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Literature summary extracted from

  • Zandberg, W.F.; Benjannet, S.; Hamelin, J.; Pinto, B.M.; Seidah, N.G.
    N-glycosylation controls trafficking, zymogen activation and substrate processing of proprotein convertases PC1/3 and subtilisin kexin isozyme-1 (2011), Glycobiology, 21, 1290-1300.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.21.61 expression in HEK293 cells Mus musculus
3.4.21.112 expression in CHO K1 and SRD-12B cells Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
3.4.21.61 N146A mutation results in the decreased zymogen activation of proPC1/3 and virtually inhibits its secretion Mus musculus
3.4.21.61 N374A mutant is processed and secreted at nearly the same rate and with the same apparent molecular mass as wild-type. Residue N374 does not appear to bear an N-glycan Mus musculus
3.4.21.61 N618A mutation does not significantly affect zymogen activation Mus musculus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.61 (3S,4S,5S,6R)-2-([(2R,3S,4S,5S,6S)-3,5-dihydroxy-2-(hydroxymethyl)-6-methoxytetrahydro-2H-pyran-4-yl]amino)-6-(hydroxymethyl)tetrahydro-2H-thiopyran-3,4,5-triol i.e. BJ-12-26-1, greatly reduces the processing of substrate proopiomelanocortin Mus musculus
3.4.21.61 (3S,4S,5S,6R)-2-([(2S,3S,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3-yl]amino)-6-(hydroxymethyl)tetrahydro-2H-thiopyran-3,4,5-triol i.e. BJ-12-21-2, greatly reduces the processing of substrate proopiomelanocortin Mus musculus
3.4.21.112 (3S,4S,5S,6R)-2-([(2R,3S,4S,5S,6S)-3,5-dihydroxy-2-(hydroxymethyl)-6-methoxytetrahydro-2H-pyran-4-yl]amino)-6-(hydroxymethyl)tetrahydro-2H-thiopyran-3,4,5-triol i.e. BJ-12-26-1, greatly reduces SKI-1 zymogen processing, and abolishes the processing of substrate SREBP-2 Homo sapiens
3.4.21.112 (3S,4S,5S,6R)-2-([(2S,3S,4R,5S,6R)-4,5-dihydroxy-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3-yl]amino)-6-(hydroxymethyl)tetrahydro-2H-thiopyran-3,4,5-triol i.e. BJ-12-21-2, greatly reduces SKI-1 zymogen processing, and abolishes the processing of substrate SREBP-2 Homo sapiens

Organism

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

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
3.4.21.61 glycoprotein mutation of N-glycosylation site N146 results in the decreased zymogen activation of proPC1/3 and virtually inhibits its secretion. Mutation of glycosylation site N618A mutation does not significantly affect zymogen activation. The presence, but not the exact structure, of N-glycans is crucial for proPC1/3 zymogen processing Mus musculus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.61 proopiomelanocortin + H2O
-
 Mus musculus beta-lipotropic hormone + adrenocorticotropic hormone + ?
-
 ?
3.4.21.112 sterol regulatory element-binding protein SREBP-2 + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.61 PC1/3
-
 Mus musculus
3.4.21.112 SKI-1
-
 Homo sapiens
3.4.21.112 subtilisin kexin isoenzyme-1
-
 Homo sapiens