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Literature summary for 7.6.2.2 extracted from

  • Fong, W.F.; Shen, X.L.; Globisch, C.; Wiese, M.; Chen, G.Y.; Zhu, G.Y.; Yu, Z.L.; Tse, A.K.; Hu, Y.J.
    Methoxylation of 3,4-aromatic side chains improves P-glycoprotein inhibitory and multidrug resistance reversal activities of 7,8-pyranocoumarin against cancer cells (2008), Bioorg. Med. Chem., 16, 3694-3703.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
cis-(Z)-flupentixol is a non-competitive inhibitor that interacts with the substrate site but is not transported Homo sapiens
curcumin modulates Pgp expression Homo sapiens
praeruptorin A modulates Pgp expression Homo sapiens
XR9576 is a non-competitive inhibitor that interacts with the substrate site but is not transported Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane
-
Homo sapiens 16020
-

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
Homo sapiens

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
170000
-
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + xenobiotic/in Homo sapiens P-glycoprotein is a membrane ATP-driven drug exporter, Pgp actively extrudes a spectrum of hydrophobic xenobiotics, including a number of anticancer drugs ADP + phosphate + xenobiotic/out
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
gene MDR1 encoding Pgp
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + doxorubicin/in
-
Homo sapiens ADP + phosphate + doxorubicin/out
-
?
ATP + H2O + paclitaxel/in
-
Homo sapiens ADP + phosphate + paclitaxel/out
-
?
ATP + H2O + puromycin/in
-
Homo sapiens ADP + phosphate + puromycin/out
-
?
ATP + H2O + vinblastine/in
-
Homo sapiens ADP + phosphate + vinblastine/out
-
?
ATP + H2O + xenobiotic/in structure-activity relationship, overview Homo sapiens ADP + phosphate + xenobiotic/out
-
?
ATP + H2O + xenobiotic/in P-glycoprotein is a membrane ATP-driven drug exporter, Pgp actively extrudes a spectrum of hydrophobic xenobiotics, including a number of anticancer drugs Homo sapiens ADP + phosphate + xenobiotic/out
-
?

Synonyms

Synonyms Comment Organism
P-glycoprotein
-
Homo sapiens
Pgp
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens