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Literature summary for 3.4.22.69 extracted from

  • Abe, K.; Kabe, Y.; Uchiyama, S.; Iwasaki, Y.W.; Ishizu, H.; Uwamino, Y.; Takenouchi, T.; Uno, S.; Ishii, M.; Maruno, T.; Noda, M.; Murata, M.; Hasegawa, N.; Saya, H.; Kitagawa, Y.; Fukunaga, K.; Amagai, M.; Siomi, H.; Suematsu, M.; Kosaki, K.; Kosaki, K.
    Pro108Ser mutation of SARS-CoV-2 3CLpro reduces the enzyme activity and ameliorates the clinical severity of COVID-19 (2022), Sci. Rep., 12, 1299 .
    View publication on PubMedView publication on EuropePMC

Application

Application Comment Organism
medicine patients infected with a SARS-Cov-2 sub-lineage (B.1.1.284) carrying the Pro108Ser mutation in 3CLpro tend to have a comparatively milder clinical course than patients infected with the same sub-lineage of virus not carrying the mutation Severe acute respiratory syndrome coronavirus 2

Protein Variants

Protein Variants Comment Organism
P108S patients infected with a SARS-Cov-2 sub-lineage (B.1.1.284) carrying the Pro108Ser mutation in 3CLpro tend to have a comparatively milder clinical course than patients infected with the same sub-lineage of virus not carrying the mutation. The Kcat/Km value of the 3CLpro enzyme containing Ser108 is 58% lower than that of Pro108 3CLpro. The reduced activity is associated with structural perturbation surrounding the substrate-binding region of the enzyme Severe acute respiratory syndrome coronavirus 2

Inhibitors

Inhibitors Comment Organism Structure
GC376
-
Severe acute respiratory syndrome coronavirus 2

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.11
-
Dabcyl-KTSAVLQSGFRKME-EDANS wild-type, pH 7.5, 25°C Severe acute respiratory syndrome coronavirus 2
0.216
-
Dabcyl-KTSAVLQSGFRKME-EDANS mutant P108S, pH 7.5, 25°C Severe acute respiratory syndrome coronavirus 2

Organism

Organism UniProt Comment Textmining
Severe acute respiratory syndrome coronavirus 2
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Dabcyl-KTSAVLQSGFRKME-EDANS + H2O
-
Severe acute respiratory syndrome coronavirus 2 Dabcyl-KTSAVLQ + SGFRKME-EDANS
-
?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.0012
-
Dabcyl-KTSAVLQSGFRKME-EDANS mutant P108S, pH 7.5, 25°C Severe acute respiratory syndrome coronavirus 2
0.0014
-
Dabcyl-KTSAVLQSGFRKME-EDANS wild-type, pH 7.5, 25°C Severe acute respiratory syndrome coronavirus 2

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00193
-
wild-type, pH 7.5, 25°C Severe acute respiratory syndrome coronavirus 2 GC376
0.00374
-
mutant P108S, pH 7.5, 25°C Severe acute respiratory syndrome coronavirus 2 GC376