Detailed view for Rv0153c

Basic information

TDR Targets ID: 6950
Mycobacterium tuberculosis, Phosphotyrosine protein phosphatase PTPB (protein-tyrosine-phosphatase) (PTPase)
Source Database / ID:  Tuberculist 

pI: 6.1425 | Length (AA): 276 | MW (Da): 30154 | Paralog Number: 0

Signal peptide: N | GPI Anchor: | Predicted trans-membrane segments: 0

Druggability Group : DG1

Targets have been classified into druggability groups (DG) according to their druggability score in network driven prioritizations. DGs range from 1 to 5; the higher the group number, the higher the chance of the target to be druggable

Pfam domains

PF13350   Tyrosine phosphatase family

Gene Ontology

Mouse over links to read term descriptions.
GO:0016791   phosphoric monoester hydrolase activity  
GO:0016311   dephosphorylation  

Metabolic Pathways

This gene is not mapped to any metabolic pathway in KEGG.

Structural information

Modbase 3D models:

There is 1 model calculated for this protein. More info on this model, including the model itself is available at: Modbase

Target Beg Target End Template Template Beg Template End Identity Evalue Model Score MPQS zDope
4 276 2oz5 (A) 4 276 99.99 0 1 2.22523 -1.77

Help me make sense of these data.

Target Beg: first modeled residue
Target End: last modeled residue
Template: template structure used for modelling (PDB accession and chain)
Template Beg: first template residue in target-template alignment
Template End: last template residue in target-template alignment
Identity: sequence identity
Evalue: E value for target-template hit
Model Score: GA341 score (>0.7 for reliable model)
MPQS: ModPipe Quality Score (>1.1 for reliable model)
zDope: zDope Score (negative for reliable model)

A more detailed description of these scores is available at the Modbase Model Evaluation Help Pages, and in the papers referenced therein.

PDB Structures:

PDB tag
  • 1YWF:
  • Resolution Method # Atoms # Residues Dep. Date Pub. Date Mod. Date
PDB tag
  • 2OZ5:
  • Resolution Method # Atoms # Residues Dep. Date Pub. Date Mod. Date

Expression

Upregulation Percent Ranking Stage Dataset
Mid 40-60% percentile Dormant phase. hasan
Upregulation Percent Ranking Stage Dataset
Lower 20-40% percentile Dormant phase. murphy
Show/Hide expression data references
  • murphy Identification of gene targets against dormant phase Mycobacterium tuberculosis infections.
  • hasan Prioritizing genomic drug targets in pathogens: application to Mycobacterium tuberculosis.

Orthologs

Ortholog group members (OG5_132308)

Species Accession Gene Product
Candida albicans CaO19.8208   similar to S. cerevisiae YDL057W
Candida albicans CaO19.577   similar to S. cerevisiae YDL057W
Leishmania donovani LdBPK_220120.1   phosphoinositide phosphatase
Leishmania infantum LinJ.22.0120   phosphoinositide phosphatase, putative;with=GeneDB:LmjF22.0250
Leishmania major LmjF.22.0250   phosphoinositide phosphatase
Leishmania mexicana LmxM.22.0250   hypothetical protein, unknown function
Mycobacterium tuberculosis Rv0153c   Phosphotyrosine protein phosphatase PTPB (protein-tyrosine-phosphatase) (PTPase)
Mycobacterium ulcerans MUL_4739   phosphotyrosine protein phosphatase PtpB
Oryza sativa 4339458   Os05g0539500
Saccharomyces cerevisiae YDL057W   hypothetical protein
Schmidtea mediterranea mk4.006237.02  
Schmidtea mediterranea mk4.023211.00  
Trichomonas vaginalis TVAG_320290   conserved hypothetical protein

Essentiality

No essentiality data collected for this gene and/or its orthologs.

Phenotypes and Validation (curated)

We have no manually annotated phenotypes for this target. What does this mean? / Care to help?

In TDR Targets, information about phenotypes that are caused by drugs, or by genetic manipulation of cells (e.g. gene knockouts or knockdowns) is manually curated from the literature. These descriptions help to describe the potential of the target for drug development. If no information is available for this gene or if the information is incomplete, this may mean that i) the papers containing this information either appeared after the curation effort for this organism was carried out or they were inadvertently missed by curators; or that ii) the curation effort for this organism has not yet started.

In any case, if you have information about papers containing relevant validation data for this target, please contact us.

Annotated validation

No validation data for this target

Associated compounds / Druggability

Druggability index (range: 0 to 1): 0.2

Known modulators for this target

Compound Source Reference
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Predicted associations

By orthology with druggable targets
Non orthologous druggable targets
By sequence similarity to non orthologous druggable targets
No additional associated druggable targets
Obtained from network model

Ranking Plot

Putative Drugs List

Compound Raw Global Species
0.0260297 1 1
0.0302 0.5904 0.8691
0.018 0.5085 0.5085
0.0187 0.4515 0.7467
0.0196 0.3415 0.7669
0.0289 1 0.5
0.0201 0.2589 1
0.0212 0.2774 1
0.0201 0.2589 1
0.0189 0.5755 0
0.0229 0.7258 1
0.0187 0.4839 0.613
0.0189 0.5686 0.5686
0.0187 0.542 1
0.0188 1 0.5
0.0183 0.459 1
0.0201 0.2589 1
0.0219 0.4586 0.5
0.0188 0.5754 0
0.019 0.4461 1
0.0188 0.5755 0
0.0188 0.3031 0.3278
0.0197 0.31 0.5817
0.0184 0.6272 0.5
0.0229 0.9958 1
0.0183 0.6173 0.5
0.0229 0.657 1
0.0194 1 0.5
0.0201 0.2589 1
0.0626 0.2592 0.3192
0.0559 0.4836 1
0.0185 0.2753 0.5
0.0197 0.2594 1
0.0229 0.5 0.5
0.0327216 1 0.5
0.0195 1 1
0.019 0.5757 0
0.018 0.5085 0.5085
0.0187 0.2716 0.2812
0.0191 0.3145 0.783
0.0194 0.5842 0.5816
0.0188 1 1
0.0229 0.5 0.5
0.0189 0.5598 1
0.0229 0.2643 1
0.0221 0.2787 0.6437
0.0188 0.5755 0
0.0185 0.3071 1
0.0338 0.9728 1
0.0195 0.4564 0.5
0.0188 1 1
0.0185 0.2753 0.5
0.0221 0.2658 1
0.0212 0.2774 1
0.018 0.5085 0.5085
0.0189 0.5796 0
0.0327216 1 0.5
0.0203 0.4533 0.475
0.019 0.2636 1
0.0278 0.3059 0.6769
0.019 0.6647 1
0.0184 0.5499 0
0.0184 0.5641 0

Assayability

Assay information

  • Inhibitory activity against MPTPB ChEMBL
  • Inhibitory activity against MPTPB
  • Inhibition of Mycobacterium tuberculosis ptpb ChEMBL
  • Inhibition of Mycobacterium tuberculosis ptpb
  • ChEMBL
  • Inhibition of N-terminal histidine-tagged Mycobacterium tuberculosis PTPB expressed in Escherichia coli BL21 (DE3) after 45 mins by fluorescence assay
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis PTPB at 100 uM after 20 mins by ELISA
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis PTPB expressed in Escherichia coli after 5 mins by microplate spectrophotometer analysis
  • ChEMBL
  • Non-competitive inhibition of Mycobacterium tuberculosis N-terminal His6-tagged PTPB assessed as production of p-nitrophenol from pNPP substrate by Lineweaver-Burk plot analysis
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis N-terminal His6-tagged PTPB preincubated with compound for 30 mins before pNPP substrate addition by microplate spectrophotometer analysis
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis PTPB expressed in mouse RAW 264.7 cells assessed as restoration of IFN gamma-induced ERK1/ERK2 phosphorylation at 10 uM after 30 mins by Western blotting
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis N-terminal His6-tagged PTPB
  • ChEMBL
  • Competitive inhibition of Mycobacterium tuberculosis N-terminal His6-tagged PTPB assessed as production of p-nitrophenol from pNPP substrate by Lineweaver-Burk plot analysis
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis N-terminal His6-tagged PTPB at 20 uM using pNPP as substrate
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis PTPB expressed in mouse RAW 264.7 cells assessed as restoration of IFN gamma-induced ERK1/ERK2 phosphorylation at 15 uM after 30 mins by Western blotting
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis PTPB expressed in mouse RAW 264.7 cells assessed as restoration of IFN gamma-induced ERK1/ERK2 phosphorylation after 30 mins by Western blotting
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis PTPB expressed in mouse RAW 264.7 cells assessed as restoration of IFN gamma-induced ERK1/ERK2 phosphorylation at 5 to 10 uM after 30 mins by Western blotting
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis ptpB
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis PTPB
  • ChEMBL
  • Competitive inhibition of Mycobacterium tuberculosis H37Rv PTP-B expressed in Escherichia coli DE3 using p-nitrophenyl phosphate as substrate preincubated for 10 mins prior substrate addition measured after 5 mins by Lineweaver-Burk plot analysis
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis PTP-B using p-nitrophenyl phosphate as substrate at 25 uM measured for 10 mins by spectrofluorimetry
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis PTP-B using p-nitrophenyl phosphate as substrate measured for 10 mins by spectrofluorimetry
  • ChEMBL
  • Competitive inhibition of Mycobacterium tuberculosis PTP-B using p-nitrophenyl phosphate as substrate measured for 10 mins by Lineweaver-Burk plot analysis
  • ChEMBL
  • Inhibition of Mycobacterium tuberculosis protein tyrosine phosphatase B

Reagent availability

No reagent availability information for this target.

Bibliographic References

27 literature references were collected for this gene.

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Gene identifier Rv0153c (Mycobacterium tuberculosis), Phosphotyrosine protein phosphatase PTPB (protein-tyrosine-phosphatase) (PTPase)
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