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Literature summary for 3.4.21.53 extracted from

  • Frase, H.; Hudak, J.; Lee, I.
    Identification of the proteasome inhibitor MG262 as a potent ATP-dependent inhibitor of the Salmonella enterica serovar Typhimurium Lon protease (2006), Biochemistry, 45, 8264-8274.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
NdeI-BamHI fragment from proEx-1/lon cloned into pET24c(+), overexpressed in Escherichia coli Rosetta (DE3) Homo sapiens
PCR product cloned into the NcoI and HindIII sites of pET24d(+), overexpressed in Escherichia coli BL21 (DE3) Salmonella enterica subsp. enterica serovar Typhimurium

Protein Variants

Protein Variants Comment Organism
V378I naturally occurring conservative mutation Salmonella enterica subsp. enterica serovar Typhimurium

Inhibitors

Inhibitors Comment Organism Structure
Cb2-Leu-Leu-Leu
-
Salmonella enterica subsp. enterica serovar Typhimurium
Cb2-Leu-Leu-Leu-aldehyde
-
Salmonella enterica subsp. enterica serovar Typhimurium
isopropylboronic acid
-
Salmonella enterica subsp. enterica serovar Typhimurium
MG262
-
Homo sapiens
MG262 most potent inhibitor, requires binding, but not hydrolysis, of ATP to initiate inhibition Salmonella enterica subsp. enterica serovar Typhimurium
additional information epoxomicin, ZL3-VS and ethylboronic acid are ineffective at inhibiting lon at micromolar concentrations Salmonella enterica subsp. enterica serovar Typhimurium

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.046
-
ATP intrinsic ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
0.15
-
ATP Y(3-NO2)-RGIT2-aminobuytric acid-SGRQ-K(anthranilamide) stimulated ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
0.172
-
ATP Y(3-NO2)-RGITCySGRQ-K(anthranilamide) stimulated ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
0.262
-
Y(3-NO2)-RGITCSGRQ-K(anthranilamide)
-
Salmonella enterica subsp. enterica serovar Typhimurium
0.276
-
Y(3-NO2)-RGIT2-aminobuytric acid-SGRQ-K(anthranilamide)
-
Salmonella enterica subsp. enterica serovar Typhimurium
1.3
-
Y(3-NO2)-RGITCysSGRQ-K(anthranilamide)
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Salmonella enterica subsp. enterica serovar Typhimurium
-
-
-

Purification (Commentary)

Purification (Comment) Organism
by gel filtration, to near homogeneity Homo sapiens
to near homogeneity Salmonella enterica subsp. enterica serovar Typhimurium

Storage Stability

Storage Stability Organism
-80°C Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + H2O
-
Salmonella enterica subsp. enterica serovar Typhimurium phosphate + ADP
-
?
Y(3-NO2)-RGIT2-aminobutyric acid-SGRQ-K(anthranilamide) + H2O
-
Salmonella enterica subsp. enterica serovar Typhimurium Y(3-NO2)-RGIT2-aminobutyrate + SGRQ-K(anthranilamide)
-
?
Y(3-NO2)-RGITCSGRQ-K(anthranilamide) + H2O
-
Salmonella enterica subsp. enterica serovar Typhimurium Y(3-NO2)-RGITC + SGRQ-K(anthranilamide)
-
?
Y(3-NO2)-RGITCSGRQ-K(anthranilamide) + H2O
-
Homo sapiens Y(3-NO2)-RGITC + SGRQ-K(anthranilamide)
-
?

Synonyms

Synonyms Comment Organism
lon
-
Salmonella enterica subsp. enterica serovar Typhimurium
lon
-
Homo sapiens
lon protease
-
Salmonella enterica subsp. enterica serovar Typhimurium
lon protease
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.41
-
ATP intrinsic ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
2
-
ATP Y(3-NO2)-RGIT2-aminobuytric acid-SGRQ-K(anthranilamide) stimulated ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
2
-
ATP Y(3-NO2)-RGITCSGRQ-K(anthranilamide) stimulated ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
5.9
-
Y(3-NO2)-RGITCysSGRQ-K(anthranilamide)
-
Homo sapiens
11
-
Y(3-NO2)-RGIT2-aminobuytric acid-SGRQ-K(anthranilamide)
-
Salmonella enterica subsp. enterica serovar Typhimurium
15
-
Y(3-NO2)-RGITCSGRQ-K(anthranilamide)
-
Salmonella enterica subsp. enterica serovar Typhimurium

Cofactor

Cofactor Comment Organism Structure
ATP in the absence of ATP, no peptide cleavage is observed Salmonella enterica subsp. enterica serovar Typhimurium
ATP in the absence of ATP, no peptide cleavage is observed Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00006
-
MG262
-
Salmonella enterica subsp. enterica serovar Typhimurium
0.002
-
Cb2-Leu-Leu-Leu-aldehyde
-
Salmonella enterica subsp. enterica serovar Typhimurium

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000122
-
-
Salmonella enterica subsp. enterica serovar Typhimurium MG262
0.0041
-
-
Salmonella enterica subsp. enterica serovar Typhimurium Cb2-Leu-Leu-Leu-aldehyde
0.74
-
-
Salmonella enterica subsp. enterica serovar Typhimurium Cb2-Leu-Leu-Leu
0.81
-
-
Salmonella enterica subsp. enterica serovar Typhimurium isopropylboronic acid