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Literature summary 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)

EC Number Cloned (Comment) Organism
3.4.21.53 NdeI-BamHI fragment from proEx-1/lon cloned into pET24c(+), overexpressed in Escherichia coli Rosetta (DE3) Homo sapiens
3.4.21.53 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

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.53 Cb2-Leu-Leu-Leu
-
 Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 Cb2-Leu-Leu-Leu-aldehyde
-
 Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 isopropylboronic acid
-
 Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 MG262
-
 Homo sapiens
3.4.21.53 MG262 most potent inhibitor, requires binding, but not hydrolysis, of ATP to initiate inhibition Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 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]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.53 0.046
-
 ATP intrinsic ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 0.15
-
 ATP Y(3-NO2)-RGIT2-aminobuytric acid-SGRQ-K(anthranilamide) stimulated ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 0.172
-
 ATP Y(3-NO2)-RGITCySGRQ-K(anthranilamide) stimulated ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 0.262
-
 Y(3-NO2)-RGITCSGRQ-K(anthranilamide)
-
 Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 0.276
-
 Y(3-NO2)-RGIT2-aminobuytric acid-SGRQ-K(anthranilamide)
-
 Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 1.3
-
 Y(3-NO2)-RGITCysSGRQ-K(anthranilamide)
-
 Homo sapiens

Organism

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

Purification (Commentary)

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

Storage Stability

EC Number Storage Stability Organism
3.4.21.53 -80°C Homo sapiens

Substrates and Products (Substrate)

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

Synonyms

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

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.21.53 0.41
-
 ATP intrinsic ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 2
-
 ATP Y(3-NO2)-RGIT2-aminobuytric acid-SGRQ-K(anthranilamide) stimulated ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 2
-
 ATP Y(3-NO2)-RGITCSGRQ-K(anthranilamide) stimulated ATP hydrolysis Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 5.9
-
 Y(3-NO2)-RGITCysSGRQ-K(anthranilamide)
-
 Homo sapiens
3.4.21.53 11
-
 Y(3-NO2)-RGIT2-aminobuytric acid-SGRQ-K(anthranilamide)
-
 Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 15
-
 Y(3-NO2)-RGITCSGRQ-K(anthranilamide)
-
 Salmonella enterica subsp. enterica serovar Typhimurium

Cofactor

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

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.53 0.00006
-
 MG262
-
 Salmonella enterica subsp. enterica serovar Typhimurium
3.4.21.53 0.002
-
 Cb2-Leu-Leu-Leu-aldehyde
-
 Salmonella enterica subsp. enterica serovar Typhimurium

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.53 0.000122
-
-
 Salmonella enterica subsp. enterica serovar Typhimurium MG262
3.4.21.53 0.0041
-
-
 Salmonella enterica subsp. enterica serovar Typhimurium Cb2-Leu-Leu-Leu-aldehyde
3.4.21.53 0.74
-
-
 Salmonella enterica subsp. enterica serovar Typhimurium Cb2-Leu-Leu-Leu
3.4.21.53 0.81
-
-
 Salmonella enterica subsp. enterica serovar Typhimurium isopropylboronic acid