of cholesterol. Research Abstract Details 

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P-glycoprotein in proteoliposomes with low residual detergent: the effects of cholesterol. Abstract Text:

Karsten Bucher,Sara Belli,Heidi Wunderli-Allenspach,Stefanie D ,

PURPOSE: There 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 METHODS: P-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. RESULTS: In 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. CONCLUSIONS: Cholesterol 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.

P-glycoprotein in proteoliposomes with low residual detergent: the effects of cholesterol. Publishing Authors By Initials

K Bucher,S Belli,H Wunderli-Allenspach,SD ,

For similar organic chemicals: amines: ethylamines: phenethylamines: verapamil research abstracts see: organic chemicals: amines: ethylamines: phenethylamines: verapamil research

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P-glycoprotein in proteoliposomes with low residual detergent: the effects of cholesterol. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Pharmaceutical research

VOLUME: 24

Page Numbers: 1993-2004

Journal Abbreviation: Pharm. Res.

ISSN: 0724-8741

DAY: 12

MONTH: 05

YEAR: 2007

P-glycoprotein in proteoliposomes with low residual detergent: the effects of cholesterol. Information

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LANGUAGE: eng

NlmUniqueID: 8406521

P-glycoprotein in proteoliposomes with low residual detergent: the effects of cholesterol. Keywords Mesh Terms:

KEYWORDS: Verapamil

MESH TERMS: metabolism

Chemical & Substance for Abstract: P-glycoprotein in proteoliposomes with low residual detergent: the effects of cholesterol. Information

Substance Name: Adenosine Triphosphatases

Registry Number: EC 3.6.1.-

Grant and Affiliation Information for P-glycoprotein in proteoliposomes with low residual detergent: the effects of cholesterol.

AFFILIATION: Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, ETH Zurich, Wolfgang-Pauli-Strasse 10, 8093, Zurich, Switzerland.

Country: United States

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MEDLINETA: Pharm Res

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