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Literature summary for 3.4.25.1 extracted from

  • Baldisserotto, A.; Marastoni, M.; Gavioli, R.; Tomatis, R.
    New cyclic peptide proteasome inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 1966-1969.
    View publication on PubMed

Inhibitors

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/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
lymphoblastoid cell line
-
Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms Comment Organism
20S proteasome
-
Homo sapiens
proteasome
-
Homo sapiens

General Information

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