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Literature summary extracted from

  • Rabah, N.; Gauthier, D.; Dikeakos, J.D.; Reudelhuber, T.L.; Lazure, C.
    The C-terminal region of the proprotein convertase 1/3 (PC1/3) exerts a bimodal regulation of the enzyme activity in vitro (2007), FEBS J., 274, 3482-3491.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
3.4.21.61 CT-peptide increases PC1/3 activity at low concentrations (nanomol). PC1/3, through its various domains, is capable of controlling its enzymatic activity in all regions of the cell that it encounters. Activation of PC1/3 by 5 nanomol CT-peptide is the same in the presence or absence of propeptide Mus musculus
3.4.21.93 PC1/3 CT peptide increases PC1/3 activity at low concentrations (nanomol range). Interaction with the active site of PC1/3 does not result in the formation of a stable complex. Activation of PC1/3 by 5 nanomol CT-peptide is the same in the presence or absence of propeptide Mus musculus

Application

EC Number Application Comment Organism
3.4.21.93 additional information PC1/3, through its various domains, is capable of controlling its enzymatic activity in all regions of the cell that it encounters Mus musculus

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.21.61 recombinant PC1/3 produced using the baculovirus expression system in Sf-9 insect cells or through intracoelemic injection in insect larvae Mus musculus
3.4.21.75 recombinant soluble C-terminus truncated furin expressed in Sf9 insect cells Homo sapiens
3.4.21.93 PC1/3 produced using the baculovirus expression system in Sf9 insect cells or through intracoelemic injection in insect larvae. PC1/3 CT-peptide from positions 592-726 cloned into a pet24b+ bacterial expression vector. The resulting C-terminally His-tagged protein expressed in Escherichia coli strain BL21 (DE3) Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.61 CT-peptide decreases PC1/3 activity at high concentrations (micromol) Mus musculus
3.4.21.61 propeptide addition of purified recombinant propeptide (20 nanomol) to PC1/3 enzymatic reaction leads to a 50% reduction in enzymatic activity. In the presence of 5 nanomol CT-peptide and 20 nanomol propeptide, inhibition is reduced to 35% Mus musculus
3.4.21.93 PC1/3 CT peptide decreases PC1/3 activity at high concentrations (micromol range) Mus musculus
3.4.21.93 PC1/3 propeptide 20 nanomol leads to a 50% reduction in enzymatic activity Mus musculus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
3.4.21.61 Ca2+
-
 Mus musculus

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
3.4.21.61 17640
-
 mass spectrometry analysis Mus musculus
3.4.21.93 17640
-
 mass spectrometry Mus musculus

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.61 Mus musculus
-
-
-
3.4.21.75 Homo sapiens
-
-
-
3.4.21.93 Mus musculus
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.21.61
-
 Mus musculus
3.4.21.93 recombinant PC1/3 purified. PC1/3 CT peptide purified by His-affinity chromatography and RP-HPLC Mus musculus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.61 additional information CT-peptide is not cleaved by enzymatically active PC1/3 Mus musculus ?
-
 ?
3.4.21.61 pGlu-Arg-Thr-Lys-Arg-4-methylcoumaryl-7-amide + H2O
-
 Mus musculus 7-amino-4-methylcoumarin
-
 ?
3.4.21.75 PC1/3 C-terminal peptide + H2O cleavage by furin into a peptide with an apparent molecular mass of 12.5 kDa. Cleavage of the C-terminal to the pair of Args occupying positions 627 and 628 Homo sapiens ?
-
 ?
3.4.21.93 additional information PC1/3 CT peptide is not cleaved by enzymatically active PC1/3 Mus musculus ?
-
 ?
3.4.21.93 pGlu-Arg-Thr-Lys-Arg-7-amido-4-methylcoumarin + H2O
-
 Mus musculus pGlu-Arg-Thr-Lys-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.61 PC1/3
-
 Mus musculus
3.4.21.61 proprotein convertase 1/3
-
 Mus musculus
3.4.21.75 Proprotein convertase
-
 Homo sapiens
3.4.21.93 PC1/3
-
 Mus musculus
3.4.21.93 proprotein convertase 1/3
-
 Mus musculus

pH Range

EC Number pH Minimum pH Maximum Comment Organism
3.4.21.93 additional information
-
 at pH 7.8 increase of enzymatic activity up to 50-60%, irrespective of the amount of PC1/3 CT peptide used up to 0.005 mM Mus musculus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.61 0.002
-
 CT-peptide
-
 Mus musculus
3.4.21.93 0.002
-
 PC1/3 CT peptide
-
 Mus musculus