Inhibitors | Comment | Organism | Structure |
---|---|---|---|
c[Ala-Leu-Leu-Glu(Leu-vinyl ester)] | - |
Homo sapiens | |
c[Gly-Leu-Leu-Glu(Leu-vinyl ester)] | - |
Homo sapiens | |
c[Ser-Leu-Leu-Glu(Leu-vinyl ester)] | - |
Homo sapiens | |
c[Val-Leu-Leu-Glu(Leu-vinyl ester)] | - |
Homo sapiens | |
H-Ala-Leu-Leu-Glu(Leu-vinyl ester)-NH2 | - |
Homo sapiens | |
H-Gly-Leu-Leu-Glu(Leu-vinyl ester)-NH2 | - |
Homo sapiens | |
H-Ser-Leu-Leu-Glu(Leu-vinyl ester)-NH2 | - |
Homo sapiens | |
H-Val-Leu-Leu-Glu(Leu-vinyl ester)-NH2 | - |
Homo sapiens | |
additional information | study of potent and selective inhibition of the 20S proteasome beta1 catalytic subsite by a series of vinyl ester cyclopeptide analogues synthesized on the basis of a class of cyclopeptides derived from linear prototype inhibitors, in which the exocyclic pharmacophoric unit Leu-vinyl ester is linked to the c-carboxyl group of the glutamic acid residue at the C-terminus. The compounds inhibit the caspase-like activity of the proteasome at nanomolar concentrations, and demonstrate good resistance to proteolysis and a capacity to permeate the cell membrane | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | three major proteolytic activities of the proteasome can be distinguished as trypsin-like, chymotrypsin-like, and peptidyl-glutamyl peptide hydrolase activities, which cleave peptide bonds on the carboxyl side of basic, hydrophobic, and acidic amino acid residues, respectively. The catalytic core of the 20S proteasome is a Thr residue, responsible for the catalytic cleavage of substrates through nucleophilic attack | ? | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
lymphoblastoid cell line | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
benzoyl-LRR-4-methyl-7-amido-coumarin + H2O | trypsin-like proteasome activity with the specific fluorogenic substrate | Homo sapiens | benzoyl-LRR + 4-methyl-7-amino-coumarin | - |
? | |
additional information | three major proteolytic activities of the proteasome can be distinguished as trypsin-like, chymotrypsin-like, and peptidyl-glutamyl peptide hydrolase activities, which cleave peptide bonds on the carboxyl side of basic, hydrophobic, and acidic amino acid residues, respectively. The catalytic core of the 20S proteasome is a Thr residue, responsible for the catalytic cleavage of substrates through nucleophilic attack | Homo sapiens | ? | - |
? | |
N-succinyl-LLVY-7-amido-4-methylcoumarin + H2O | chymotrypsin-like proteasome activity with the specific fluorogenic substrate | Homo sapiens | N-succinyl-LLVY + 7-amino-4-methylcoumarin | - |
? | |
Z-LLE-4-methyl-7-amido-coumarin + H2O | post-acidic proteasome activity with the specific fluorogenic substrate | Homo sapiens | Z-LLE + 4-methyl-7-amino-coumarin | - |
? |
Synonyms | Comment | Organism |
---|---|---|
20S proteasome | - |
Homo sapiens |
proteasome | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
additional information | inhibition of this enzymatic activity with beta-subunit-specific proteasome inhibitors may provide an anti-tumoral effect by inhibiting cell proliferation and angiogenesis, and by selectively inducing apoptosis of tumor cells | Homo sapiens |