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Literature summary for 3.4.22.34 extracted from

  • Stern, L.; Perry, R.; Ofek, P.; Many, A.; Shabat, D.; Satchi-Fainaro, R.
    A novel antitumor prodrug platform designed to be cleaved by the endoprotease legumain (2009), Bioconjug. Chem., 20, 500-510.
    View publication on PubMed
Search for more literature for 3.4.22.34

Activating Compound

Activating Compound Comment Organism Structure
additional information expression levels of endogenous legumain elevate in HEK-293 cells following stress Homo sapiens

Application

Application Comment Organism
drug development enzyme serves as a promising candidate for prodrug tumor therapy Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
embryonic kidney cells are stably transfected with human legumain to achieve overexpression in vitro, HEK-Leg cells expressed both active and inactive legumain and secreted it to the medium Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Homo sapiens 5764
-

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
36000
-
 mature, active form, determined by SDS-PAGE and Westen blot analysis Homo sapiens
46000
-
 non-mature, active form, determined by SDS-PAGE and Westen blot analysis Homo sapiens
56000
-
 inactive proform, determined by SDS-PAGE and Westen blot analysis Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens enzyme promote cell migration and is associated with enhanced tissue invasion and metastases ?
-
 ?
additional information Homo sapiens legumain is a member of the C13 family of peptidases that specifically cleaves asparaginyl bonds ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation recombinant legumain Homo sapiens
-
HEK-293 cell
-
 Homo sapiens
-
PC-3 cell
-
 Homo sapiens
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
additional information
-
 HEK-293 serum-starved cells show a slight 1.2fold increase in enzymatic activity toward carbobenzyloxy-Ala-Ala-Asn-amido-4-methyl coumarin compared to that of nonstarved 293 HEK cells, while PC-3 serum-starved or nonstarved cells shows no significant difference in enzymatic activity Homo sapiens
additional information
-
 HEK-293-overexpressing legumain cells cleave 100% of the prodrug carbobenzyloxy-Ala-Ala-Asn-ethylenediamine-etoposide, whereas HEK-293 cells, which express low levels of legumain, cleave only 33% of it Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
carbobenzyloxy-Ala-Ala-Asn-ethylenediamine-etoposide + H2O legumain releases the chemotherapeutic agent etoposide, as the active drug Homo sapiens etoposide-ethylenediamine + carbobenzyloxy-Ala-Ala-Asn
-
 ?
CBZ-Ala-Ala-Asn-amido-4-methylcoumarin + H2O
-
 Homo sapiens CBZ-Ala-Ala-Asn + 7-amino-4-methylcoumarin
-
 ?
additional information enzyme promote cell migration and is associated with enhanced tissue invasion and metastases Homo sapiens ?
-
 ?
additional information legumain is a member of the C13 family of peptidases that specifically cleaves asparaginyl bonds Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
legumain
-
 Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.5
-
 recombinant legumain cleaves carbobenzyloxy-Ala-Ala-Asn-amido-4-methyl coumarin more potently at pH 6.5 than at pH 5.0 Homo sapiens

pH Stability

pH Stability pH Stability Maximum Comment Organism
7
-
 no enzymatic activity at pH 7.0, legumain undergoes denaturation at these basic conditions Homo sapiens