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Literature summary for 3.4.25.1 extracted from
- Synthesis and biological evaluation of boron peptide analogues of Belactosin C as proteasome inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 3220-3224.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| belactosin A | isolated from a Streptomyces sp. strain | Homo sapiens |  |
| Belactosin C | isolated from a Streptomyces sp. strain | Homo sapiens | |
| epoxomicin | irreversible inhibitor | Homo sapiens | |
| MG-132 | reversible inhibitor | Homo sapiens | |
| additional information | design and synthesis of boron peptide analogue proteasome inhibitors based on the structure of belactosin C, overview | Homo sapiens | |
| N-(tert-butoxycarbonyl)-L-alanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | - |
Homo sapiens | |
| N-(tert-butoxycarbonyl)-L-alanyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | - |
Homo sapiens | |
| N-(tert-butoxycarbonyl)-L-isoleucyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | - |
Homo sapiens | |
| N-(tert-butoxycarbonyl)-L-phenylalanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | - |
Homo sapiens | |
| N-(tert-butoxycarbonyl)glycyl-N1-benzyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-L-glutamamide | shows significant inhibition of 20S proteasome chymotrypsin-like, b5 activity | Homo sapiens | |
| N-(tert-butoxycarbonyl)glycyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | shows significant inhibition of 20S proteasome chymotrypsin-like, b5 activity | Homo sapiens | |
| N-(tert-butoxycarbonyl)glycyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | - |
Homo sapiens | |
| N2-(tert-butoxycarbonyl)-N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-3-[(naphthalen-2-ylmethyl)amino]-3-oxo-D-alaninamide | - |
Homo sapiens | |
| N2-(tert-butoxycarbonyl)-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | - |
Homo sapiens | |
| N2-(tert-butoxycarbonyl)-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | - |
Homo sapiens | |
| NLVS | irreversible inhibitor | Homo sapiens | |
| PS-341 | reversible inhibitor | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| HeLa-S3 cell | - |
Homo sapiens | - |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| 20S proteasome | - |
Homo sapiens |
| proteasome | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| additional information | - |
cell growth inhibition activities, overview | Homo sapiens | additional information | |
| 0.00028 | - |
chymotrypsin-like, b5 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.00054 | - |
chymotrypsin-like, b5 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N1-benzyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-L-glutamamide | |
| 0.00068 | - |
caspase-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N2-(tert-butoxycarbonyl)-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
| 0.00084 | - |
chymotrypsin-like, b5 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-alanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.00147 | - |
chymotrypsin-like, b5 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-phenylalanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.0015 | - |
chymotrypsin-like, b5 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-isoleucyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.00274 | - |
chymotrypsin-like, b5 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
| 0.00412 | - |
chymotrypsin-like, b5 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N2-(tert-butoxycarbonyl)-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
| 0.00428 | - |
chymotrypsin-like, b5 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-alanyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
| 0.00451 | - |
chymotrypsin-like, b5 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N2-(tert-butoxycarbonyl)-N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-3-[(naphthalen-2-ylmethyl)amino]-3-oxo-D-alaninamide | |
| 0.00723 | - |
caspase-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N2-(tert-butoxycarbonyl)-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.00854 | - |
caspase-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.00984 | - |
caspase-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N1-benzyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-L-glutamamide | |
| 0.01 | - |
above, caspase-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-alanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.01 | - |
above, caspase-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-phenylalanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.01 | - |
above, caspase-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
| 0.01 | - |
above, caspase-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-alanyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
| 0.01 | - |
above, caspase-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-isoleucyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.01 | - |
above, caspase-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N2-(tert-butoxycarbonyl)-N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-3-[(naphthalen-2-ylmethyl)amino]-3-oxo-D-alaninamide | |
| 0.01 | - |
above, chymotrypsin-like, b5 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N2-(tert-butoxycarbonyl)-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.01 | - |
above, trypsin-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.01 | - |
above, trypsin-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-alanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.01 | - |
above, trypsin-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-phenylalanyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.01 | - |
above, trypsin-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N1-benzyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-L-glutamamide | |
| 0.01 | - |
above, trypsin-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)glycyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
| 0.01 | - |
above, trypsin-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-alanyl-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
| 0.01 | - |
above, trypsin-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N2-(tert-butoxycarbonyl)-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.01 | - |
above, trypsin-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N2-(tert-butoxycarbonyl)-N6-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N-(naphthalen-2-ylmethyl)-6-oxo-L-lysinamide | |
| 0.01 | - |
above, trypsin-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N-(tert-butoxycarbonyl)-L-isoleucyl-N5-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-N1-(naphthalen-2-ylmethyl)-L-glutamamide | |
| 0.01 | - |
above, trypsin-like, b1 activity of 20S proteasome, pH not specified in the publication, temperature not specified in the publication | Homo sapiens | N2-(tert-butoxycarbonyl)-N-[(1R)-1-(dihydroxyboranyl)-3-methylbutyl]-3-[(naphthalen-2-ylmethyl)amino]-3-oxo-D-alaninamide | |
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