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Literature summary for 3.4.21.59 extracted from

  • Harris, J.L.; Niles, A.; Burdick, K.; Maffitt, M.; Backes, B.J.; Ellman, J.A.; Kuntz, I.; Haak-Frendscho, M.; Craik, C.S.
    Definition of the extended substrate specificity determinants for b-tryptases I and II (2001), J. Biol. Chem., 276, 34941-34947.
    View publication on PubMed

Application

Application Comment Organism
medicine tryptase is a potent activator of pro-uPA, the zymogen form of a protease asociated with tumor metastasis and invasion, viable drug target to create therapeutically useful inhibitors Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
tryptases betaI and betaII heterolougously expressed in the yeast Pichia pastoris Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
acetyl-PRNK-chloromethylketone
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0089
-
Ac-PRNK-AAC pH 7.5, 30°C, betaII tryptase Homo sapiens
0.0145
-
Ac-PRNK-AAC pH 7.5, 30°C, betaI tryptase Homo sapiens
0.0147
-
Ac-PRTK-AAC pH 7.5, 30°C, betaII tryptase Homo sapiens
0.0165
-
Ac-PRNR-AAC pH 7.5, 30°C, betaII tryptase Homo sapiens
0.0186
-
Ac-PRNR-AAC pH 7.5, 30°C, betaI tryptase Homo sapiens
0.0234
-
Ac-PRTK-AAC pH 7.5, 30°C, betaI tryptase Homo sapiens
0.1105
-
Ac-PANK-AAC pH 7.5, 30°C, betaII tryptase Homo sapiens
0.1333
-
Ac-PANK-AAC pH 7.5, 30°C, betaI tryptase Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
secretory granule
-
Homo sapiens 30141
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
additional information Homo sapiens currently unknown whether tryptases perform redundant or unique functions in vivo ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
human
-

Purification (Commentary)

Purification (Comment) Organism
recombinant tryptases betaI and betaII Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-PANKAAC + H2O betaI and betaII tryptase Homo sapiens Ac-PANK + Ala-Ala-Cys
-
?
Ac-PRNKAAC + H2O betaI and betaII tryptase Homo sapiens Ac-PRNK + Ala-Ala-Cys
-
?
Ac-PRNRAAC + H2O betaI and betaII tryptase Homo sapiens Ac-PRNR + Ala-Ala-Cys
-
?
Ac-PRTKAAC + H2O betaI and betaII tryptase Homo sapiens Ac-PRTK + Ala-Ala-Cys
-
?
additional information tryptases betaI and betaII have a strict preference for cleavage after the basic amino acids, lysine and arginine, with only a slight preference for lysine over arginine, prefernce for proline at P4, preference for arginine or lysine at P3 and P2, these enzymes are not controlled by blood plasma proteinase inhibitors and only cleave a few physiological substrates in vitro Homo sapiens ?
-
?
additional information currently unknown whether tryptases perform redundant or unique functions in vivo Homo sapiens ?
-
?

Subunits

Subunits Comment Organism
tetramer
-
Homo sapiens

Synonyms

Synonyms Comment Organism
beta tryptase I
-
Homo sapiens
beta tryptase II
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.97
-
Ac-PRNK-AAC pH 7.5, 30°C, betaII tryptase Homo sapiens
0.99
-
Ac-PRNK-AAC pH 7.5, 30°C, betaI tryptase Homo sapiens
0.99
-
Ac-PRTK-AAC pH 7.5, 30°C, betaI tryptase Homo sapiens
1.1
-
Ac-PANK-AAC pH 7.5, 30°C, betaI tryptase Homo sapiens
1.1
-
Ac-PRTK-AAC pH 7.5, 30°C, betaII tryptase Homo sapiens
3.5
-
Ac-PANK-AAC pH 7.5, 30°C, betaII tryptase Homo sapiens
3.8
-
Ac-PRNR-AAC pH 7.5, 30°C, betaI tryptase Homo sapiens
21.75
-
Ac-PRNR-AAC pH 7.5, 30°C, betaII tryptase Homo sapiens
21.8
-
Ac-PRNR-AAC pH 7.5, 30°C, betaII tryptase Homo sapiens