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Literature summary for 3.4.22.1 extracted from

  • Dong, Y.; Lin, J.; Lu, X.; Zheng, Z.; Ren, X.; Zhang, H.; He, J.; Yang, J.
    Cathepsin B inhibitory tetraene lactones from the fungus Talaromyces wortmannii (2009), Helv. Chim. Acta, 92, 567-574.
No PubMed abstract available
Search for more literature for 3.4.22.1

Application

Application Comment Organism
drug development cathepsin B is a possible therapeutic target for the control of tumor progression Mus musculus

Inhibitors

Inhibitors Comment Organism Structure
leupeptin
-
 Mus musculus
additional information cathepsin B inhibitory activity of tetraene lactones from the fungus Talaromyces wortmannii, overview Mus musculus
wortmannilactone E i.e. (19S)-(4S,7R)-7-[(1E,3E,5E,7E)-8-[(2S,5S,6S)-5,6-dihydro-5-hydroxy-3,5,6-trimethyl-2H-pyran-2-yl]nona-1,3,5,7-tetraen-1-yl]-4,6,7-trimethyl-2-oxabicyclo[2.2.1]heptane-3,5-dione, isolated from the culture medium of the soil filamentous fungus Talaromyces wortmannii, Chuxiong, Yunnan Province, China. Determination of structure and relative configuration by 1D- and 2D-NMR techniques, overview Mus musculus
wortmannilactone F i.e. (19R)-(4S,7R)-7-[(1E,3E,5E,7E)-8-[(2S,5R,6S)-5,6-dihydro-5-hydroxy-3,5,6-trimethyl-2H-pyran-2-yl]nona-1,3,5,7-tetraen-1-yl]-4,6,7-trimethyl-2-oxabicyclo[2.2.1]heptane-3,5-dione, isolated from the culture medium of the soil filamentous fungus Talaromyces wortmannii, Chuxiong, Yunnan Province, China. Determination of structure and relative configuration by 1D- and 2D-NMR techniques, overview Mus musculus
wortmannilactone G i.e. methyl (2R)-2-[(3R,4R)-3-[(1E,3E,5E,7E)-8-[(2S,3R,6S)-3,6-dihydro-3-hydroxy-3,5,6-trimethyl-2H-pyran-2-yl]nona-1,3,5,7-tetraen-1-yl]-3,4-dimethyl-5-oxotetrahydrofuran-2-yl]propanoate, isolated from the culture medium of the soil filamentous fungus Talaromyces wortmannii, Chuxiong, Yunnan Province, China. Determination of structure and relative configuration by 1D- and 2D-NMR techniques, overview Mus musculus
wortmannilactone H i.e. (4S,7R)-7-[(1E,3E,5E,7E)-8-[(2S,3R,6S)-3,6-dihydro-3-hydroxy-3,6-dimethyl-2H-pyran-2-yl]nona-1,3,5,7-tetraen-1-yl]-4,6,7-trimethyl-2-oxabicyclo[2.2.1]heptane-3,5-dione, isolated from the culture medium of the soil filamentous fungus Talaromyces wortmannii, Chuxiong, in Chinas Yunnan Province. Determination of structure and relative configuration by 1D- and 2D-NMR techniques, overview Mus musculus

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Mus musculus 5764
-

Organism

Organism UniProt Comment Textmining
Mus musculus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-benzyloxycarbonyl-Arg-Arg-4-methylcoumarin 7-amide + H2O
-
 Mus musculus N-benzyloxycarbonyl-Arg-Arg + 7-amino-4-methylcoumarin
-
 ?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 assay at room temperature Mus musculus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5.5
-
 assay at Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0043
-
 pH 5.5, 22°C Mus musculus wortmannilactone E
0.006
-
 pH 5.5, 22°C Mus musculus wortmannilactone H
0.0065
-
 pH 5.5, 22°C Mus musculus wortmannilactone F
0.013
-
 pH 5.5, 22°C Mus musculus wortmannilactone G
0.075
-
 pH 5.5, 22°C Mus musculus leupeptin