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Literature summary for 3.1.3.3 extracted from

  • Arora, G.; Tiwari, P.; Mandal, R.S.; Gupta, A.; Sharma, D.; Saha, S.; Singh, R.
    High throughput screen identifies small molecule inhibitors specific for Mycobacterium tuberculosis phosphoserine phosphatase (2014), J. Biol. Chem., 289, 25149-25165.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.3.3

Activating Compound

Activating Compound Comment Organism Structure
Triton X-100 presence of 0.01% Triton X-100 enhances isoform SerB2 activity by 15-20% Mycobacterium tuberculosis

Application

Application Comment Organism
analysis development of a malachite green-based high throughput assay system to identify isoform SerB2 inhibitors Mycobacterium tuberculosis

Cloned(Commentary)

Cloned (Comment) Organism
expression in Eschericia coli Mycobacterium tuberculosis

Crystallization (Commentary)

Crystallization (Comment) Organism
construction of a homology model and molecular docking of O-phospho-L-serine. Residues Asp185, Ser273, Lys-318, and Asp-341 are part of the substrate binding pocket. Val186 and Ser188 might also interact with O-phospho-L-serine Mycobacterium tuberculosis

Protein Variants

Protein Variants Comment Organism
D185G complete loss of activity Mycobacterium tuberculosis
D341G about 10% residual activity, no change in secondary structure compared to wild-type Mycobacterium tuberculosis
K318E complete loss of activity Mycobacterium tuberculosis
S188A activity similar to wild-type Mycobacterium tuberculosis
S273A about 30% residual activity, no change in secondary structure compared to wild-type Mycobacterium tuberculosis
V186Q about 55% residual activity Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
Clorobiocin displays bactericidal activity and kills intracellular bacteria in a dose-dependent manner, highly specific in the ability to inhibit isoform SerB2 in comparison with human phosphoserine phosphatase Mycobacterium tuberculosis
DL-2-amino-3-phosphonopropionic acid
-
 Mycobacterium tuberculosis
rosaniline displays bactericidal activity and kills intracellular bacteria in a dose-dependent manner Mycobacterium tuberculosis
sodium orthovanadate
-
 Mycobacterium tuberculosis
Zn2+
-
 Mycobacterium tuberculosis

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0927
-
 O-phospho-L-serine pH 7.4, 37°C Mycobacterium tuberculosis

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ optimum activity upon inclusion of 5 mM Mg2+ or Mn2+ ions in the assay buffer Mycobacterium tuberculosis
Mn2+ optimum activity upon inclusion of 5 mM Mg2+ or Mn2+ ions in the assay buffer Mycobacterium tuberculosis

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
45000
-
 x * 45000, SDS-PAGE, His-tagged recombinant protein Mycobacterium tuberculosis

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis O53289 isoform SerB2
-
Mycobacterium tuberculosis ATCC 25618 O53289 isoform SerB2
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
additional information no substrate: O-phospho-L-threonine Mycobacterium tuberculosis ?
-
 ?
additional information no substrate: O-phospho-L-threonine Mycobacterium tuberculosis ATCC 25618 ?
-
 ?
O-phospho-L-serine + H2O
-
 Mycobacterium tuberculosis L-serine + phosphate
-
 ?
O-phospho-L-serine + H2O
-
 Mycobacterium tuberculosis ATCC 25618 L-serine + phosphate
-
 ?

Subunits

Subunits Comment Organism
? x * 45000, SDS-PAGE, His-tagged recombinant protein Mycobacterium tuberculosis

Synonyms

Synonyms Comment Organism
SerB2
-
 Mycobacterium tuberculosis

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.15
-
 O-phospho-L-serine pH 7.4, 37°C Mycobacterium tuberculosis

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.5
-
-
 Mycobacterium tuberculosis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0168
-
 pH 7.4, 37°C Mycobacterium tuberculosis Clorobiocin
0.0315
-
 pH 7.4, 37°C Mycobacterium tuberculosis rosaniline
0.458
-
 pH 7.4, 37°C Mycobacterium tuberculosis sodium orthovanadate
0.67
-
 pH 7.4, 37°C Mycobacterium tuberculosis DL-2-amino-3-phosphonopropionic acid

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
0.00159
-
 O-phospho-L-serine pH 7.4, 37°C Mycobacterium tuberculosis