Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
1-2
|
| pubmed:dateCreated |
1999-4-13
|
| pubmed:abstractText |
P-glycoprotein (P-gp), a plasma membrane glycoprotein associated with the multidrug resistance phenotype, is responsible for the ATP-dependent efflux of various amphiphilic drugs. Using membrane vesicles prepared from the multidrug resistant cell line DC-3F/ADX, we studied the perturbation of the basal (i.e. in the absence of drug) and verapamil-dependent P-gp ATPase activities induced by various detergents, at non-solubilizing, as well as at solubilizing, concentrations. The progressive membrane solubilization with increasing detergent concentration was monitored by light scattering and centrifugation experiments. For non-solubilizing detergent concentrations, all tested detergents except DOC induced a partial inhibition of P-gp ATPase activity, which was not correlated with the amount of the various tested detergents incorporated in the membranes. Analysis of the verapamil-induced P-gp activation reveals that P-gp ATPase activity is differently modulated by the various detergents at non-solubilizing concentrations. Thus, specific interactions between P-gp and detergents are more likely to occur rather than a global membrane perturbation. After solubilization by the various tested detergents, the basal P-gp ATPase activity was virtually completely inhibited, except in the presence of CHAPS which was able to preserve this activity at a level comparable to that measured in native membranes. However, the verapamil-induced P-gp ATPase activation was lost during P-gp solubilization by CHAPS, but recovered after dilution of CHAPS below its critical micellar concentration. These observations indicate specific interactions between P-gp and CHAPS molecules within the mixed micelles. On the whole, our data evidencing specific interactions P-gp/detergents are consistent with the location of the drug transport sites on P-gp transmembrane domains.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/3-((3-cholamidopropyl)dimethylammoni...,
http://linkedlifedata.com/resource/pubmed/chemical/Adenosine Triphosphatases,
http://linkedlifedata.com/resource/pubmed/chemical/Cholic Acids,
http://linkedlifedata.com/resource/pubmed/chemical/Deoxycholic Acid,
http://linkedlifedata.com/resource/pubmed/chemical/Detergents,
http://linkedlifedata.com/resource/pubmed/chemical/Ethylene Glycol,
http://linkedlifedata.com/resource/pubmed/chemical/Glucosides,
http://linkedlifedata.com/resource/pubmed/chemical/Octoxynol,
http://linkedlifedata.com/resource/pubmed/chemical/P-Glycoprotein,
http://linkedlifedata.com/resource/pubmed/chemical/Polyethylene Glycols,
http://linkedlifedata.com/resource/pubmed/chemical/Quaternary Ammonium Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/Verapamil,
http://linkedlifedata.com/resource/pubmed/chemical/dodecyl maltoside,
http://linkedlifedata.com/resource/pubmed/chemical/dodecyloctaethyleneglycol monoether,
http://linkedlifedata.com/resource/pubmed/chemical/octyl-beta-D-glucoside,
http://linkedlifedata.com/resource/pubmed/chemical/zwittergent 3-12
|
| pubmed:status |
MEDLINE
|
| pubmed:month |
Jun
|
| pubmed:issn |
0305-7232
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:volume |
16
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
85-110
|
| pubmed:dateRevised |
2006-11-15
|
| pubmed:meshHeading |
pubmed-meshheading:9923970-Adenosine Triphosphatases,
pubmed-meshheading:9923970-Animals,
pubmed-meshheading:9923970-Cell Line,
pubmed-meshheading:9923970-Cells, Cultured,
pubmed-meshheading:9923970-Cholic Acids,
pubmed-meshheading:9923970-Cricetinae,
pubmed-meshheading:9923970-Deoxycholic Acid,
pubmed-meshheading:9923970-Detergents,
pubmed-meshheading:9923970-Dose-Response Relationship, Drug,
pubmed-meshheading:9923970-Drug Resistance, Multiple,
pubmed-meshheading:9923970-Ethylene Glycol,
pubmed-meshheading:9923970-Fibroblasts,
pubmed-meshheading:9923970-Glucosides,
pubmed-meshheading:9923970-Membranes,
pubmed-meshheading:9923970-Octoxynol,
pubmed-meshheading:9923970-P-Glycoprotein,
pubmed-meshheading:9923970-Polyethylene Glycols,
pubmed-meshheading:9923970-Quaternary Ammonium Compounds,
pubmed-meshheading:9923970-Solubility,
pubmed-meshheading:9923970-Temperature,
pubmed-meshheading:9923970-Verapamil
|
| pubmed:year |
1998
|
| pubmed:articleTitle |
Effects of detergents on P-glycoprotein atpase activity: differences in perturbations of basal and verapamil-dependent activities.
|
| pubmed:affiliation |
Section de Biophysique des Protéines et des Membranes, DBCM, CEA, and URA 2096 CNRS, Gif/Yvette, France.
|
| pubmed:publicationType |
Journal Article
|