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Literature summary for 3.4.22.43 extracted from

  • Severino, R.P.; Guido, R.V.; Marques, E.F.; Broemme, D.; da Silva, M.F.; Fernandes, J.B.; Andricopulo, A.D.; Vieira, P.C.
    Acridone alkaloids as potent inhibitors of cathepsin V (2011), Bioorg. Med. Chem., 19, 1477-1481.
    View publication on PubMed
Search for more literature for 3.4.22.43

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Pichia pastoris Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1,3,5-trihydroxy-2,8-bis(3-methylbut-2-enyl)-10-methyl-9-acridone
-
 Homo sapiens
1,3,5-trihydroxy-4-methoxy-10-methyl-2,8-bis(3-methylbut-2-enyl)acridin-9(10H)-one
-
 Homo sapiens
2,3-dihydro-4,9-dihydroxy-2-(2-hydroxy-propan-2-yl)-11-methoxy-10-methylfuro[3,2-b]acridin-5(10H)-one
-
 Homo sapiens
3,4-dihydro-3,5,8-trihydroxy-6-methoxy-2,2,7-trimethyl-2H-pyrano[2,3-a]acridin-12(7H)-one
-
 Homo sapiens
5-hydroxynoracronycine
-
 Homo sapiens
citibrasine
-
 Homo sapiens
citrusinine-I
-
 Homo sapiens
citrusinine-II
-
 Homo sapiens
glycocitrine-I
-
 Homo sapiens
glycocitrine-IV
-
 Homo sapiens
pyranofoline
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Homo sapiens 5764
-

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Z-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Z-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
CatV
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0002
-
 citibrasine in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens
0.0005
-
 1,3,5-trihydroxy-4-methoxy-10-methyl-2,8-bis(3-methylbut-2-enyl)acridin-9(10H)-one in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens
0.001
-
 citrusinine-I in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens
0.0011
-
 glycocitrine-IV in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens
0.0012
-
 1,3,5-trihydroxy-2,8-bis(3-methylbut-2-enyl)-10-methyl-9-acridone in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens
0.0017
-
 3,4-dihydro-3,5,8-trihydroxy-6-methoxy-2,2,7-trimethyl-2H-pyrano[2,3-a]acridin-12(7H)-one in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens
0.0042
-
 citrusinine-II in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens
0.0044
-
 2,3-dihydro-4,9-dihydroxy-2-(2-hydroxy-propan-2-yl)-11-methoxy-10-methylfuro[3,2-b]acridin-5(10H)-one in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens
0.01
-
 glycocitrine-I in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0012
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens citibrasine
0.0022
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens glycocitrine-IV
0.0022
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens citrusinine-I
0.0025
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens 1,3,5-trihydroxy-4-methoxy-10-methyl-2,8-bis(3-methylbut-2-enyl)acridin-9(10H)-one
0.0028
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens 3,4-dihydro-3,5,8-trihydroxy-6-methoxy-2,2,7-trimethyl-2H-pyrano[2,3-a]acridin-12(7H)-one
0.0039
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens 1,3,5-trihydroxy-2,8-bis(3-methylbut-2-enyl)-10-methyl-9-acridone
0.0052
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens 2,3-dihydro-4,9-dihydroxy-2-(2-hydroxy-propan-2-yl)-11-methoxy-10-methylfuro[3,2-b]acridin-5(10H)-one
0.01
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens citrusinine-II
0.025
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens glycocitrine-I
0.044
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens pyranofoline
0.048
-
 in 100 mM sodium acetate buffer (pH 5.5) containing 5 mM EDTA and 5 mM dithioerythritol, at 27°C Homo sapiens 5-hydroxynoracronycine