Application | Comment | Organism |
---|---|---|
drug development | design of a new class of boron peptides as inhibitors of the chymotrypsin-like activity of the 20S proteasome based around the structure of Belactosin C, proteasome inhibitors with therapeutic utility | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
Belactosin C | irreversible inhibitor | Homo sapiens | |
MG-132 | reversible inhibitor | Homo sapiens | |
additional information | boron peptides selectively inhibit the chymotrypsin-like activity (beta5) of 20S proteasome | Homo sapiens | |
N-(tert-butoxycarbonyl)-L-alanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | irreversible inhibitor | Homo sapiens | |
N-(tert-butoxycarbonyl)-L-alanyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | irreversible inhibitor | Homo sapiens | |
N-(tert-butoxycarbonyl)-L-leucyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | irreversible inhibitor | Homo sapiens | |
N-(tert-butoxycarbonyl)-L-phenylalanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | irreversible inhibitor | Homo sapiens | |
N-(tert-butoxycarbonyl)glycyl-N1-benzyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-L-glutamamide | irreversible inhibitor, significant inhibition of 20S proteasome chymotrypsin-like (beta5) activity, inhibitory potency is similar to that of Belactosin C | Homo sapiens | |
N-(tert-butoxycarbonyl)glycyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | irreversible inhibitor, possesses the greatest inhibition of the chymotrypsin-like activity, inhibitory potency is similar to that of Belactosin C. Increases the G2/M cell distribution in a similar manner to that of PS-341, and induces apoptosis at more than 0.001 mM concentration of compound in HeLa cells | Homo sapiens | |
N-(tert-butoxycarbonyl)glycyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | irreversible inhibitor | Homo sapiens | |
N2-(tert-butoxycarbonyl)-N4-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-aspartamide | irreversible inhibitor | Homo sapiens | |
N2-(tert-butoxycarbonyl)-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | irreversible inhibitor | Homo sapiens | |
N2-(tert-butoxycarbonyl)-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | irreversible inhibitor | Homo sapiens | |
PS-341 | reversible inhibitor | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
20S proteasome | - |
Homo sapiens | - |
- |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
erythrocyte | - |
Homo sapiens | - |
HeLa cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | succinyl-Leu-Leu-Val-Tyr + 7-amino-4-methylcoumarin | - |
? |
Synonyms | Comment | Organism |
---|---|---|
chymotrypsin | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00002 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | PS-341 | |
0.00007 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | MG-132 | |
0.00028 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
0.00054 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N1-benzyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-L-glutamamide | |
0.00084 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | N-(tert-butoxycarbonyl)-L-alanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
0.00147 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | N-(tert-butoxycarbonyl)-L-phenylalanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
0.0015 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | N-(tert-butoxycarbonyl)-L-leucyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
0.00274 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
0.00412 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | N2-(tert-butoxycarbonyl)-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
0.00428 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | N-(tert-butoxycarbonyl)-L-alanyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
0.00451 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | N2-(tert-butoxycarbonyl)-N4-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-aspartamide | |
0.01 | - |
at 37°C for 1 h, in 20 mM Tris buffer, pH 8.0, 0.5 mM EDTA and 0.035% SDS | Homo sapiens | N2-(tert-butoxycarbonyl)-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide |