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Literature summary for 2.7.7.65 extracted from

  • Sambanthamoorthy, K.; Sloup, R.E.; Parashar, V.; Smith, J.M.; Kim, E.E.; Semmelhack, M.F.; Neiditch, M.B.; Waters, C.M.
    Identification of small molecules that antagonize diguanylate cyclase enzymes to inhibit biofilm formation (2012), Antimicrob. Agents Chemother., 56, 5202-5211.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.7.65

Cloned(Commentary)

Cloned (Comment) Organism
expressed as a His-tagged fusion protein in Escherichia coli Pseudomonas aeruginosa
residues 142-579 are expressed as a His-tagged fusion protein in Escherichia coli Vibrio cholerae

Protein Variants

Protein Variants Comment Organism
D484E RXXD allosteric inhibition site of the protein is mutated (VC2370(142)-D484E) because it is shown, using HPLC-MS-MS, that c-di-GMP copurifies with native VC2370. Mutation of this RXXD site prevents c-di-GMP copurification. Also, mutation of the site ensures that c-di-GMP produced during the in vitro reaction is not able to inhibit enzyme activity Vibrio cholerae
R242A mutant sows activity and is used as a target enzyme. Mutation locks the enzyme in a constitutively active state Pseudomonas aeruginosa

Inhibitors

Inhibitors Comment Organism Structure
4(R)-1-(benzylsulfonyl)-3-phenoxy-2-propanol
-
 Pseudomonas aeruginosa
4(R)-1-(benzylsulfonyl)-3-phenoxy-2-propanol
-
 Vibrio cholerae
4(S)-1-(benzylsulfonyl)-3-phenoxy-2-propanol
-
 Pseudomonas aeruginosa
4(S)-1-(benzylsulfonyl)-3-phenoxy-2-propanol
-
 Vibrio cholerae
N-(((2-phenylethyl)amino)carbonothioyl)benzamide
-
 Pseudomonas aeruginosa
N-(((2-phenylethyl)amino)carbonothioyl)benzamide significantly reduces the total concentration of c-di-GMP in Vibrio cholerae Vibrio cholerae
N-(4-anilinophenyl)benzamide
-
 Pseudomonas aeruginosa
N-(4-anilinophenyl)benzamide significantly reduces the total concentration of c-di-GMP in Vibrio cholerae Vibrio cholerae
N-(4-bromophenyl)-3-phenylpropanamide
-
 Pseudomonas aeruginosa
N-(4-bromophenyl)-3-phenylpropanamide
-
 Vibrio cholerae
N-(4-chlorophenyl)-3-phenylpropanamide
-
 Pseudomonas aeruginosa
N-(4-chlorophenyl)-3-phenylpropanamide
-
 Vibrio cholerae
N-(4-methoxyphenyl)-3-phenylpropanamide
-
 Pseudomonas aeruginosa
N-(4-methoxyphenyl)-3-phenylpropanamide
-
 Vibrio cholerae
N-(4-phenoxyphenyl)-2-thiophenecarboxamide
-
 Pseudomonas aeruginosa
N-(4-phenoxyphenyl)-2-thiophenecarboxamide
-
 Vibrio cholerae

Organism

Organism UniProt Comment Textmining
Pseudomonas aeruginosa
-
-
-
Vibrio cholerae Q9KPJ7
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GTP
-
 Pseudomonas aeruginosa cyclic di-3',5'-guanylate + diphosphate
-
 ?
GTP
-
 Vibrio cholerae cyclic di-3',5'-guanylate + diphosphate
-
 ?

Synonyms

Synonyms Comment Organism
DGC
-
 Vibrio cholerae
diguanylate cyclase
-
 Pseudomonas aeruginosa
diguanylate cyclase
-
 Vibrio cholerae
VC2370
-
 Vibrio cholerae

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
20
-
 assay at Pseudomonas aeruginosa
20
-
 assay at Vibrio cholerae

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
 assay at Pseudomonas aeruginosa
7.5
-
 assay at Vibrio cholerae

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0009
-
 pH 7.5, 20°C Vibrio cholerae N-(((2-phenylethyl)amino)carbonothioyl)benzamide
0.001
-
 pH 7.5, 20°C Vibrio cholerae N-(4-anilinophenyl)benzamide
0.0029
-
 pH 7.5, 20°C Vibrio cholerae 4(R)-1-(benzylsulfonyl)-3-phenoxy-2-propanol
0.0066
-
 pH 7.5, 20°C Vibrio cholerae N-(4-chlorophenyl)-3-phenylpropanamide
0.0069
-
 pH 7.5, 20°C Vibrio cholerae N-(4-bromophenyl)-3-phenylpropanamide
0.008
-
 pH 7.5, 20°C Vibrio cholerae N-(4-phenoxyphenyl)-2-thiophenecarboxamide
0.00817
-
 pH 7.5, 20°C Pseudomonas aeruginosa 4(R)-1-(benzylsulfonyl)-3-phenoxy-2-propanol
0.0098
-
 pH 7.5, 20°C Vibrio cholerae N-(4-methoxyphenyl)-3-phenylpropanamide
0.0122
-
 pH 7.5, 20°C Pseudomonas aeruginosa N-(((2-phenylethyl)amino)carbonothioyl)benzamide
0.0135
-
 pH 7.5, 20°C Pseudomonas aeruginosa N-(4-chlorophenyl)-3-phenylpropanamide
0.0175
-
 pH 7.5, 20°C Pseudomonas aeruginosa N-(4-bromophenyl)-3-phenylpropanamide
0.0178
-
 pH 7.5, 20°C Pseudomonas aeruginosa N-(4-anilinophenyl)benzamide
0.0189
-
 pH 7.5, 20°C Pseudomonas aeruginosa N-(4-phenoxyphenyl)-2-thiophenecarboxamide
0.03
-
 pH 7.5, 20°C Pseudomonas aeruginosa N-(4-methoxyphenyl)-3-phenylpropanamide