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Literature summary extracted from

  • Al-Shawi, M.K.; Polar, M.K.; Omote, H.; Figler, R.A.
    Transition state analysis of the coupling of drug transport to ATP hydrolysis by P-glycoprotein (2003), J. Biol. Chem., 278, 52629-52640.
    View publication on PubMed

Application

EC Number Application Comment Organism
7.6.2.2 medicine Pgp plays a central role in compromising cancer chemotherapy and in modulating the bioavailability and distribution of therapeutic agents Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
7.6.2.2 MDR1 gene, expression in Saccharomyces cerevisiae Homo sapiens
7.6.2.2 pgp1 gene, expression in Chinese hamster ovary CR1R12 cells Cricetulus griseus

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 additional information ATPase activity associated with P-glycoprotein is characterized by three drug-dependent phases: basal without drug, drug-activated, and drug-inhibited Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
7.6.2.2 additional information
-
additional information kinetic data, kinetic model of drug transport Cricetulus griseus
7.6.2.2 additional information
-
additional information kinetic data, kinetic model of drug transport Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
7.6.2.2 plasma membrane
-
Cricetulus griseus 5886
-
7.6.2.2 plasma membrane recombinant Pgp, expressed in Saccharomyces cerevisiae Homo sapiens 5886
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
7.6.2.2 additional information Homo sapiens Pgp transports drugs out of cells ?
-
?

Organism

EC Number Organism UniProt Comment Textmining
7.6.2.2 Cricetulus griseus
-
-
-
7.6.2.2 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
7.6.2.2
-
Cricetulus griseus
7.6.2.2 recombinant Pgp Homo sapiens

Reaction

EC Number Reaction Comment Organism Reaction ID
7.6.2.2 ATP + H2O + xenobiotic[side 1] = ADP + phosphate + xenobiotic[side 2] thermodynamic data of ATP hydrolysis, mechanism Cricetulus griseus
7.6.2.2 ATP + H2O + xenobiotic[side 1] = ADP + phosphate + xenobiotic[side 2] thermodynamic data of ATP hydrolysis, mechanism Homo sapiens

Source Tissue

EC Number Source Tissue Comment Organism Textmining
7.6.2.2 ovary
-
Cricetulus griseus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 ATP + H2O + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/in Hoechst 33342 Homo sapiens ADP + phosphate + 2'-(4-ethoxyphenyl)-5-(4-methyl-1-piperazinyl)-2,5'-bis-1H-benzimidazole/out
-
?
7.6.2.2 ATP + H2O + colchicine/in
-
Homo sapiens ADP + phosphate + colchicine/out
-
?
7.6.2.2 ATP + H2O + rhodamine 123/in
-
Homo sapiens ADP + phosphate + rhodamine 123/out
-
?
7.6.2.2 ATP + H2O + valinomycin/in
-
Cricetulus griseus ADP + phosphate + valinomycin/out
-
?
7.6.2.2 ATP + H2O + valinomycin/in
-
Homo sapiens ADP + phosphate + valinomycin/out
-
?
7.6.2.2 ATP + H2O + verapamil/in
-
Cricetulus griseus ADP + phosphate + verapamil/out
-
?
7.6.2.2 ATP + H2O + verapamil/in unlabeled and spin-labeled verapamil Homo sapiens ADP + phosphate + verapamil/out
-
?
7.6.2.2 ATP + H2O + vinblastine/in
-
Homo sapiens ADP + phosphate + vinblastine/out
-
?
7.6.2.2 ATP + H2O + xenobiotic/in Pgp transports drugs out of cells, very broad specificity drug pump, thermodynamic analysis of ATP hydrolysis in the presence and absence of transport substrates, mechanism, model of drug transport Homo sapiens ADP + phosphate + xenobiotic/out
-
?
7.6.2.2 ATP + H2O + xenobiotic/in thermodynamic analysis of ATP hydrolysis in the presence and absence of transport substrates, mechanism Cricetulus griseus ADP + phosphate + xenobiotic/out
-
?
7.6.2.2 additional information Pgp transports drugs out of cells Homo sapiens ?
-
?
7.6.2.2 additional information ATPase activity associated with P-glycoprotein is characterized by three drug-dependent phases: basal without drug, drug-activated, and drug-inhibited, the basal ATPase activity is not a consequence of transport of an endogenous lipid or other substrate, but rather an intrinsic mechanistic property of enzyme Homo sapiens ?
-
?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 ABCB1
-
Homo sapiens
7.6.2.2 MDR1
-
Homo sapiens
7.6.2.2 P-glycoprotein
-
Homo sapiens
7.6.2.2 PGP1
-
Cricetulus griseus

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
7.6.2.2 35 37 assay at Cricetulus griseus
7.6.2.2 35 37 assay at Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
7.6.2.2 additional information
-
additional information
-
Cricetulus griseus
7.6.2.2 additional information
-
additional information
-
Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
7.6.2.2 7.4 7.5 assay at Cricetulus griseus
7.6.2.2 7.4 7.5 assay at Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
7.6.2.2 additional information
-
additional information data for drug inhibition of the basal ATPase activity Homo sapiens