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Literature summary extracted from

  • Revalde, J.; Li, Y.; Hawkins, B.; Rosengren, R.; Paxton, J.
    Heterocyclic cyclohexanone monocarbonyl analogs of curcumin can inhibit the activity of ATP-binding cassette transporters in cancer multidrug resistance (2015), Biochem. Pharmacol., 93, 305-317 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
7.6.2.2 (2E,4E)-8-methyl-2,4-bis[(pyridin-3-yl)methylidene]-8-azabicyclo[3.2.1]octan-3-one
-
 Homo sapiens
7.6.2.2 (2E,4E)-8-methyl-2,4-bis[(pyridin-4-yl)methylidene]-8-azabicyclo[3.2.1]octan-3-one
-
 Homo sapiens
7.6.2.2 (2E,5E)-2,5-bis[(pyridin-3-yl)methylidene]cyclopentan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(1-methyl-1H-imidazol-2-yl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(1-methyl-1H-imidazol-5-yl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(1-methyl-1H-indol-2-yl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(1-methyl-1H-pyrrol-2-yl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(2,5-dimethoxyphenyl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(2-fluoro-4,5-dimethoxyphenyl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(2-fluoropyridin-3-yl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(2-fluoropyridin-4-yl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(3,4,5-trimethoxyphenyl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(4-hydroxy-3-methoxyphenyl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(pyridin-3-yl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(pyridin-4-yl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (2E,6E)-2,6-bis[(thiophen-2-yl)methylidene]cyclohexan-1-one
-
 Homo sapiens
7.6.2.2 (3E,5E)-1-methyl-3,5-bis[(1-methyl-1H-imidazol-2-yl)methylidene]piperidin-4-one
-
 Homo sapiens
7.6.2.2 (3E,5E)-1-methyl-3,5-bis[(3,4,5-trimethoxyphenyl)methylidene]piperidin-4-one
-
 Homo sapiens
7.6.2.2 (3E,5E)-1-methyl-3,5-bis[(pyridin-3-yl)methylidene]piperidin-4-one
-
 Homo sapiens
7.6.2.2 (3E,5E)-1-methyl-3,5-bis[(pyridin-4-yl)methylidene]piperidin-4-one
-
 Homo sapiens
7.6.2.2 (3E,5E)-1-methyl-3,5-bis[(thiophen-2-yl)methylidene]piperidin-4-one
-
 Homo sapiens
7.6.2.2 (3E,5E)-3,5-bis[(2,5-dimethoxyphenyl)methylidene]-1-methylpiperidin-4-one
-
 Homo sapiens
7.6.2.2 (3E,5E)-3,5-bis[(2-fluoro-4,5-dimethoxyphenyl)methylidene]-1-methylpiperidin-4-one
-
 Homo sapiens
7.6.2.2 curcumin
-
 Homo sapiens
7.6.2.2 Ko143
-
 Homo sapiens
7.6.2.2 MK-571
-
 Homo sapiens
7.6.2.2 tert-butyl (3E,5E)-3,5-bis[(2,5-dimethoxyphenyl)methylidene]-4-oxopiperidine-1-carboxylate
-
 Homo sapiens
7.6.2.2 verapamil
-
 Homo sapiens

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[side 1] Homo sapiens
-
 ADP + phosphate + xenobiotic[side 2]
-
 ?

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 BeWo cell
-
 Homo sapiens
-
7.6.2.2 HEK-293 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
7.6.2.2 ATP + H2O + 2,7-bis-(2-carboxyethyl)-5-(and-6)-carboxyfluorescein acetoxymethyl ester[side 1]
-
 Homo sapiens ADP + phosphate + 2,7-bis-(2-carboxyethyl)-5-(and-6)-carboxyfluorescein acetoxymethyl ester[side 2]
-
 ?
7.6.2.2 ATP + H2O + calcein[side 1]
-
 Homo sapiens ADP + phosphate + calcein[side 2]
-
 ?
7.6.2.2 ATP + H2O + doxorubicin[side 1]
-
 Homo sapiens ADP + phosphate + doxorubicin[side 2]
-
 ?
7.6.2.2 ATP + H2O + etoposide[side 1]
-
 Homo sapiens ADP + phosphate + etoposide[side 2]
-
 ?
7.6.2.2 ATP + H2O + mitoxantrone[side 1]
-
 Homo sapiens ADP + phosphate + mitoxantrone[side 2]
-
 ?
7.6.2.2 ATP + H2O + rhodamine-123[side 1]
-
 Homo sapiens ADP + phosphate + rhodamine-123[side 2]
-
 ?
7.6.2.2 ATP + H2O + topotecan[side 1]
-
 Homo sapiens ADP + phosphate + topotecan[side 2]
-
 ?
7.6.2.2 ATP + H2O + xenobiotic[side 1]
-
 Homo sapiens ADP + phosphate + xenobiotic[side 2]
-
 ?

Synonyms

EC Number Synonyms Comment Organism
7.6.2.2 BCRP
-
 Homo sapiens
7.6.2.2 breast cancer resistance protein
-
 Homo sapiens
7.6.2.2 MRP1
-
 Homo sapiens
7.6.2.2 MRP5
-
 Homo sapiens
7.6.2.2 multidrug resistance-associated protein 1
-
 Homo sapiens
7.6.2.2 multidrug resistance-associated protein 5
-
 Homo sapiens
7.6.2.2 P-glycoprotein
-
 Homo sapiens
7.6.2.2 P-gp
-
 Homo sapiens
7.6.2.2 xenobiotic ABC efflux transporter
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
7.6.2.2 0.0028
-
 pH and temperature not specified in the publication Homo sapiens (2E,4E)-8-methyl-2,4-bis[(pyridin-4-yl)methylidene]-8-azabicyclo[3.2.1]octan-3-one
7.6.2.2 0.0161
-
 with calcein as substrate, pH and temperature not specified in the publication Homo sapiens curcumin
7.6.2.2 0.0169
-
 with 2,7-bis-(2-carboxyethyl)-5-(and-6)-carboxyfluorescein as substrate, pH and temperature not specified in the publication Homo sapiens curcumin