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Literature summary for 3.4.21.89 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

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

Inhibitors

Inhibitors Comment Organism Structure
decanoyl-AKAPSKIDD complete inhibition at 0.2 mM Staphylococcus aureus
decanoyl-LTPTAKAPS 7.1% inhibition at 0.2 mM Staphylococcus aureus
LTPTAKAPSKIDD 21.6% inhibition at 0.2 mM Staphylococcus aureus
additional information a substrate based peptide aldehyde inhibits signal peptidases with a lower IC(50) value than other lipopeptides 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 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

Organism UniProt Comment Textmining
Staphylococcus aureus
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-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
bacterial type I signal peptidase
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Staphylococcus aureus
Spase I
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Staphylococcus aureus
SpsB
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Staphylococcus aureus
type I signal peptidase
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Staphylococcus aureus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
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
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