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Literature summary for 7.6.2.2 extracted from

  • Wang, E.J.; Casciano, C.N.; Clement, R.P.; Johnson, W.W.
    Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein (2001), Drug Metab. Dispos., 29, 1080-1083.
    View publication on PubMed
Search for more literature for 7.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
MDR1 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
cyclosporin A inhibits daunorubicin transport, IC50: 0.001 nM Homo sapiens
desloratadine weakly inhibits daunorubicin transport, 19% of the inhibition caused by vanadate, IC50: 0.043 nM, desloratadine is no significant inhibitor of P-gp and should not cause clinical drug interactions with agents that are P-gp substrates Homo sapiens
loratadine inhibits daunorubicin transport, IC50: 0.011 nM, much less inhibitory than cyclosporin A or verapamil, 43% of the inhibition caused by vanadate Homo sapiens
vanadate very potent inhibitor of MDR1 efflux function Homo sapiens
verapamil inhibits daunorubicin transport, IC50: 0.004 nM Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
 additional information
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
plasma membrane MDR1 encodes a 170 kDa integral plasma membrane protein Homo sapiens 5886
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + xenobiotic/in Homo sapiens MDR1, multiple drug resistance, ABC transporter, which acts as ATP-driven pump that removes xenobiotics from the interior of cells ADP + phosphate + xenobiotic/out
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
glycoprotein MDR1, phosphorylated glycoprotein Homo sapiens
phosphoprotein MDR1, phosphorylated glycoprotein Homo sapiens

Source Tissue

Source Tissue Comment Organism Textmining
NIH 3T3-G185 cell cell line overexpressing the cloned human MDR1 gene product Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + daunorubicin/in
-
 Homo sapiens ADP + phosphate + daunorubicin/out
-
 ?
ATP + H2O + loratadine/in
-
 Homo sapiens ADP + phosphate + loratadine/out
-
 ?
ATP + H2O + nifedipine/in
-
 Homo sapiens ADP + phosphate + nifedipine/out
-
 ?
ATP + H2O + xenobiotic/in MDR1, multiple drug resistance, ABC transporter, which acts as ATP-driven pump that removes xenobiotics from the interior of cells Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?
ATP + H2O + xenobiotic/in MDR1, ABC transporter, which acts as ATP-driven pump that removes xenobiotics from the interior of cells, uses a wide variety of substrates Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?
additional information not: desloratadine Homo sapiens ?
-
 ?

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000000001
-
 inhibits daunorubicin transport, IC50: 0.001 nM Homo sapiens cyclosporin A
0.000000004
-
 inhibits daunorubicin transport, IC50: 0.004 nM Homo sapiens verapamil
0.000000011
-
 inhibits daunorubicin transport, IC50: 0.011 nM, much less inhibitory than cyclosporin A or verapamil, 43% of the inhibition caused by vanadate Homo sapiens loratadine
0.000000043
-
 weakly inhibits daunorubicin transport, 19% of the inhibition caused by vanadate, IC50: 0.043 nM, desloratadine is no significant inhibitor of P-gp and should not cause clinical drug interactions with agents that are P-gp substrates Homo sapiens desloratadine