Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(4R)-3-(4-methoxyphenyl)-4-(pent-4-yn-1-yl)oxetan-2-one | inhibitor efficiently alters the oligomerization of the enzyme to smaller species, almost quantitative shift from the tetradecamer to the heptamer with modification of 35% of the active sites | Staphylococcus aureus | |
1-(1,1-dioxido-1,2-thiazetidin-2-yl)hexan-1-one | alkyne-free beta-sultam analogue. Treatment leads to dehydroalanine formation of the active site serine. The reaction proceeds through sulfonylation and subsequent elimination, thereby obliterating the catalytic charge relay system | Staphylococcus aureus | |
1-(4-benzoyl-1,1-dioxido-1,2-thiazetidin-2-yl)ethanone | alkyne-free beta-sultam analogue. Treatment leads to dehydroalanine formation of the active site serine. The reaction proceeds through sulfonylation and subsequent elimination, thereby obliterating the catalytic charge relay system | Staphylococcus aureus | |
1-[4-(4-ethynylbenzoyl)-1,1-dioxido-1,2-thiazetidin-2-yl]ethanone | treatment results in almost instant covalent modification of all 14 active sites and complete inhibition of peptidase activity | Staphylococcus aureus | |
1-[4-(4-ethynylbenzoyl)-1,1-dioxido-1,2-thiazetidin-2-yl]undec-10-en-1-one | inhibitor efficiently alters the oligomerization of the enzyme to smaller species, almost quantitative shift from the tetradecamer to the heptamer with modification of 63% of the active sites | Staphylococcus aureus | |
1-[4-benzoyl-1,1-dioxido-1,2-thiazetidin-2-yl]undec-10-en-1-one | alkyne-free beta-sultam analogue. Treatment leads to dehydroalanine formation of the active site serine. The reaction proceeds through sulfonylation and subsequent elimination, thereby obliterating the catalytic charge relay system | Staphylococcus aureus | |
diisopropyl fluorophosphate | inhibitor efficiently alters the oligomerization of the enzyme to smaller species, almost quantitative shift from the tetradecamer to the heptamer with modification of 57% of the active sites | Staphylococcus aureus | |
additional information | not inhibitory: 4-(2-aminoethyl) benzenesulfonyl fluoride, phenylmethylsulfonyl fluoride as well as Z-L-CMK and N-p-tosylphenylalanyl chloromethyl ketone | Staphylococcus aureus |
Molecular Weight [Da] | Molecular Weight Maximum [Da] | Comment | Organism |
---|---|---|---|
150000 | - |
gel filtration, enzyme treated with inhibitor diisopropyl fluorophosphate, 1-[4-(4-ethynylbenzoyl)-1,1-dioxido-1,2-thiazetidin-2-yl]undec-10-en-1-one, or beta-lactone (4R)-3-(4-methoxyphenyl)-4-(pent-4-yn-1-yl)oxetan-2-one | Staphylococcus aureus |
304000 | - |
gel filtration, native enzyme | Staphylococcus aureus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Staphylococcus aureus | - |
- |
- |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
98 | - |
pH not specified in the publication, temperature not specified in the publication | Staphylococcus aureus | 1-[4-(4-ethynylbenzoyl)-1,1-dioxido-1,2-thiazetidin-2-yl]ethanone |