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Literature summary for 2.4.2.30 extracted from

  • Arnoldo, A.; Curak, J.; Kittanakom, S.; Chevelev, I.; Lee, V.T.; Sahebol-Amri, M.; Koscik, B.; Ljuma, L.; Roy, P.J.; Bedalov, A.; Giaever, G.; Nislow, C.; Merrill, R.A.; Lory, S.; Stagljar, I.
    Identification of small molecule inhibitors of Pseudomonas aeruginosa exoenzyme S using a yeast phenotypic screen (2008), PLoS Genet., 4, e1000005.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.4.2.30

Activating Compound

Activating Compound Comment Organism Structure
Bmh1p a yeast homologue of the human FAS, acts as an activating ExoS cofactor, overview Pseudomonas aeruginosa

Application

Application Comment Organism
drug development the enzyme can be a target for anti-bacterial treatment Pseudomonas aeruginosa

Inhibitors

Inhibitors Comment Organism Structure
0469-0796 restores yeast growth after treatment with ExoS Pseudomonas aeruginosa
4296-1011 restores yeast growth after treatment with ExoS Pseudomonas aeruginosa
diosmin restores yeast growth after treatment with ExoS Pseudomonas aeruginosa
E216-5303 restores yeast growth after treatment with ExoS Pseudomonas aeruginosa
everninic acid restores yeast growth after treatment with ExoS Pseudomonas aeruginosa
exosin a small molecule inhibitor, that modulates ExoS ADP-ribosyltransferase activity in vitro, suggesting the inhibition is direct. Exosin and two of its analogues display a significant protective effect against Pseudomonas infection in vivo, competitive against NAD+ Pseudomonas aeruginosa
flavokawain B restores yeast growth after treatment with ExoS Pseudomonas aeruginosa
additional information identification of small molecule inhibitors of Pseudomonas aeruginosa exoenzyme S using a yeast phenotypic screening, overview Pseudomonas aeruginosa

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.009
-
 NAD+ pH 6.0, 30°C, in absence of exosin Pseudomonas aeruginosa
0.03
-
 NAD+ pH 6.0, 30°C, in presence of exosin Pseudomonas aeruginosa

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+
-
 Pseudomonas aeruginosa

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Pseudomonas aeruginosa ExoS is a toxin playing a pivotal role during Pseudomonas aeruginosa infections, it is a virulence factor causing growth inhibition in Saccharomyces cerevisiae. Exoenzyme S ADP-ribosylates identical targets in both human and yeast ?
-
 ?
NAD+ + (ADP-D-ribosyl)n-acceptor Pseudomonas aeruginosa
-
 nicotinamide + (ADP-D-ribosyl)n+1-acceptor + H+
-
 ?

Organism

Organism UniProt Comment Textmining
Pseudomonas aeruginosa
-
 strains PAK and PA14
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information ExoS is a toxin playing a pivotal role during Pseudomonas aeruginosa infections, it is a virulence factor causing growth inhibition in Saccharomyces cerevisiae. Exoenzyme S ADP-ribosylates identical targets in both human and yeast Pseudomonas aeruginosa ?
-
 ?
NAD+ + (ADP-D-ribosyl)n-acceptor
-
 Pseudomonas aeruginosa nicotinamide + (ADP-D-ribosyl)n+1-acceptor + H+
-
 ?
NAD+ + Ras2p Ras2p is a yeast protein, activity absolutely requires the yeast protein Bmh1p Pseudomonas aeruginosa nicotinamide + (ADP-D-ribosyl)-Ras2p + H+
-
 ?

Synonyms

Synonyms Comment Organism
ADP-ribosyltransferase
-
 Pseudomonas aeruginosa
ADPRT
-
 Pseudomonas aeruginosa
exoenzyme S
-
 Pseudomonas aeruginosa
ExoS
-
 Pseudomonas aeruginosa

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
 assay at Pseudomonas aeruginosa

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6
-
 assay at Pseudomonas aeruginosa

Cofactor

Cofactor Comment Organism Structure
additional information Bmh1p, a yeast homologue of the human FAS, acts as an ExoS cofactor, overview Pseudomonas aeruginosa
NAD+
-
 Pseudomonas aeruginosa

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.033
-
 exosin pH 6.0, 30°C Pseudomonas aeruginosa

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.003
-
 pH 6.0, 30°C Pseudomonas aeruginosa diosmin
0.006
-
 pH 6.0, 30°C Pseudomonas aeruginosa 4296-1011
0.021
-
 pH 6.0, 30°C Pseudomonas aeruginosa everninic acid
0.023
-
 pH 6.0, 30°C Pseudomonas aeruginosa E216-5303