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Literature summary for 7.6.2.2 extracted from

  • Zhang, L.; Ma, S.
    Efflux pump inhibitors: a strategy to combat P-glycoprotein and the NorA multidrug resistance pump (2010), ChemMedChem, 5, 811-822.
    View publication on PubMed

Application

Application Comment Organism
medicine the presence of P-gp in various drug-resistant cancer cells can cause failure in chemotherapy, as it is able to transport a variety of anticancer drugs out of the cell Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-[4-(3-ethoxy-1-propenyl)phenyl]-4,5-bis-[4-(2-propylamino)phenyl]-1H-imidazole i.e. OC144-093. Coadministration of OC144-093 with docetaxel enhances the oral bioavailability of docetaxel to a limited extent (8-26%) in humans, and has a good safety profile as well Homo sapiens
9,10-dihydro-5-methoxy-9-oxo-N-{4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]phenyl}-4-acridine i.e. GF120918. A good and safe P-gp inhibitor alternative for cyclosporin A in enhancing the oral bioavailability of paclitaxel Homo sapiens
elacridar GF120918 Homo sapiens
KR30031
-
Homo sapiens
laniquidar R101933 Homo sapiens
additional information the main mechanisms of P-gp inhibitors involves the regulation of P-gp expression by binding to drug binding sites or modulator binding sites Homo sapiens
PSC833 i.e. valspodar Homo sapiens
tariquidar XR9576 Homo sapiens
verapamil
-
Homo sapiens
zosuquidar LY335979 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
MDR1
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.16
-
pH and temperature not specified in the publication Homo sapiens 2-[4-(3-ethoxy-1-propenyl)phenyl]-4,5-bis-[4-(2-propylamino)phenyl]-1H-imidazole

General Information

General Information Comment Organism
physiological function overexpression of P-gp is often associated with multidrug resistance, as it can efflux a wide range of large hydrophobic and amphiprotic substrates Homo sapiens