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Literature summary for 3.4.24.13 extracted from

  • Garner, A.L.; Fullagar, J.L.; Day, J.A.; Cohen, S.M.; Janda, K.D.
    Development of a high-throughput screen and its use in the discovery of Streptococcus pneumoniae immunoglobulin A1 protease inhibitors (2013), J. Am. Chem. Soc., 135, 10014-10017.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
1,2-diethyl-3-hydroxypyridine-4(1H)-thione
-
Streptococcus pneumoniae
1-ethyl-3-hydroxy-2-methylpyridine-4(1H)-thione
-
Streptococcus pneumoniae
1-[2-(3-bromophenyl)ethyl]-3-hydroxy-2-methylpyridine-4(1H)-thione
-
Streptococcus pneumoniae
1-[2-(3-chloro-4-methoxyphenyl)ethyl]-3-hydroxy-2-methylpyridine-4(1H)-thione
-
Streptococcus pneumoniae
1-[2-(3-chlorophenyl)ethyl]-3-hydroxy-2-methylpyridine-4(1H)-thione
-
Streptococcus pneumoniae
1-[2-(3-fluorophenyl)ethyl]-3-hydroxy-2-methylpyridine-4(1H)-thione
-
Streptococcus pneumoniae
3-hydroxy-1,2-dimethylpyridine-4(1H)-thione
-
Streptococcus pneumoniae
3-hydroxy-1-[2-(3-methoxyphenyl)ethyl]-2-methylpyridine-4(1H)-thione
-
Streptococcus pneumoniae
3-hydroxy-1-[2-(4-methoxyphenyl)ethyl]-2-methylpyridine-4(1H)-thione
-
Streptococcus pneumoniae
3-hydroxy-2-methyl-1-(2-phenylethyl)pyridine-4(1H)-thione
-
Streptococcus pneumoniae
3-hydroxy-2-methyl-1-[2-(3-methylphenyl)ethyl]pyridine-4(1H)-thione
-
Streptococcus pneumoniae
Berberine
-
Streptococcus pneumoniae
norharmane
-
Streptococcus pneumoniae
remerine
-
Streptococcus pneumoniae

Localization

Localization Comment Organism GeneOntology No. Textmining
extracellular
-
Streptococcus pneumoniae
-
-

Metals/Ions

Metals/Ions Comment Organism Structure
Zn2+ contains zinc Streptococcus pneumoniae

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
immunoglobulin A1 + H2O Streptococcus pneumoniae
-
immunoglobulin A1 Fabalpha fragments + immunglobulin A1 Fcalpha
-
?

Organism

Organism UniProt Comment Textmining
Streptococcus pneumoniae
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
immunoglobulin A1 + H2O
-
Streptococcus pneumoniae immunoglobulin A1 Fabalpha fragments + immunglobulin A1 Fcalpha
-
?

Synonyms

Synonyms Comment Organism
IgA1P
-
Streptococcus pneumoniae
immunoglobulin A1 protease
-
Streptococcus pneumoniae

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0043
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 1-[2-(3-chlorophenyl)ethyl]-3-hydroxy-2-methylpyridine-4(1H)-thione
0.00498
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 1-[2-(3-chloro-4-methoxyphenyl)ethyl]-3-hydroxy-2-methylpyridine-4(1H)-thione
0.00614
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 1-[2-(3-bromophenyl)ethyl]-3-hydroxy-2-methylpyridine-4(1H)-thione
0.00664
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 3-hydroxy-1-[2-(3-methoxyphenyl)ethyl]-2-methylpyridine-4(1H)-thione
0.007
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 3-hydroxy-1-[2-(4-methoxyphenyl)ethyl]-2-methylpyridine-4(1H)-thione
0.00774
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 1-[2-(3-fluorophenyl)ethyl]-3-hydroxy-2-methylpyridine-4(1H)-thione
0.00914
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 3-hydroxy-2-methyl-1-[2-(3-methylphenyl)ethyl]pyridine-4(1H)-thione
0.0127
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 3-hydroxy-2-methyl-1-(2-phenylethyl)pyridine-4(1H)-thione
0.0231
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae remerine
0.0523
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae Berberine
0.152
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae norharmane
0.887
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 1-ethyl-3-hydroxy-2-methylpyridine-4(1H)-thione
0.962
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 1,2-diethyl-3-hydroxypyridine-4(1H)-thione
1.3
-
in 50 mM Tris-HCl, pH 7.0, at 37°C Streptococcus pneumoniae 3-hydroxy-1,2-dimethylpyridine-4(1H)-thione

General Information

General Information Comment Organism
physiological function the enzyme catalyzes the proteolysis of human IgA1 at its hinge region to leave the bacterial cell surface masked by IgA1 Fab, enabling the bacteria to evade the host's immune system and adhere to host epithelial cells to promote colonization Streptococcus pneumoniae