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Literature summary extracted from

  • Chandra, K.; Dutta, D.; Das, A.K.; Basak, A.
    Design, synthesis and inhibition activity of novel cyclic peptides against protein tyrosine phosphatase A from Mycobacterium tuberculosis (2010), Bioorg. Med. Chem., 18, 8365-8373.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.3.48 (3S,6S,9R)-3,6-dimethyl-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
 Mycobacterium tuberculosis
3.1.3.48 (3S,6S,9R,12R)-3,6,9-trimethyl-12-[(R)-phenyl(phenylamino)methyl]-1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone
-
 Mycobacterium tuberculosis
3.1.3.48 (3S,9R)-3-(4-hydroxybenzyl)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
 Mycobacterium tuberculosis
3.1.3.48 (6R)-6-[(R)-phenyl(phenylamino)methyl]-1,4-diazepane-2,5-dione
-
 Mycobacterium tuberculosis
3.1.3.48 (9R)-9-[(R)-furan-2-yl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
 Mycobacterium tuberculosis
3.1.3.48 (9R)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
 Mycobacterium tuberculosis
3.1.3.48 benzyl (3R,6S)-4,9-dioxo-3-[(R)-phenyl(phenylamino)methyl]-1,5-diazonane-6-carboxylate
-
 Mycobacterium tuberculosis
3.1.3.48 additional information design of structure based cyclic peptide inhibitors, synthesis involves a crucial intramolecular transamidation via a ring opening reaction. All the compounds show moderate to good inhibitory activities against MPtpA in micromolar concentrations, enzyme docking study, overview Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
3.1.3.48 Mycobacterium tuberculosis
-
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
3.1.3.48 [a protein]-tyrosine phosphate + H2O = [a protein]-tyrosine + phosphate mechanism of the dephosphorylation catalysed by MptpA Mycobacterium tuberculosis
a

Synonyms

EC Number Synonyms Comment Organism
3.1.3.48 MPtpA
-
 Mycobacterium tuberculosis
3.1.3.48 protein tyrosine phosphatase A
-
 Mycobacterium tuberculosis

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.1.3.48 25
-
 assay at Mycobacterium tuberculosis

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.1.3.48 7.5
-
 assay at Mycobacterium tuberculosis

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.1.3.48 0.008
-
 (3S,9R)-3-(4-hydroxybenzyl)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione pH 7.5, 25°C Mycobacterium tuberculosis
3.1.3.48 0.0363
-
 benzyl (3R,6S)-4,9-dioxo-3-[(R)-phenyl(phenylamino)methyl]-1,5-diazonane-6-carboxylate pH 7.5, 25°C Mycobacterium tuberculosis
3.1.3.48 0.0855
-
 (9R)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione pH 7.5, 25°C Mycobacterium tuberculosis
3.1.3.48 0.14
-
 (6R)-6-[(R)-phenyl(phenylamino)methyl]-1,4-diazepane-2,5-dione pH 7.5, 25°C Mycobacterium tuberculosis
3.1.3.48 0.199
-
 (3S,6S,9R,12R)-3,6,9-trimethyl-12-[(R)-phenyl(phenylamino)methyl]-1,4,7,10-tetraazacyclotridecane-2,5,8,11-tetrone pH 7.5, 25°C Mycobacterium tuberculosis
3.1.3.48 0.215
-
 (9R)-9-[(R)-furan-2-yl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione pH 7.5, 25°C Mycobacterium tuberculosis
3.1.3.48 0.22
-
 (3S,6S,9R)-3,6-dimethyl-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione pH 7.5, 25°C Mycobacterium tuberculosis

General Information

EC Number General Information Comment Organism
3.1.3.48 metabolism MPtpA is a signalling protein belonging to the tyrosine phosphatase superfamily, and is involved in phagocytosis and is active in virulent mycobacterial form Mycobacterium tuberculosis