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3.4.22.49: separase

This is an abbreviated version!
For detailed information about separase, go to the full flat file.

Word Map on EC 3.4.22.49

Reaction

all bonds known to be hydrolysed by this endopeptidase have arginine in P1 and an acidic residue in P4. P6 is often occupied by an acidic residue or by an hydroxy-amino-acid residue, the phosphorylation of which enhances cleavage =

Synonyms

AESP, AtESP, Cut1, Cut1/separase, ESP, Esp1, ESPL1, sep-1, separase, separin, SSE, TbSep

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.22 Cysteine endopeptidases
                3.4.22.49 separase

Inhibitors

Inhibitors on EC 3.4.22.49 - separase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1,3-dihydroxy-2,2-dimethyl-5-(trifluoromethyl)-2H-benzimidazole-1,3-diium
0.1 mM, 8.0% inhibition
1,3-dihydroxy-2,2-dimethyl-5-nitro-2H-benzimidazole-1,3-diium
0.1 mM, 95.9% inhibition
1,3-dihydroxy-2,2-dimethyl-5-[(trifluoromethoxy)sulfinyl]-2H-benzimidazole-1,3-diium
0.1 mM, 64.6% inhibition
1,3-dihydroxy-5-nitrospiro[benzimidazole-1,3-diium-2,1'-cyclohexane]
0.1 mM, 99.5% inhibition
1,3-dihydroxy-5-nitrospiro[benzimidazole-1,3-diium-2,1'-cyclopentane]
0.1 mM, 96.2% inhibition
1,3-dihydroxy-5-[hydroxy(methoxy)methyl]-2,2-dimethyl-2H-benzimidazole-1,3-diium
0.1 mM, 14.6% inhibition
2-(4-carboxyphenyl)-1,3-dihydroxy-2-methyl-5-nitro-2H-benzimidazole-1,3-diium
0.1 mM, 84.1% inhibition
2-butyl-1,3-dihydroxy-2-methyl-5-nitro-2H-benzimidazole-1,3-diium
0.1 mM, 99.8% inhibition
2-ethyl-1,3-dihydroxy-2-methyl-5-nitro-2H-benzimidazole-1,3-diium
0.1 mM, 99.6% inhibition
2-ethyl-1,3-dihydroxy-5-nitro-2-propyl-2H-benzimidazole-1,3-diium
0.1 mM, 99.2% inhibition
4-bromo-1,3-dihydroxy-2,2-dimethyl-6-nitro-2H-benzimidazole-1,3-diium
0.1 mM, 100% inhibition
5-(butylamino)-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium
0.1 mM, 40.9% inhibition
5-bromo-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium
0.1 mM, 24.6% inhibition
5-carboxy-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium
0.1 mM, 24.4% inhibition
5-ethoxy-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium
0.1 mM, 21.2% inhibition
5-ethoxy-6-fluoro-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium
0.1 mM, 25.2% inhibition
5-fluoro-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium
0.1 mM, 35.4% inhibition
5-fluoro-1,3-dihydroxy-2,2-dimethyl-6-nitro-2H-benzimidazole-1,3-diium
0.1 mM, 60.1% inhibition
5-hexyl-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium
0.1 mM, 39.3% inhibition
5-nitro-2,1,3-benzoxadiazole
0.1 mM, 43.1% inhibition
Cdc55
-
results suggest that Cdc55 acts as inhibitor downstream from shugoshin
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Cdk1 kinase
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phosphorylation-dependent binding of the cyclin B1 subunit of Cdk1 kinase to a Cdc6-like domain of separase inhibits separase
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cyclin B
-
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cyclin B1
-
cyclin-dependent kinase 1-cyclin B1
Cdk1-cyclin B1 triggers precipitation of separase by phosphorylation but stabilizes it by inhibitory binding. Only separase that is first complexed by Cdk1-cyclin B1 can later be activated by cyclin B1 degradation
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Pds1
Pds1 is a chaperone, inhibition of Esp1 by overexpression of undegradable Pds1 blocks mitotic exit via blockage of cohesin cleavage
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peptide
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acyloxymethyl ketone derivative of human SCC1 cleavage site peptide, chloromethyl ketone derivatives of the yeast Scc1 cleavage site
securin
securin Pds1
-
an inhibitor of separase Esp1 in budding yeast. As Pds1 is degraded, Esp1 is activated, and cells transit into anaphase
securing
the motif containing H134 in securing isoform PTTG1 has a strong affinity for separase and is involved in inhibiting it, while another domain(s) in isoform is involved in activating separase and has a weaker affinity for it. Isoform PTTG2 does not interact with separase
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sercurin
securin persistently binds and inhibits separase during much of metaphase
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shugoshin
-
prevents separase activation independently of securin, protein phosphatase 2A coupled to regulatory subunit Cdc55 is essential for Shugoshin-mediated inhibition
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additional information
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