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Literature summary for 2.4.2.30 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
Search for more literature for 2.4.2.30

Activating Compound

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

Cloned(Commentary)

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

Inhibitors

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

KM Value [mM]

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

Organism

Organism UniProt Comment Textmining
Pseudomonas aeruginosa
-
-
-
Pseudomonas aeruginosa PAK
-
-
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Synonyms

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
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

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
0.0249
-
 at pH 7.5 and 22°C Pseudomonas aeruginosa 4-(4-oxo-3,4-dihydroquinazolin-2-yl)butanoic acid
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
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
0.135
-
 at pH 7.5 and 22°C Pseudomonas aeruginosa 3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanoic acid
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
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