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Literature summary for 2.7.1.189 extracted from

  • Zhu, J.; Hixon, M.S.; Globisch, D.; Kaufmann, G.F.; Janda, K.D.
    Mechanistic insights into the LsrK kinase required for autoinducer-2 quorum sensing activation (2013), J. Am. Chem. Soc., 135, 7827-7830.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
1,2-dihydroxydecane-3,4-dione
-
Salmonella enterica
1,2-dihydroxyheptane-3,4-dione
-
Salmonella enterica
1,2-dihydroxyhexane-3,4-dione weak inhibition Salmonella enterica
1,2-dihydroxyoctane-3,4-dione
-
Salmonella enterica

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
additional information
-
additional information the bi-substrate kinetic mechanism is rapid equilibrium ordered, Michaelis-Menten kinetics, overview Salmonella enterica
0.15
-
ATP pH and temperature not specified in the publication Salmonella enterica
0.27
-
1,2-dihydroxyoctane-3,4-dione pH and temperature not specified in the publication Salmonella enterica
1
-
4,5-dihydroxypentane-2,3-dione pH and temperature not specified in the publication Salmonella enterica
1.1
-
1,2-dihydroxyhexane-3,4-dione pH and temperature not specified in the publication Salmonella enterica
1.4
-
1,2-dihydroxyheptane-3,4-dione pH and temperature not specified in the publication Salmonella enterica

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Salmonella enterica

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + (4S)-4,5-dihydroxypentane-2,3-dione Salmonella enterica the kinase LsrK phosphorylates C5 of the open form of the substrate ADP + 2-hydroxy-3,4-dioxopentyl phosphate
-
?

Organism

Organism UniProt Comment Textmining
Salmonella enterica
-
serovar Typhimurium, gene lsrK
-

Reaction

Reaction Comment Organism Reaction ID
ATP + (S)-4,5-dihydroxypentane-2,3-dione = ADP + (S)-4-hydroxypentane-2,3-dione 5-phosphate apid equilibrium ordered mechanism with ATP binding first Salmonella enterica

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + (4S)-4,5-dihydroxypentane-2,3-dione the kinase LsrK phosphorylates C5 of the open form of the substrate Salmonella enterica ADP + 2-hydroxy-3,4-dioxopentyl phosphate
-
?
ATP + 1,2-dihydroxyheptane-3,4-dione
-
Salmonella enterica ADP + 2-hydroxy-3,4-dioxoheptyl phosphate
-
?
ATP + 1,2-dihydroxyhexane-3,4-dione
-
Salmonella enterica ADP + 2-hydroxy-3,4-dioxohexyl phosphate
-
?
ATP + 1,2-dihydroxyoctane-3,4-dione
-
Salmonella enterica ADP + 2-hydroxy-3,4-dioxooctyl phosphate
-
?
ATP + 4,5-dihydroxypentane-2,3-dione the kinase LsrK phosphorylates C5 of the open form of the substrate Salmonella enterica ADP + 2-hydroxy-3,4-dioxopentyl phosphate
-
?
additional information no activity with 1,2-dihydroxy-6-methylheptane-3,4-dione Salmonella enterica ?
-
?

Synonyms

Synonyms Comment Organism
LsrK kinase
-
Salmonella enterica

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
1.5
-
1,2-dihydroxyoctane-3,4-dione pH and temperature not specified in the publication Salmonella enterica
5.8
-
1,2-dihydroxyhexane-3,4-dione pH and temperature not specified in the publication Salmonella enterica
5.8
-
1,2-dihydroxyheptane-3,4-dione pH and temperature not specified in the publication Salmonella enterica
7.6
-
ATP pH and temperature not specified in the publication Salmonella enterica
7.6
-
4,5-dihydroxypentane-2,3-dione pH and temperature not specified in the publication Salmonella enterica

Cofactor

Cofactor Comment Organism Structure
ATP
-
Salmonella enterica

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.005
-
pH and temperature not specified in the publication Salmonella enterica 1,2-dihydroxyoctane-3,4-dione
0.0053
-
pH and temperature not specified in the publication Salmonella enterica 1,2-dihydroxyheptane-3,4-dione
0.025
-
pH and temperature not specified in the publication Salmonella enterica 1,2-dihydroxydecane-3,4-dione
0.05
-
above, pH and temperature not specified in the publication Salmonella enterica 1,2-dihydroxyhexane-3,4-dione

General Information

General Information Comment Organism
metabolism the enzyme is involved in quorum sensing, one type of bacterial cell-to-cell communication, which co-ordinates bacterial behaviors within a population. The communication is mediated by a plethora of diffusible signaling molecules, called autoinducers. AI-2 signaling is carried out by the Lsr proteins Salmonella enterica
additional information analysis of structure-activity relationship, overview Salmonella enterica
physiological function in enteric bacteria, the kinase LsrK catalyzes the phosphorylation of the C5-hydroxyl group in the linear form of 4,5-dihydroxypentane-2,3-dione, the precursor of the type II bacterial quorum sensing molecule (AI-2), the enzyme is required for phosphorylation is required for autoinducer-2 sequestration in the cytoplasm and subsequent derepression of AI-2 related genes necessary for quorum development and autoinducer-2 quorum sensing activation, catalytic mechanism, overview. Phosphorylated AI-2 (phospho-DPD) binds and inactivates the transcriptional repressor protein LsrR thereby inducing the expression of the lsr operon and potentially other LsrR-regulated, QS-related genes Salmonella enterica