NDLI: P-Glycoprotein in Proteoliposomes with Low Residual Detergent: The Effects of Cholesterol

Content Provider	Springer Nature Link
Author	Bucher, Karsten Belli, Sara Wunderli Allenspach, Heidi Krämer, Stefanie D.
Copyright Year	2007
Abstract	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.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.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.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.
Starting Page	1993
Ending Page	2004
Page Count	12
File Format	PDF
ISSN	07248741
Journal	Pharmaceutical Research
Volume Number	24
Issue Number	11
e-ISSN	1573904X
Language	English
Publisher	Springer US
Publisher Date	2007-05-12
Publisher Place	Boston
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	ATPase activity binding cholesterol P-glycoprotein verapamil Biomedical Engineering Medical Law Biochemistry Pharmacy Pharmacology/Toxicology
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Pharmacology Molecular Medicine Pharmacology (medical) Biotechnology Pharmaceutical Science

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

Isolated Rafts from Adriamycin-Resistant P388 Cells Contain Functional ATPases and Provide an Easy Test System for P-glycoprotein–Related Activities

The Enantioselective Binding of Mefloquine Enantiomers to P-glycoprotein Determined Using An Immobilized P-glycoprotein Liquid Chromatographic Stationary Phase

Modeling Cardiac Uptake and Negative Inotropic Response of Verapamil in Rat Heart: Effect of Amiodarone

Grapefruit Juice Activates P-Glycoprotein-Mediated Drug Transport

P-Glycoprotein Attenuating Effect of Human Intestinal Fluid

Influence of P-Glycoprotein Modulators on Cardiac Uptake, Metabolism, and Effects of Idarubicin

Effects of Intestinal CYP3A4 and P-Glycoprotein on Oral Drug Absorption—Theoretical Approach

Influence of Passive Permeability on Apparent P-glycoprotein Kinetics

Structural Determinants of P-Glycoprotein-Mediated Transport of Glucocorticoids

P-Glycoprotein in Proteoliposomes with Low Residual Detergent: The Effects of Cholesterol

Similar Documents

Isolated Rafts from Adriamycin-Resistant P388 Cells Contain Functional ATPases and Provide an Easy Test System for P-glycoprotein–Related Activities

The Enantioselective Binding of Mefloquine Enantiomers to P-glycoprotein Determined Using An Immobilized P-glycoprotein Liquid Chromatographic Stationary Phase

Modeling Cardiac Uptake and Negative Inotropic Response of Verapamil in Rat Heart: Effect of Amiodarone

Grapefruit Juice Activates P-Glycoprotein-Mediated Drug Transport

P-Glycoprotein Attenuating Effect of Human Intestinal Fluid

Influence of P-Glycoprotein Modulators on Cardiac Uptake, Metabolism, and Effects of Idarubicin

Effects of Intestinal CYP3A4 and P-Glycoprotein on Oral Drug Absorption—Theoretical Approach

Influence of Passive Permeability on Apparent P-glycoprotein Kinetics

Structural Determinants of P-Glycoprotein-Mediated Transport of Glucocorticoids

P-Glycoprotein in Proteoliposomes with Low Residual Detergent: The Effects of Cholesterol