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Literature summary extracted from

  • Jimenez-Alonso, S.; Perez-Lomas, A.L.; Estevez-Braun, A.; Munoz Martinez, F.; Chavez Orellana, H.; Ravelo, A.G.; Gamarro, F.; Castanys, S.; Lopez, M.
    Bis-pyranobenzoquinones as a new family of reversal agents of the multidrug resistance phenotype mediated by P-glycoprotein in mammalian cells and the protozoan parasite Leishmania (2008), J. Med. Chem., 51, 7132-7143.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
7.6.2.2 overexpression of P-glycoprotein, MRP1, or BCRP in NIH-3T3 cells and in Leishmania tropica Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 (2aR,6aR,12bS,14bS)-10,17-dimethoxy-3,3,6,6-tetramethyl-2a,3,6a,7,12b,14b-hexahydro-2H,6H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[3,2-h]chromene-13,14-dione inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells Homo sapiens
7.6.2.2 (2aR,6aS,12bR,14bS)-10,17-dimethoxy-3,3,6,6-tetramethyl-2a,3,6a,7,12b,14b-hexahydro-2H,6H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[3,2-h]chromene-13,14-dione inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells Homo sapiens
7.6.2.2 (2R,4aR,7bR,9R,11aR,14bR)-2,5,5,9,12,12-hexamethyl-1,3,4,4a,5,8,9,10,11,11a,12,14b-dodecahydrobenzo[c]isochromeno[3,4-g]chromene-7,14(2H,7bH)-dione inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells Homo sapiens
7.6.2.2 (6aS,9bR,15aS,18bR)-2,4,11,13-tetrabromo-7,7,16,16-tetramethyl-6a,15a,16,18b-tetrahydro-6H,15H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[2,3-g]chromene-9,18(7H,9bH)-dione inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells Homo sapiens
7.6.2.2 (6aS,9bR,15aS,18bR)-3,12-dimethoxy-7,7,16,16-tetramethyl-6a,15a,16,18b-tetrahydro-6H,15H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[2,3-g]chromene-9,18(7H,9bH)-dione inhibits Pgp- and MDR1-mediated daunorubicin transport in NIH-3T3 MDR1 cells Homo sapiens
7.6.2.2 additional information inhibitor effects on daunorubicin resistance and cell growth, overview Homo sapiens
7.6.2.2 verapamil
-
 Homo sapiens
7.6.2.2 zosuquidar
-
 Homo sapiens

Localization

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

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
7.6.2.2 ATP + H2O + xenobiotic/in Homo sapiens
-
 ADP + phosphate + xenobiotic/out
-
 ?

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
7.6.2.2 carcinoma cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 ATP + H2O + daunorubicin/in
-
 Homo sapiens ADP + phosphate + daunorubicin/out
-
 ?
7.6.2.2 ATP + H2O + xenobiotic/in
-
 Homo sapiens ADP + phosphate + xenobiotic/out
-
 ?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 BCRP
-
 Homo sapiens
7.6.2.2 MRP1
-
 Homo sapiens
7.6.2.2 P-glycoprotein
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
7.6.2.2 ATP
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
7.6.2.2 0.00042
-
 (2aR,6aS,12bR,14bS)-10,17-dimethoxy-3,3,6,6-tetramethyl-2a,3,6a,7,12b,14b-hexahydro-2H,6H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[3,2-h]chromene-13,14-dione recombinant MDR1in NIH-3T3 cells Homo sapiens
7.6.2.2 0.00051
-
 (6aS,9bR,15aS,18bR)-3,12-dimethoxy-7,7,16,16-tetramethyl-6a,15a,16,18b-tetrahydro-6H,15H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[2,3-g]chromene-9,18(7H,9bH)-dione recombinant MDR1in NIH-3T3 cells Homo sapiens
7.6.2.2 0.00077
-
 (2R,4aR,7bR,9R,11aR,14bR)-2,5,5,9,12,12-hexamethyl-1,3,4,4a,5,8,9,10,11,11a,12,14b-dodecahydrobenzo[c]isochromeno[3,4-g]chromene-7,14(2H,7bH)-dione recombinant MDR1in NIH-3T3 cells Homo sapiens
7.6.2.2 0.001
-
 (2aR,6aR,12bS,14bS)-10,17-dimethoxy-3,3,6,6-tetramethyl-2a,3,6a,7,12b,14b-hexahydro-2H,6H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[3,2-h]chromene-13,14-dione recombinant MDR1in NIH-3T3 cells Homo sapiens
7.6.2.2 0.001
-
 (6aS,9bR,15aS,18bR)-2,4,11,13-tetrabromo-7,7,16,16-tetramethyl-6a,15a,16,18b-tetrahydro-6H,15H-chromeno[3,4-c]chromeno[4',3':4,5]pyrano[2,3-g]chromene-9,18(7H,9bH)-dione recombinant MDR1in NIH-3T3 cells Homo sapiens