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Literature summary extracted from

  • Buzder-Lantos, P.; Bockstael, K.; Anne, J.; Herdewijn, P.
    Substrate based peptide aldehyde inhibits bacterial type I signal peptidase (2009), Bioorg. Med. Chem. Lett., 19, 2880-2883.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.21.89 drug development type I signal peptidase is a potential target for the development of novel antibacterial agents Staphylococcus aureus
3.4.21.89 drug development bacterial type I signal peptidase is a potential target for the development of antibacterial agents Staphylococcus aureus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.89 decanoyl-AKAPSKIDD complete inhibition at 0.2 mM Staphylococcus aureus
3.4.21.89 decanoyl-LTPTAKAPS 7.1% inhibition at 0.2 mM Staphylococcus aureus
3.4.21.89 LTPTAKAPSKIDD 21.6% inhibition at 0.2 mM Staphylococcus aureus
3.4.21.89 additional information a substrate based peptide aldehyde inhibits signal peptidases with a lower IC(50) value than other lipopeptides Staphylococcus aureus
3.4.21.89 N-[(2S)-4-[(2S)-1-decanoylpyrrolidin-2-yl]-2-(1-hydroxyethyl)-4-oxobutanoyl]-L-alanyl-N1-[(2S)-1-oxopropan-2-yl]-L-aspartamide i.e. decanoyl-PTANA-aldehyde, inhibition by the synthetic substrate-based peptide aldehyde, overview. The length of the core lipopeptide can be reduced by removing several amino acids from both termini. Conversion of this peptide to an aldehyde. The signal peptide consists of three domains, a positively charged N-terminal domain, n-region, a hydrophobic middle domain, which contains usually 7-15 amino acids forming an alpha-helix, h-region, and a C-terminal domain, c-region, which is responsible for substrate recognition Staphylococcus aureus

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.89 Staphylococcus aureus
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.89 additional information the enzyme shows a unique Ser/Lys dyad protease mechanism Staphylococcus aureus ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.89 bacterial type I signal peptidase
-
 Staphylococcus aureus
3.4.21.89 Spase I
-
 Staphylococcus aureus
3.4.21.89 SpsB
-
 Staphylococcus aureus
3.4.21.89 type I signal peptidase
-
 Staphylococcus aureus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.89 additional information
-
 conversion of a substrate based peptide to an aldehyde results in a molecule with an IC(50) value of 0.09 micromol Staphylococcus aureus additional information
3.4.21.89 0.00009
-
 pH not specified in the publication, temperature not specified in the publication Staphylococcus aureus N-[(2S)-4-[(2S)-1-decanoylpyrrolidin-2-yl]-2-(1-hydroxyethyl)-4-oxobutanoyl]-L-alanyl-N1-[(2S)-1-oxopropan-2-yl]-L-aspartamide