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Literature summary for 3.4.22.28 extracted from

  • Kim, Y.; Lovell, S.; Tiew, K.C.; Mandadapu, S.R.; Alliston, K.R.; Battaile, K.P.; Groutas, W.C.; Chang, K.O.
    Broad-spectrum antivirals against 3C or 3C-like proteases of picornaviruses, noroviruses, and coronaviruses (2012), J. Virol., 86, 11754-11762.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.28

Application

Application Comment Organism
drug development the conserved key site of the enzyme may serve as attractive target for the design of broad-spectrum antivirals for multiple viruses in the supercluster Human rhinovirus sp.
drug development the conserved key site of the enzyme may serve as attractive target for the design of broad-spectrum antivirals for multiple viruses in the supercluster Human poliovirus 1

Crystallization (Commentary)

Crystallization (Comment) Organism
purified recombinant enzyme bound to inhibitor GC376, X-ray diffraction structure determination and analysis at 1.6 A resolution, molecular replacement Human poliovirus 1

Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-1-hydroxy-3-(2-oxopyrrolidin-3-yl)propane-1-sulfonic acid
-
 Human poliovirus 1
(2S)-2-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-1-hydroxy-3-(2-oxopyrrolidin-3-yl)propane-1-sulfonic acid
-
 Human rhinovirus sp.
additional information efficiency of inhibitors in inhibition of virus replication, quantitative realtime PCR expression analysis, overview Human poliovirus 1
additional information efficiency of inhibitors in inhibition of virus replication, quantitative realtime PCR expression analysis, overview Human rhinovirus sp.
N2-[(benzyloxy)carbonyl]-N-[(2S)-1-oxo-3-(2-oxopyrrolidin-3-yl)propan-2-yl]-L-leucinamide
-
 Human poliovirus 1
N2-[(benzyloxy)carbonyl]-N-[(2S)-1-oxo-3-(2-oxopyrrolidin-3-yl)propan-2-yl]-L-leucinamide
-
 Human rhinovirus sp.
N2-[(benzyloxy)carbonyl]-N-[(2S)-3,4-dioxo-1-(2-oxopyrrolidin-3-yl)-4-(propan-2-ylamino)butan-2-yl]-L-leucinamide
-
 Human poliovirus 1
N2-[(benzyloxy)carbonyl]-N-[(2S)-3,4-dioxo-1-(2-oxopyrrolidin-3-yl)-4-(propan-2-ylamino)butan-2-yl]-L-leucinamide
-
 Human rhinovirus sp.
rupintrivir
-
 Human poliovirus 1
rupintrivir
-
 Human rhinovirus sp.

Organism

Organism UniProt Comment Textmining
Human poliovirus 1
-
-
-
Human poliovirus 1 Mahoney
-
-
-
Human rhinovirus sp.
-
 HRV, strains 18, 51, and 68
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Dabcyl-KTSAVLQSGFRKME-EDANS + H2O
-
 Human poliovirus 1 Dabcyl-KTSAVLQ + SGFRKME-EDANS
-
 ?
Dabcyl-KTSAVLQSGFRKME-EDANS + H2O
-
 Human poliovirus 1 Mahoney Dabcyl-KTSAVLQ + SGFRKME-EDANS
-
 ?
Edans-DFHLQGP-Dabcyl + H2O
-
 Human rhinovirus sp. Edans-DFHLQ + GP-Dabcyl
-
 ?

Synonyms

Synonyms Comment Organism
3C protease
-
 Human rhinovirus sp.
3C protease
-
 Human poliovirus 1
3C-like protease
-
 Human rhinovirus sp.
3cLpro
-
 Human rhinovirus sp.
3Cpro
-
 Human rhinovirus sp.
3Cpro
-
 Human poliovirus 1

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Human rhinovirus sp.
37
-
 assay at Human poliovirus 1

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
 assay at Human rhinovirus sp.
8
-
 assay at Human poliovirus 1

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0002
-
 pH 8.0, 37°C, recombinant enzyme Human rhinovirus sp. (2S)-2-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-1-hydroxy-3-(2-oxopyrrolidin-3-yl)propane-1-sulfonic acid
0.00034
-
 pH 8.0, 37°C, recombinant enzyme Human rhinovirus sp. rupintrivir
0.00055
-
 pH 8.0, 37°C, recombinant enzyme Human rhinovirus sp. N2-[(benzyloxy)carbonyl]-N-[(2S)-3,4-dioxo-1-(2-oxopyrrolidin-3-yl)-4-(propan-2-ylamino)butan-2-yl]-L-leucinamide
0.00065
-
 pH 8.0, 37°C, recombinant enzyme Human rhinovirus sp. N2-[(benzyloxy)carbonyl]-N-[(2S)-1-oxo-3-(2-oxopyrrolidin-3-yl)propan-2-yl]-L-leucinamide
0.00177
-
 pH 8.0, 37°C, recombinant enzyme Human poliovirus 1 (2S)-2-([N-[(benzyloxy)carbonyl]-L-leucyl]amino)-1-hydroxy-3-(2-oxopyrrolidin-3-yl)propane-1-sulfonic acid
0.00183
-
 pH 8.0, 37°C, recombinant enzyme Human poliovirus 1 rupintrivir
0.00202
-
 pH 8.0, 37°C, recombinant enzyme Human poliovirus 1 N2-[(benzyloxy)carbonyl]-N-[(2S)-1-oxo-3-(2-oxopyrrolidin-3-yl)propan-2-yl]-L-leucinamide
0.00284
-
 pH 8.0, 37°C, recombinant enzyme Human poliovirus 1 N2-[(benzyloxy)carbonyl]-N-[(2S)-3,4-dioxo-1-(2-oxopyrrolidin-3-yl)-4-(propan-2-ylamino)butan-2-yl]-L-leucinamide