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Literature summary for 7.6.2.2 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

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + H2O + xenobiotic[side 1] Homo sapiens
-
ADP + phosphate + xenobiotic[side 2]
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
BeWo cell
-
Homo sapiens
-
HEK-293 cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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]
-
?
ATP + H2O + calcein[side 1]
-
Homo sapiens ADP + phosphate + calcein[side 2]
-
?
ATP + H2O + doxorubicin[side 1]
-
Homo sapiens ADP + phosphate + doxorubicin[side 2]
-
?
ATP + H2O + etoposide[side 1]
-
Homo sapiens ADP + phosphate + etoposide[side 2]
-
?
ATP + H2O + mitoxantrone[side 1]
-
Homo sapiens ADP + phosphate + mitoxantrone[side 2]
-
?
ATP + H2O + rhodamine-123[side 1]
-
Homo sapiens ADP + phosphate + rhodamine-123[side 2]
-
?
ATP + H2O + topotecan[side 1]
-
Homo sapiens ADP + phosphate + topotecan[side 2]
-
?
ATP + H2O + xenobiotic[side 1]
-
Homo sapiens ADP + phosphate + xenobiotic[side 2]
-
?

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
0.0161
-
with calcein as substrate, pH and temperature not specified in the publication Homo sapiens curcumin
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