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Literature summary for 2.7.11.1 extracted from

  • Molle, V.; Reynolds, R.C.; Alderwick, L.J.; Besra, G.S.; Cozzone, A.J.; Fuetterer, K.; Kremer, L.
    EmbR2, a structural homologue of EmbR, inhibits the Mycobacterium tuberculosis kinase/substrate pair PknH/EmbR (2008), Biochem. J., 410, 309-317.
    View publication on PubMed

Application

Application Comment Organism
molecular biology EmbR2 is a regulator of PknH activation, thus directly participating in the control of the PknH/EmbR pair Mycobacterium tuberculosis

Inhibitors

Inhibitors Comment Organism Structure
EmbR2 EmbR2, a homologue of EmbR, inhibits PknH by binding to at least two of the three threonine sites known to undergo autophosphorylation in PknH which leads to a dose-response inhibition of the autokinase activity. Moreover, EmbR2 inhibits PknH-dependent phosphorylation of EmbR in a dose-dependent manner Mycobacterium tuberculosis
O6-cyclohexylmethylguanine
-
Mycobacterium tuberculosis

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis P9WI71
-
-
Mycobacterium tuberculosis H37Rv P9WI71
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein PknH autophosphorylates itsself Mycobacterium tuberculosis

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + EmbR PknH phosphorylates the transcriptional regulator EmbR, but not its homologue EmbR2 Mycobacterium tuberculosis ADP + phosphorylated-EmbR
-
?
ATP + EmbR PknH phosphorylates the transcriptional regulator EmbR, but not its homologue EmbR2 Mycobacterium tuberculosis H37Rv ADP + phosphorylated-EmbR
-
?

Synonyms

Synonyms Comment Organism
mycobacterial serine/threonine protein kinase
-
Mycobacterium tuberculosis
PknH
-
Mycobacterium tuberculosis
serine-threonine kinase
-
Mycobacterium tuberculosis
StpK
-
Mycobacterium tuberculosis

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Mycobacterium tuberculosis

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
assay at Mycobacterium tuberculosis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0011
-
-
Mycobacterium tuberculosis EmbR2
0.005
-
-
Mycobacterium tuberculosis O6-cyclohexylmethylguanine