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Literature summary for 7.6.2.2 extracted from

  • Lu, P.; Liu, R.; Sharom, F.J.
    Drug transport by reconstituted P-glycoprotein in proteoliposomes. Effect of substrates and modulators, and dependence on bilayer phase state (2001), Eur. J. Biochem., 268, 1687-1697.
    View publication on PubMed
Search for more literature for 7.6.2.2

Activating Compound

Activating Compound Comment Organism Structure
Colchicine activates the transport of tetramethylrosamine, probably by a positive allosteric effect Cricetulus griseus

Inhibitors

Inhibitors Comment Organism Structure
cyclosporin A inhibits the transport of tetramethylrosamine in a concentration-dependent manner, 0.004 mM: almost complete inhibition, competes for tetramethylrosamine transport at the drug binding site Cricetulus griseus
additional information not inhibited by colchicine Cricetulus griseus
vanadate inhibits Pgp ATPase and tetramethylrosamine transport activity, interacts with the nucleotide-binding domain Cricetulus griseus
verapamil inhibits the transport of tetramethylrosamine in a concentration-dependent manner, 0.02 mM: almost complete inhibition, competes for tetramethylrosamine transport at the drug binding site Cricetulus griseus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0003
-
 tetramethylrhodamine/in
-
 Cricetulus griseus
0.48
-
 ATP
-
 Cricetulus griseus

Localization

Localization Comment Organism GeneOntology No. Textmining
plasma membrane intimate association of both Pgp and its substrates with the membrane, dependence of the rate of tetramethylrosamine transport by Pgp on the bilayer phase state, the transport rate is relatively high in the rigid gel phase, reaches a maximum at the melting temperature of the bilayer, and then decreases in the fluid liquid crystalline phase Cricetulus griseus 5886
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Cricetulus griseus multidrug transporter, ATP-driven drug transport, the intimate association of both Pgp and its substrates with the membrane suggests that its function may be regulated by the biophysical properties of the lipid bilayer ?
-
 ?

Organism

Organism UniProt Comment Textmining
Cricetulus griseus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Cricetulus griseus

Source Tissue

Source Tissue Comment Organism Textmining
CHRB30 cell Chinese hamster ovary cell line Cricetulus griseus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + colchicine/in
-
 Cricetulus griseus ADP + phosphate + colchicine/out
-
 ?
ATP + H2O + rhodamine 123/in less efficient substrate than tetramethylrosamine Cricetulus griseus ADP + phosphate + rhodamine 123/out
-
 ?
ATP + H2O + tetramethylrhodamine/in better substrate than rhodamine 123, temperature dependence of the rate of tetramethylrosamine transport, the rate of drug transport may be dominated by partitioning of drug into the membrane bilayer Cricetulus griseus ADP + phosphate + tetramethylrhodamine/out
-
 ?
additional information multidrug transporter, ATP-driven drug transport, the intimate association of both Pgp and its substrates with the membrane suggests that its function may be regulated by the biophysical properties of the lipid bilayer Cricetulus griseus ?
-
 ?

Temperature Range [°C]

Temperature Minimum [°C] Temperature Maximum [°C] Comment Organism
additional information
-
 pattern of temperature dependence of the rate of tetramethylrosamine transport by Pgp, the transport rate is relatively high in the rigid gel phase, reaches a maximum at the melting temperature of the bilayer, and then decreases in the fluid liquid crystalline phase Cricetulus griseus