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Literature summary for 3.4.22.56 extracted from

  • Shimmyo, Y.; Kihara, T.; Akaike, A.; Niidome, T.; Sugimoto, H.
    Three distinct neuroprotective functions of myricetin against glutamate-induced neuronal cell death: involvement of direct inhibition of caspase-3 (2008), J. Neurosci. Res., 86, 1836-1845.
    View publication on PubMed
Search for more literature for 3.4.22.56

Inhibitors

Inhibitors Comment Organism Structure
myricetin myricetin directly interacts with the active site of caspase-3 via three hydrogen bonds, via two hydroxyl groups on the B ring of myricetin interacting with Glu123 and the ether oxygen on the C ring interacting with Arg207, and myricetin directly inhibits caspase-3 activity, thereby inhibiting glutamate-induced cell death, but myricetin inhibits glutamate-induced neuronal toxicity by multiple biochemical pathways, e.g. inhibition of NMDA receptor 1 Ser-890 phosphorylation, overview. Molecular docking analysis by Monte Carlo and molecular dynamics simulations Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Rattus norvegicus caspase-3 is involved in glutamate-induced neuronal cell death, overview ?
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 ?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
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-
-

Source Tissue

Source Tissue Comment Organism Textmining
cell culture priary neuronal cell culture derived from cerebral cortex of fetal rats Rattus norvegicus
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cerebral cortex
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 Rattus norvegicus
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neuron
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 Rattus norvegicus
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Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-DEVD-7-amido-4-methylcoumarin + H2O the active site of caspase-3 is located at Cys163, which plays a key role in substrate hydration Rattus norvegicus Ac-DEVD + 7-amino-4-methylcoumarin
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 ?
additional information caspase-3 is involved in glutamate-induced neuronal cell death, overview Rattus norvegicus ?
-
 ?

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0102
-
 pH 7.4, 37°C Rattus norvegicus myricetin