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Literature summary for 3.4.25.1 extracted from

  • Wang, C.C.; Bozdech, Z.; Liu, C.l.; Shipway, A.; Backes, B.J.; Harris, J.L.; Bogyo, M.
    Biochemical analysis of the 20 S proteasome of Trypanosoma brucei (2003), J. Biol. Chem., 278, 15800-15808.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
leupeptin IC50: 0.0015 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin, most potent inhibitor for hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.1 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin Trypanosoma brucei
NPLLLVS IC50: 0.04 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.007 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin, most potent inhibitor for hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin Trypanosoma brucei
NPLLNVS IC50: 0.063 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-carbamoylcoumarin. IC50: 0.077 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin Trypanosoma brucei
YLLLVS IC50: 0.048 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.033 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin Trypanosoma brucei

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.027
-
acetyl-YWTQ-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Homo sapiens
0.032
-
acetyl-EPFD-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Homo sapiens
0.038
-
acetyl-YWTQ-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Trypanosoma brucei
0.088
-
acetyl-EPFD-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Trypanosoma brucei
0.11
-
acetyl-norleucine-Arg-norleucine-Arg-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Homo sapiens
0.36
-
acetyl-HHSL-7-amido-4-carbamoylcoumarin pH 7.5, 25°C Homo sapiens
0.67
-
acetyl-norleucine-Arg-norleucine-Arg-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Trypanosoma brucei

Molecular Weight [Da]

Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
22700
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
23200
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
23800
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
24000
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
24300
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
24500
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
24700
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
25000
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
27000
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
27500
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
28000
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
29000
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei
33000
-
1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Trypanosoma brucei O96780 beta2 subunit
-
Trypanosoma brucei O96787 beta1 subunit
-
Trypanosoma brucei O96788 alpha6 subunit
-
Trypanosoma brucei Q9BMX8 beta7 subunit
-
Trypanosoma brucei Q9GU36 alpha3 subunit
-
Trypanosoma brucei Q9GU37 alpha1 subunit
-
Trypanosoma brucei Q9NDA1 beta3 subunit
-
Trypanosoma brucei Q9NDA2 alpha4 subunit
-
Trypanosoma brucei Q9NDA3 alpha7 subunit
-
Trypanosoma brucei Q9NHC5 beta5 subunit
-
Trypanosoma brucei Q9NHC6 beta4 subunit
-
Trypanosoma brucei Q9U793 alpha2 subunit
-
Trypanosoma brucei Q9U794 beta6 subunit
-
Trypanosoma brucei Q9XZG5 alpha5 subunit
-

Posttranslational Modification

Posttranslational Modification Comment Organism
proteolytic modification the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei

Purification (Commentary)

Purification (Comment) Organism
-
Trypanosoma brucei

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-hydroxy-3-nitrophenol-Leu-Leu-Asn-vinylsulfone + H2O
-
Trypanosoma brucei ?
-
?
4-hydroxy-3-nitrophenyl-Leu-Leu-Lys-vinylsulfone + H2O
-
Trypanosoma brucei ?
-
?
acetyl-EPFD-7-amido-4-carbamoylcoumarin + H2O
-
Homo sapiens ?
-
?
acetyl-EPFD-7-amido-4-carbamoylcoumarin + H2O
-
Trypanosoma brucei ?
-
?
acetyl-HHSL-7-amido-4-carbamoylcoumarin + H2O
-
Homo sapiens ?
-
?
acetyl-norleucine-Arg-norleucine-Arg-7-amido-4-carbamoylcoumarin + H2O
-
Homo sapiens ?
-
?
acetyl-norleucine-Arg-norleucine-Arg-7-amido-4-carbamoylcoumarin + H2O
-
Trypanosoma brucei ?
-
?
acetyl-YWTQ-7-amido-4-carbamoylcoumarin + H2O
-
Homo sapiens ?
-
?
acetyl-YWTQ-7-amido-4-carbamoylcoumarin + H2O
-
Trypanosoma brucei ?
-
?
Gly-Gly-Arg-7-amido-4-methylcoumarin + H2O
-
Trypanosoma brucei ?
-
?
additional information overall substrate preference for hydrophobic residues at the P1 to P4 positions in a substrate. This overall stringency is relaxed in the 11 S regulatory (PA26)-20 S proteasome complex, which shows both appreciable activities for cleavage after acidic amino acids and a broadened activity for cleavage after basic amino acids. The 20S proteasome shows appreciable activity for cleavage after P1-Gln that is minimally observed in the human counterpart Trypanosoma brucei ?
-
?
additional information the 20S proteasome of Trypanosoma brucei shows appreciable activity for cleavage after P1-Gln that is minimally observed in the human counterpart Homo sapiens ?
-
?
succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin + H2O
-
Trypanosoma brucei ?
-
?
Tyr-Leu-Leu-Leu-vinylsulfone + H2O
-
Trypanosoma brucei ?
-
?

Subunits

Subunits Comment Organism
tetradecamer 1 * 28000, alpha1, + 1 * 24300, alpha2, + 1 * 33000, alpha3, + 1 * 27000, alpha4, + 1 * 27500, alpha5, + 1 * 29000, alpha6, + 1 * 25000, alpha7, + 1 * 24700, beta1, + 1 * 24000, beta2, + 1 * 23200, beta3, + 1 * 23800, beta4, + 1 * 22700, beta5, + 1 * 24500, beta6, + 1 * 24000, beta7, the 20S proteasome is made up of seven alpha-subunits and seven beta-subunits. Of the seven beta-type subunits, five contain pro-sequences that are proteolytically removed during assembly, and three of them are predicted to be catalytic based on primary sequence Trypanosoma brucei

Synonyms

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

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.031 0.51 acetyl-norleucine-Arg-norleucine-Arg-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Trypanosoma brucei
0.27
-
acetyl-YWTQ-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Homo sapiens
0.97
-
acetyl-EPFD-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Homo sapiens
2.7
-
acetyl-EPFD-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Trypanosoma brucei
3.3
-
acetyl-norleucine-Arg-norleucine-Arg-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Homo sapiens
3.3
-
acetyl-YWTQ-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Trypanosoma brucei
4.67
-
acetyl-YWTQ-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Trypanosoma brucei
5.34
-
acetyl-norleucine-Arg-norleucine-Arg-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Homo sapiens
8.15
-
acetyl-norleucine-Arg-norleucine-Arg-7-amido-4-carbamoylcoumarin pH 7.8, 25°C Trypanosoma brucei
36.3
-
acetyl-HHSL-7-amido-4-carbamoylcoumarin pH 7.5, 25°C Homo sapiens

pI Value

Organism Comment pI Value Maximum pI Value
Trypanosoma brucei pI-values of the subunits
-
additional information

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.007
-
IC50: 0.04 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.007 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin, most potent inhibitor for hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-meth Trypanosoma brucei NPLLLVS
0.033
-
IC50: 0.048 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.033 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin Trypanosoma brucei YLLLVS
0.077
-
IC50: 0.063 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-carbamoylcoumarin. IC50: 0.077 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin Trypanosoma brucei NPLLNVS
0.1
-
IC50: 0.0015 mM, inhibition of hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin, most potent inhibitor for hydrolysis of Gly-Gly-Arg-7-amido-4-methylcoumarin. IC50: 0.1 mM, inhibition of hydrolysis of succinyl-Leu-Leu-Val-Tyr-7-amido-4-methylcoumarin Trypanosoma brucei leupeptin