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Literature summary for 7.2.2.13 extracted from

  • Piacente, S.; Masullo, M.; De Neve, N.; Dewelle, J.; Hamed, A.; Kiss, R.; Mijatovic, T.
    Cardenolides from Pergularia tomentosa display cytotoxic activity resulting from their potent inhibition of Na+/K+-ATPase (2009), J. Nat. Prod., 72, 1087-1091.
    View publication on PubMed
Search for more literature for 7.2.2.13

Inhibitors

Inhibitors Comment Organism Structure
(1R,2R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15aR)-2,3a,11,11a-tetrahydroxy-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
-
 Homo sapiens
(1R,2R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9-(hydroxymethyl)-15a-methyl-1-(5-oxo-2,5-dihydrofuran-3-yl)-2-(2-oxopropanoyl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
-
 Homo sapiens
(1R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15aR)-13a-formyl-3a,11a-dihydroxy-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-11-yl beta-D-glucopyranoside
-
 Homo sapiens
(1R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
-
 Homo sapiens
(1R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9-(hydroxymethyl)-15a-methyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
-
 Homo sapiens
19-hydroxy-2''-oxovoruscharin i.e. UNBS1450, a trans-trans-cis cardiotonic steroid Homo sapiens
4-[(1R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15R,15aS)-3a,11,11a,15-tetrahydroxy-13a-(hydroxymethyl)-9,15a-dimethylicosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-1-yl]furan-2(5H)-one
-
 Homo sapiens
4-[(1R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9,13a-bis(hydroxymethyl)-15a-methylicosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-1-yl]furan-2(5H)-one
-
 Homo sapiens
4-[(1R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15R,15aS)-3a,11,11a,15-tetrahydroxy-9,13a-bis(hydroxymethyl)-15a-methylicosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-1-yl]furan-2(5H)-one
-
 Homo sapiens
additional information inhibitory potencies of cardenolide glycosides, isolated from the roots of Pergularia tomentosa, on Na+,K+-ATPase activity Homo sapiens

Localization

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

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
 Homo sapiens
-
BxPC-3 cell
-
 Homo sapiens
-
carcinoma cell
-
 Homo sapiens
-
LoVo cell
-
 Homo sapiens
-
MCF-7 cell
-
 Homo sapiens
-
PC-3 cell
-
 Homo sapiens
-
U-373MG cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O + Na+/in + K+/out
-
 Homo sapiens ADP + phosphate + Na+/out + K+/in
-
 ?

Synonyms

Synonyms Comment Organism
Na+/K+-ATPase
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.8
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0003
-
 pH 7.8, 37°C Homo sapiens 4-[(1R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15R,15aS)-3a,11,11a,15-tetrahydroxy-9,13a-bis(hydroxymethyl)-15a-methylicosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-1-yl]furan-2(5H)-one
0.0004
-
 pH 7.8, 37°C Homo sapiens (1R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
0.0004
-
 pH 7.8, 37°C Homo sapiens 4-[(1R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9,13a-bis(hydroxymethyl)-15a-methylicosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-1-yl]furan-2(5H)-one
0.0005
-
 pH 7.8, 37°C Homo sapiens (1R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9-(hydroxymethyl)-15a-methyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
0.0005
-
 pH 7.8, 37°C Homo sapiens (1R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15aR)-13a-formyl-3a,11a-dihydroxy-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-11-yl beta-D-glucopyranoside
0.0007
-
 pH 7.8, 37°C Homo sapiens 4-[(1R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15R,15aS)-3a,11,11a,15-tetrahydroxy-13a-(hydroxymethyl)-9,15a-dimethylicosahydro-1H,7aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxin-1-yl]furan-2(5H)-one
0.0012
-
 pH 7.8, 37°C Homo sapiens (1R,2R,3aS,5aS,6aR,7aS,9S,11R,11aS,12aR,13aR,15aR)-3a,11,11a-trihydroxy-9-(hydroxymethyl)-15a-methyl-1-(5-oxo-2,5-dihydrofuran-3-yl)-2-(2-oxopropanoyl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde
0.0017
-
 pH 7.8, 37°C Homo sapiens (1R,2R,3aS,5aS,6aR,7aS,9R,11R,11aS,12aR,13aR,15aR)-2,3a,11,11a-tetrahydroxy-9,15a-dimethyl-1-(5-oxo-2,5-dihydrofuran-3-yl)icosahydro-7aH,13aH-cyclopenta[7,8]phenanthro[2,3-b]pyrano[3,2-e][1,4]dioxine-13a-carbaldehyde