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Literature summary for 3.4.22.69 extracted from

  • Akaji, K.; Konno, H.; Onozuka, M.; Makino, A.; Saito, H.; Nosaka, K.
    Evaluation of peptide-aldehyde inhibitors using R188I mutant of SARS 3CL protease as a proteolysis-resistant mutant (2008), Bioorg. Med. Chem., 16, 9400-9408.
    View publication on PubMed
Search for more literature for 3.4.22.69

Cloned(Commentary)

Cloned (Comment) Organism
high level of expression of of proteolysis-resistant mutant R188I in Escherichia coli Severe acute respiratory syndrome-related coronavirus

Protein Variants

Protein Variants Comment Organism
R188I replacing Arg with Ile at position 188 renders the protease resistant to proteolysis. The catalytic ability of 3CL-R188I protease was found to be extreme as compared to that of a mature 3CL protease containing a C-terminal His tag. The kcat values is 0.0203 per sec for mature 3CL protease and 4753 per sec for the 3CL-R188I Severe acute respiratory syndrome-related coronavirus

General Stability

General Stability Organism
replacing Arg with Ile at position 188 renders the protease resistant to proteolysis Severe acute respiratory syndrome-related coronavirus

Inhibitors

Inhibitors Comment Organism Structure
acetyl-Ala-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO
-
 Severe acute respiratory syndrome-related coronavirus
acetyl-Ser-Ala-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO
-
 Severe acute respiratory syndrome-related coronavirus
acetyl-Thr-Ser-Ala-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO
-
 Severe acute respiratory syndrome-related coronavirus
acetyl-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO
-
 Severe acute respiratory syndrome-related coronavirus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0338
-
 TSAVLQSGFRK-NH2 pH 7.5, 37°C, mutant enzyme R188I Severe acute respiratory syndrome-related coronavirus
0.046
-
 GPFVDRQTAQAAGTDT-NH2 pH 7.5, 37°C, mutant enzyme R188I Severe acute respiratory syndrome-related coronavirus
0.051
-
 KVATVQSKMSD-NH2 pH 7.5, 37°C, mutant enzyme R188I Severe acute respiratory syndrome-related coronavirus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Severe acute respiratory syndrome-related coronavirus the genomic RNA produces two large proteins with overlapping sequences, polyproteins 1a and 1ab, which are autocatalytically cleaved by two or three viral proteases to yield functional polypeptides. The key enzyme in this processing is SARS 3CL protease ?
-
 ?

Organism

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

Purification (Commentary)

Purification (Comment) Organism
purification of proteolysis-resistant mutant R188I of the SARS 3CL protease Severe acute respiratory syndrome-related coronavirus

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
GPFVDRQTAQAAGTDT-NH2 + H2O 1% of the activity with TSAVLQSGFRK-NH2 Severe acute respiratory syndrome-related coronavirus ?
-
 ?
KVATVQSKMSD-NH2 undecapeptide containing the non-canonical P3/P4 cleavage site of 3CL protease, 6% of the activity with TSAVLQSGFRK-NH2 Severe acute respiratory syndrome-related coronavirus ?
-
 ?
additional information the genomic RNA produces two large proteins with overlapping sequences, polyproteins 1a and 1ab, which are autocatalytically cleaved by two or three viral proteases to yield functional polypeptides. The key enzyme in this processing is SARS 3CL protease Severe acute respiratory syndrome-related coronavirus ?
-
 ?
TSAVLQSGFRK-NH2 + H2O peptide containing the P1/P2 cleavage site, the N-terminal self-cleavage site of the protease, most suitable substrate Severe acute respiratory syndrome-related coronavirus TSAVLQ + SGFRK-NH2
-
 ?

Synonyms

Synonyms Comment Organism
SARS 3CL protease
-
 Severe acute respiratory syndrome-related coronavirus

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
76
-
 GPFVDRQTAQAAGTDT-NH2 pH 7.5, 37°C, mutant enzyme R188I Severe acute respiratory syndrome-related coronavirus
455
-
 KVATVQSKMSD-NH2 pH 7.5, 37°C, mutant enzyme R188I Severe acute respiratory syndrome-related coronavirus
4753
-
 TSAVLQSGFRK-NH2 pH 7.5, 37°C, mutant enzyme R188I Severe acute respiratory syndrome-related coronavirus

pI Value

Organism Comment pI Value Maximum pI Value
Severe acute respiratory syndrome-related coronavirus mutant enzyme R188I, calculated from sequence
-
 6.24

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.026
-
-
 Severe acute respiratory syndrome-related coronavirus acetyl-Thr-Ser-Ala-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO
0.037
-
-
 Severe acute respiratory syndrome-related coronavirus acetyl-Ser-Ala-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO
0.155
-
-
 Severe acute respiratory syndrome-related coronavirus acetyl-Ala-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO
6
-
-
 Severe acute respiratory syndrome-related coronavirus acetyl-Val-Leu-NHCH(CH2CH2CON(CH3)2)-CHO