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Literature summary for 7.6.2.2 extracted from

  • Murakami, M.; Ohnuma, S.; Fukuda, M.; Chufan, E.E.; Kudoh, K.; Kanehara, K.; Sugisawa, N.; Ishida, M.; Naitoh, T.; Shibata, H.; Iwabuchi, Y.; Ambudkar, S.V.; Unno, M.
    Synthetic analogs of curcumin modulate the function of multidrug resistance-linked ATP-binding cassette transporter ABCG2 (2017), Drug Metab. Dispos., 45, 1166-1177 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 7.6.2.2

Cloned(Commentary)

Cloned (Comment) Organism
expressed in High Five insect cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-4,4-dibromopent-1-en-3-one 58.7% inhibition at 0.01 mM Homo sapiens
(1E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-4,4-dichloropent-1-en-3-one 51.5% inhibition at 0.01 mM Homo sapiens
(1E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-4,4-difluoropent-1-en-3-one 44.4% inhibition at 0.01 mM Homo sapiens
(1E)-1-[3,5-bis(methoxymethoxy)phenyl]-4,4-dimethylpent-1-en-3-one 14.9% inhibition at 0.01 mM Homo sapiens
(1E,4E)-1,5-bis(4-hydroxy-3-methoxyphenyl)penta-1,4-dien-3-one 51.8% inhibition at 0.01 mM Homo sapiens
(1E,4E)-1,5-bis[3,4-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one 84.3% inhibition at 0.01 mM Homo sapiens
(1E,4E)-1-(2H-1,3-benzodioxol-5-yl)-5-[3,5-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one 57.4% inhibition at 0.01 mM Homo sapiens
(1E,4E)-1-(4-hydroxy-3,5-dimethoxyphenyl)-5-(3,4,5-trimethoxyphenyl)penta-1,4-dien-3-one 82.9% inhibition at 0.01 mM Homo sapiens
(1Z,4E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-2-chloropenta-1,4-dien-3-one 83.2% inhibition at 0.01 mM Homo sapiens
(1Z,4E)-5-[3,5-bis(methoxymethoxy)phenyl]-2-bromo-1-[2-bromo-3,5-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one 77.4% inhibition at 0.01 mM Homo sapiens
(2E)-3-[3,5-bis(methoxymethoxy)phenyl]-N-methylprop-2-enamide 6.1% inhibition at 0.01 mM Homo sapiens
(2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enal 9.2% inhibition at 0.01 mM Homo sapiens
(2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enoic acid 0.3% inhibition at 0.01 mM Homo sapiens
(2E,6E)-2,6-bis[(2-fluorophenyl)methylidene]cyclohexan-1-one 30.5% inhibition at 0.01 mM Homo sapiens
(2E,6E)-2,6-bis[[3,5-bis(methoxymethoxy)phenyl]methylidene]cyclohexan-1-one 69.8% inhibition at 0.01 mM Homo sapiens
(3E,5E)-3,5-bis[[3,5-bis(methoxymethoxy)phenyl]methylidene]-1-methylpiperidin-4-one 52% inhibition at 0.01 mM Homo sapiens
(4E)-5-[3,5-bis(methoxymethoxy)phenyl]-2-[[3,4-bis(methoxymethoxy)phenyl]methyl]-3-oxopent-4-enenitrile 29.9% inhibition at 0.01 mM Homo sapiens
1,5-bis[3,4-bis(methoxymethoxy)phenyl]-1,5-bis(phenylsulfanyl)pentan-3-one 26.6% inhibition at 0.01 mM Homo sapiens
1,5-bis[3,4-bis(methoxymethoxy)phenyl]-1,5-bis[(2,3-dihydroxypropyl)sulfanyl]pentan-3-one 1.6% inhibition at 0.01 mM Homo sapiens
1,5-bis[3,5-bis(methoxymethoxy)phenyl]-1,5-bis(ethylsulfanyl)pentan-3-one 37.1% inhibition at 0.01 mM Homo sapiens
curcumin 99.5% inhibition at 0.01 mM Homo sapiens
Kol43
-
 Homo sapiens
methyl (2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enoate 8.6% inhibition at 0.01 mM Homo sapiens
N,N'-[[1,5-bis[3,4-bis(methoxymethoxy)phenyl]-3-oxopentane-1,5-diyl]bis(sulfanediylethane-2,1-diyl)]diacetamide 15.2% inhibition at 0.01 mM Homo sapiens
S-propyl (2E)-3-[3,5-bis(methoxymethoxy)phenyl]prop-2-enethioate 28.2% inhibition at 0.01 mM 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 Q9UNQ0
-
-

Source Tissue

Source Tissue Comment Organism Textmining
K-562 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + iodoarylazidoprazosin[side 1]
-
 Homo sapiens ADP + phosphate + iodoarylazidoprazosin[side 2]
-
 ?
ATP + H2O + mitoxantrone[side 1]
-
 Homo sapiens ADP + phosphate + mitoxantrone[side 2]
-
 ?
ATP + H2O + pheophorbide A[side 1]
-
 Homo sapiens ADP + phosphate + pheophorbide A[side 2]
-
 ?
ATP + H2O + SN-38[side 1] SN-38 is 7-ethyl-10-hydroxy-CPT Homo sapiens ADP + phosphate + SN-38[side 2]
-
 ?
ATP + H2O + xenobiotic[side 1]
-
 Homo sapiens ADP + phosphate + xenobiotic[side 2]
-
 ?

Synonyms

Synonyms Comment Organism
ABCG2
-
 Homo sapiens
BCRP
-
 Homo sapiens
breast cancer resistance protein
-
 Homo sapiens
multidrug resistance-linked ATP-binding cassette transporter
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00019
-
 at 37°C, pH not specified in the publication Homo sapiens Kol43
0.00025
-
 at 37°C, pH not specified in the publication Homo sapiens (1Z,4E)-1,5-bis[3,5-bis(methoxymethoxy)phenyl]-2-chloropenta-1,4-dien-3-one
0.00031
-
 at 37°C, pH not specified in the publication Homo sapiens (1E,4E)-1-(4-hydroxy-3,5-dimethoxyphenyl)-5-(3,4,5-trimethoxyphenyl)penta-1,4-dien-3-one
0.00037
-
 at 37°C, pH not specified in the publication Homo sapiens (1Z,4E)-5-[3,5-bis(methoxymethoxy)phenyl]-2-bromo-1-[2-bromo-3,5-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one
0.00051
-
 at 37°C, pH not specified in the publication Homo sapiens (1E,4E)-1,5-bis[3,4-bis(methoxymethoxy)phenyl]penta-1,4-dien-3-one
0.00062
-
 at 37°C, pH not specified in the publication Homo sapiens curcumin