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Literature summary for 3.4.22.56 extracted from

  • Van Kersavond, T.; Konopatzki, R.; Chakrabarty, S.; Blank-Landeshammer, B.; Sickmann, A.; Verhelst, S.H.L.
    Short peptides with uncleavable peptide bond mimetics as photoactivatable caspase-3 inhibitors (2019), Molecules, 24, E206 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expression in Escherichia coli Mammalia

Inhibitors

Inhibitors Comment Organism Structure
acetyl-Asp-Glu-Val-Asp(psi)(CH2NH)-Ala-NH2 no ihibition without irradiation, complete inhibition when the sample is irradiated Mammalia
hexynoyl-Asp-Glu-Val-Asp(psi)(CH2NH)-Ala-Bpa-NH2 no ihibition without irradiation, complete inhibition when the sample is irradiated Mammalia
hexynoyl-Asp-Glu-Val-Asp(psi)(CH2NH)-Ala-NH2 no ihibition without irradiation, complete inhibition when the sample is irradiated Mammalia
hexynoyl-Asp-Glu-Val-Asp(psi)(CH2NH)-Ala-photoLeu-NH2 no ihibition without irradiation, complete inhibition when the sample is irradiated Mammalia
hexynoyl-Asp-Glu-Val-Asp(triazolo)-Ala-Bpa-Gly-NH2 weak inhibition Mammalia
hexynoyl-Bpa-Asp-Glu-Val-Asp(psi)(CH2NH)-Ala-NH2 no ihibition without irradiation, complete inhibition when the sample is irradiated Mammalia
hexynoyl-photoLeu-Asp-Glu-Val-Asp(psi)(CH2NH)-Ala-NH2 no ihibition without irradiation, complete inhibition when the sample is irradiated Mammalia
additional information molecules with psi(CH2NH) or triazole uncleavable peptide bond do not show any inhibition of caspase activity without irradiation. When the samples are irradiated, the psi(CH2NH) peptides with benzophenone or diazirine photocrosslinkers show complete inhibition Mammalia

Organism

Organism UniProt Comment Textmining
Mammalia
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-Asp-Glu-Val-Asp-7-amido-4-methylcoumarin + H2O
-
Mammalia Ac-Asp-Glu-Val-Asp + 7-amino-4-methylcoumarin
-
?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Mammalia

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Mammalia