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Results 1 - 10 of 28 > >>
EC Number
Inhibitors
Commentary
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
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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
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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
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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
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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
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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
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3-(4-methoxyphenyl)-4-(pent-4-ynyl)oxetan-2-one
shows stronger inhibitory effect
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3-(non-8-ynyl)-4-(pent-4-ynyl)oxetan-2-one
exerts the weakest effect on peptidase activity
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3-butyl-4-(pent-4-ynyl)oxetan-2-one
shows stronger inhibitory effect
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CAANDENYALAA
-
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Results 1 - 10 of 28 > >>