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Literature summary extracted from

  • Zeinyeh, W.; Alameh, G.; Radix, S.; Grenot, C.; Dumontet, C.; Walchshofer, N.
    Design, synthesis and evaluation of progesterone-adenine hybrids as bivalent inhibitors of P-glycoprotein-mediated multidrug efflux (2010), Bioorg. Med. Chem. Lett., 20, 3165-3168.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 (17beta)-N-([trans-4-[(6-amino-9H-purin-9-yl)methyl]cyclohexyl]methyl)-3-oxoandrost-4-ene-17-carboxamide daunorubicin accumulation is 99% of the accumulation in presence of 0.01 mM progesterone Homo sapiens
7.6.2.2 (17beta)-N-[(2E)-4-(6-amino-9H-purin-9-yl)but-2-en-1-yl]-3-oxoandrost-4-ene-17-carboxamide daunorubicin accumulation is 72% of the accumulation in presence of 0.01 mM progesterone Homo sapiens
7.6.2.2 (17beta)-N-[(2Z)-4-(6-amino-9H-purin-9-yl)but-2-en-1-yl]-3-oxoandrost-4-ene-17-carboxamide daunorubicin accumulation is 86% of the accumulation in presence of 0.01 mM progesterone Homo sapiens
7.6.2.2 (17beta)-N-[4-(6-amino-9H-purin-9-yl)but-2-yn-1-yl]-3-oxoandrost-4-ene-17-carboxamide daunorubicin accumulation is 61% of the accumulation in presence of 0.01 mM progesterone Homo sapiens
7.6.2.2 (17beta)-N-[4-(6-amino-9H-purin-9-yl)butyl]-3-oxoandrost-4-ene-17-carboxamide daunorubicin accumulation is 78% of the accumulation in presence of 0.01 mM progesterone Homo sapiens
7.6.2.2 (17beta)-N-[4-[(6-amino-9H-purin-9-yl)methyl]benzyl]-3-oxoandrost-4-ene-17-carboxamide daunorubicin accumulation is 98% of the accumulation in presence of 0.01 mM progesterone Homo sapiens
7.6.2.2 (17beta)-N-[6-(6-amino-9H-purin-9-yl)hexyl]-3-oxoandrost-4-ene-17-carboxamide daunorubicin accumulation is 111% of the accumulation in presence of 0.01 mM progesterone Homo sapiens
7.6.2.2 progesterone
-
 Homo sapiens

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 K-562/R7 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
-
 ?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 ABCB1
-
 Homo sapiens
7.6.2.2 P-glycoprotein
-
 Homo sapiens