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Literature summary extracted from

  • Pinto, A.F.; Ebrahimi, M.; Saleeb, M.; Forsberg, A.; Elofsson, M.; Schueler, H.
    Identification of inhibitors of Pseudomonas aeruginosa exotoxin-S ADP-ribosyltransferase activity (2016), J. Biomol. Screen., 21, 590-595.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
2.4.2.30 peptide 14-3-3beta
-
Pseudomonas aeruginosa

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.2.30 expressed in Escherichia coli BL21(DE3) or C41 cells Pseudomonas aeruginosa

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.30 2-(3-hydroxypropyl)-3,5,6,7-tetrahydro-4H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-one
-
Pseudomonas aeruginosa
2.4.2.30 2-(3-hydroxypropyl)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
-
Pseudomonas aeruginosa
2.4.2.30 3-(4-methoxy-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-2-yl)propanoic acid
-
Pseudomonas aeruginosa
2.4.2.30 3-(4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl)propanoic acid
-
Pseudomonas aeruginosa
2.4.2.30 3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanoic acid
-
Pseudomonas aeruginosa
2.4.2.30 3-(4-oxo-3,5,6,7-tetrahydro-4H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-2-yl)propanoic acid inhibitor with micromolar potency Pseudomonas aeruginosa
2.4.2.30 4-(4-oxo-3,4-dihydroquinazolin-2-yl)butanoic acid
-
Pseudomonas aeruginosa

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
2.4.2.30 0.0225
-
N6-etheno-NAD+ at pH 7.5 and 22°C Pseudomonas aeruginosa

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.30 Pseudomonas aeruginosa
-
-
-
2.4.2.30 Pseudomonas aeruginosa PAK
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.4.2.30 glutathione Sepharose column chromatography and gel filtration Pseudomonas aeruginosa

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.30 nicotinamide 1,N6-ethenoadenine dinucleotide + (ADP-D-ribosyl)n-vH-Ras protein
-
Pseudomonas aeruginosa nicotinamide + ?
-
?
2.4.2.30 nicotinamide 1,N6-ethenoadenine dinucleotide + (ADP-D-ribosyl)n-vH-Ras protein
-
Pseudomonas aeruginosa PAK nicotinamide + ?
-
?

Synonyms

EC Number Synonyms Comment Organism
2.4.2.30 ADP-ribosyltransferase
-
Pseudomonas aeruginosa
2.4.2.30 ART
-
Pseudomonas aeruginosa
2.4.2.30 ExoS
-
Pseudomonas aeruginosa
2.4.2.30 exotoxin-S
-
Pseudomonas aeruginosa

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
2.4.2.30 0.00862
-
3-(4-oxo-3,5,6,7-tetrahydro-4H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-2-yl)propanoic acid at pH 7.5 and 22°C Pseudomonas aeruginosa

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.30 0.019
-
at pH 7.5 and 22°C Pseudomonas aeruginosa 3-(4-oxo-3,5,6,7-tetrahydro-4H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-2-yl)propanoic acid
2.4.2.30 0.0249
-
at pH 7.5 and 22°C Pseudomonas aeruginosa 4-(4-oxo-3,4-dihydroquinazolin-2-yl)butanoic acid
2.4.2.30 0.0479
-
at pH 7.5 and 22°C Pseudomonas aeruginosa 3-(4-oxo-3,4,5,6,7,8-hexahydro[1]benzothieno[2,3-d]pyrimidin-2-yl)propanoic acid
2.4.2.30 0.0524
-
at pH 7.5 and 22°C Pseudomonas aeruginosa 2-(3-hydroxypropyl)-3,5,6,7-tetrahydro-4H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-4-one
2.4.2.30 0.135
-
at pH 7.5 and 22°C Pseudomonas aeruginosa 3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanoic acid
2.4.2.30 0.169
-
at pH 7.5 and 22°C Pseudomonas aeruginosa 2-(3-hydroxypropyl)-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one
2.4.2.30 0.294
-
at pH 7.5 and 22°C Pseudomonas aeruginosa 3-(4-methoxy-6,7-dihydro-5H-cyclopenta[4,5]thieno[2,3-d]pyrimidin-2-yl)propanoic acid