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Literature summary for 7.6.2.2 extracted from

  • Garrigues, A.; Escargueil, A.E.; Orlowski, S.
    The multidrug transporter, P-glycoprotein, actively mediates cholesterol redistribution in the cell membrane (2002), Proc. Natl. Acad. Sci. USA, 99, 10347-10352.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 7.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
MDR1 gene expression in Sf9 cells, pgp1 gene overexpression in DC-3F/ADX cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
cyclosporin A
-
 Homo sapiens
Digitonin inhibits ATPase activity of P-gp Homo sapiens
methyl-beta-cyclodextrin inhibits ATPase activity of P-gp, 5-10 mM, total inhibition Homo sapiens
PSC833 specific P-gp inhibitor Homo sapiens
vinblastine
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
plasma membrane
-
 Homo sapiens 5886
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + cholesterol/in Homo sapiens P-gp may actively mediate cholesterol redistribution in the cell membrane, P-gp mediates the ATP-dependent relocation of cholesterol from the cytosolic leaflet to the exoplasmic leaflet of the plasma membrane, P-gp likely contributes in stabilizing the cholesterol-rich microdomains, rafts and caveolae, and is involved in the regulation of cholesterol trafficking in cells ADP + phosphate + cholesterol/out
-
 ?
additional information Homo sapiens the ABC transporter P-glycoprotein is responsible for multidrug resistance in tumor cells ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
DC-3F/ADX cell MDR cell line overexpressing pgp1 gene Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + cholesterol/in P-gp may actively mediate cholesterol redistribution in the cell membrane, P-gp mediates the ATP-dependent relocation of cholesterol from the cytosolic leaflet to the exoplasmic leaflet of the plasma membrane, P-gp likely contributes in stabilizing the cholesterol-rich microdomains, rafts and caveolae, and is involved in the regulation of cholesterol trafficking in cells Homo sapiens ADP + phosphate + cholesterol/out
-
 ?
ATP + H2O + cholesterol/in P-gp may actively mediate cholesterol redistribution in the cell membrane, in the absence of substrates P-gp exhibits an apparently futile, basal ATPase activity, which is tightly dependent on the presence of cholesterol in the membrane by using native membrane vesicles containing high amounts of P-gp Homo sapiens ADP + phosphate + cholesterol/out
-
 ?
ATP + H2O + progesterone/in P-gp substrate Homo sapiens ADP + phosphate + progesterone/out
-
 ?
ATP + H2O + verapamil/in P-gp substrate Homo sapiens ADP + phosphate + verapamil/out
-
 ?
ATP + H2O + xenobiotic/in P-gp catalyzes the ATP hydrolysis-dependent efflux of numerous amphiphilic compounds of unrelated chemical structures Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?
additional information the ABC transporter P-glycoprotein is responsible for multidrug resistance in tumor cells Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
MDR1
-
 Homo sapiens
P-gp
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Homo sapiens