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Literature summary for 3.1.3.48 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

Inhibitors Comment Organism Structure
(3S,6S,9R)-3,6-dimethyl-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
Mycobacterium tuberculosis
(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
(3S,9R)-3-(4-hydroxybenzyl)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
Mycobacterium tuberculosis
(6R)-6-[(R)-phenyl(phenylamino)methyl]-1,4-diazepane-2,5-dione
-
Mycobacterium tuberculosis
(9R)-9-[(R)-furan-2-yl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
Mycobacterium tuberculosis
(9R)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione
-
Mycobacterium tuberculosis
benzyl (3R,6S)-4,9-dioxo-3-[(R)-phenyl(phenylamino)methyl]-1,5-diazonane-6-carboxylate
-
Mycobacterium tuberculosis
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

Organism UniProt Comment Textmining
Mycobacterium tuberculosis
-
-
-

Reaction

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

Synonyms

Synonyms Comment Organism
MPtpA
-
Mycobacterium tuberculosis
protein tyrosine phosphatase A
-
Mycobacterium tuberculosis

Temperature Optimum [°C]

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

pH Optimum

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
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
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
0.0855
-
(9R)-9-[(R)-phenyl(phenylamino)methyl]-1,4,7-triazecane-2,5,8-trione pH 7.5, 25°C Mycobacterium tuberculosis
0.14
-
(6R)-6-[(R)-phenyl(phenylamino)methyl]-1,4-diazepane-2,5-dione pH 7.5, 25°C Mycobacterium tuberculosis
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
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
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

General Information Comment Organism
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