3.4.22.49 1,3-dihydroxy-2,2-dimethyl-5-(trifluoromethyl)-2H-benzimidazole-1,3-diium 0.1 mM, 8.0% inhibition 235780 3.4.22.49 1,3-dihydroxy-2,2-dimethyl-5-nitro-2H-benzimidazole-1,3-diium 0.1 mM, 95.9% inhibition 235781 3.4.22.49 1,3-dihydroxy-2,2-dimethyl-5-[(trifluoromethoxy)sulfinyl]-2H-benzimidazole-1,3-diium 0.1 mM, 64.6% inhibition 235782 3.4.22.49 1,3-dihydroxy-5-nitrospiro[benzimidazole-1,3-diium-2,1'-cyclohexane] 0.1 mM, 99.5% inhibition 235783 3.4.22.49 1,3-dihydroxy-5-nitrospiro[benzimidazole-1,3-diium-2,1'-cyclopentane] 0.1 mM, 96.2% inhibition 235784 3.4.22.49 1,3-dihydroxy-5-[hydroxy(methoxy)methyl]-2,2-dimethyl-2H-benzimidazole-1,3-diium 0.1 mM, 14.6% inhibition 235785 3.4.22.49 2-(4-carboxyphenyl)-1,3-dihydroxy-2-methyl-5-nitro-2H-benzimidazole-1,3-diium 0.1 mM, 84.1% inhibition 236018 3.4.22.49 2-butyl-1,3-dihydroxy-2-methyl-5-nitro-2H-benzimidazole-1,3-diium 0.1 mM, 99.8% inhibition 236061 3.4.22.49 2-ethyl-1,3-dihydroxy-2-methyl-5-nitro-2H-benzimidazole-1,3-diium 0.1 mM, 99.6% inhibition 236072 3.4.22.49 2-ethyl-1,3-dihydroxy-5-nitro-2-propyl-2H-benzimidazole-1,3-diium 0.1 mM, 99.2% inhibition 236073 3.4.22.49 4-bromo-1,3-dihydroxy-2,2-dimethyl-6-nitro-2H-benzimidazole-1,3-diium 0.1 mM, 100% inhibition 236232 3.4.22.49 5-(butylamino)-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium 0.1 mM, 40.9% inhibition 236290 3.4.22.49 5-bromo-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium 0.1 mM, 24.6% inhibition 236293 3.4.22.49 5-carboxy-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium 0.1 mM, 24.4% inhibition 236294 3.4.22.49 5-ethoxy-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium 0.1 mM, 21.2% inhibition 236295 3.4.22.49 5-ethoxy-6-fluoro-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium 0.1 mM, 25.2% inhibition 236296 3.4.22.49 5-fluoro-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium 0.1 mM, 35.4% inhibition 236297 3.4.22.49 5-fluoro-1,3-dihydroxy-2,2-dimethyl-6-nitro-2H-benzimidazole-1,3-diium 0.1 mM, 60.1% inhibition 236298 3.4.22.49 5-hexyl-1,3-dihydroxy-2,2-dimethyl-2H-benzimidazole-1,3-diium 0.1 mM, 39.3% inhibition 236299 3.4.22.49 5-nitro-2,1,3-benzoxadiazole 0.1 mM, 43.1% inhibition 236303 3.4.22.49 actin - 796 3.4.22.49 Aki1 - 201890 3.4.22.49 astrin - 201889 3.4.22.49 Cdc55 results suggest that Cdc55 acts as inhibitor downstream from shugoshin 151686 3.4.22.49 Cdk1 kinase phosphorylation-dependent binding of the cyclin B1 subunit of Cdk1 kinase to a Cdc6-like domain of separase inhibits separase 139105 3.4.22.49 cyclin B - 3739 3.4.22.49 cyclin B1 - 23594 3.4.22.49 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 201892 3.4.22.49 additional information nuclear exclusion of separase might provide the means to preclude cohesin cleavage at telophase and G1 stage of the cell cycle 2 3.4.22.49 additional information cohesin cleavage is inhibited by a PP2ACdc55-dependent mechanism 2 3.4.22.49 additional information separase is kept inactive in human cells by Cdk(Cdc2)-dependent phosphorylation even when securin is degraded 2 3.4.22.49 Pds1 Pds1 is a chaperone, inhibition of Esp1 by overexpression of undegradable Pds1 blocks mitotic exit via blockage of cohesin cleavage 151687 3.4.22.49 peptide acyloxymethyl ketone derivative of human SCC1 cleavage site peptide, chloromethyl ketone derivatives of the yeast Scc1 cleavage site 1329 3.4.22.49 securin securin homolog pimples, i.e. PIM, binds and inhibits separase 2052 3.4.22.49 securin - 2052 3.4.22.49 securin small protein that binds to and inhibits separase until all pairs of chromatids have established bipolar spindle attachments 2052 3.4.22.49 securin inhibits the proteolytic activity of separase 2052 3.4.22.49 securin securin inhibits separase by blocking the access of substrates to the active site 2052 3.4.22.49 securin securin regulates both the proteolytic and non-proteolytic activities of separase 2052 3.4.22.49 securin destruction of securin occurs only upon the correct attachment of chromosomes to the spindle 2052 3.4.22.49 securin activity inhibited prior to the onset of the anaphase 2052 3.4.22.49 securin in addition to its inhibitory role, can act as a molecular chaperone of separase, essential for its proper folding 2052 3.4.22.49 securin in addition to its inhibitory role, can act as a molecular chaperone of separase, essential for its proper folding. Securin is dispensable for the growth of normal human cells, in contrast to cancer cells, where depletion of PTTG1 leads to chromosome instability. The human separase-securin complex shows a whale-type distinct elongated pattern. In this complex, securin is thought to interact with the N-part of separase spanned by the ARM repeats. The N- to C-terminus intramolecular interaction in separase molecules is considered to be necessary for their catalytic activation, and this interaction is abolished by securin binding 2052 3.4.22.49 securin in addition to its inhibitory role, can act as a molecular chaperone of separase, essential for its proper folding. The first 156 amino acids of Esp1 seem imperative for the binding of securin Pds1, it interacts with other parts of Esp1 as well 2052 3.4.22.49 securin in addition to its inhibitory role, can act as a molecular chaperone of separase, essential for its proper folding. Interaction takes place between the N-terminus of separase and the C-terminus of securin 2052 3.4.22.49 securin inhibits separase by binding as a pseudo substrate 2052 3.4.22.49 securin Pds1 an inhibitor of separase Esp1 in budding yeast. As Pds1 is degraded, Esp1 is activated, and cells transit into anaphase 167860 3.4.22.49 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 201893 3.4.22.49 sercurin securin persistently binds and inhibits separase during much of metaphase 201891 3.4.22.49 shugoshin prevents separase activation independently of securin, protein phosphatase 2A coupled to regulatory subunit Cdc55 is essential for Shugoshin-mediated inhibition 151685