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Literature summary for 3.4.21.117 extracted from

  • Doering, K.; Meder, G.; Hinnenberger, M.; Woelcke, J.; Mayr, L.M.; Hassiepen, U.
    A fluorescence lifetime-based assay for protease inhibitor profiling on human kallikrein 7 (2009), J. Biomol. Screen., 14, 1-9.
    View publication on PubMed
Search for more literature for 3.4.21.117

Application

Application Comment Organism
molecular biology an activity assay for human kallikrein 7 is developed using a blue-fluorescent acridone dye, featuring a remarkably long lifetime that can be quenched by either of the 2 natural amino acids, tyrosine and tryptophan. Incorporating this probe and 1 of the quenching amino acids on either side of the scissile bond of the substrate peptide makes it possible to monitor the enzymatic activity by quantifying the increase in the fluorescence lifetime signal. A systematic investigation of substrate structures leads to a homogenous, microplate-based, compound profiling assay that yields inhibitory constants down into the single-digit nanomolar range Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
expressed as a His-tagged fusionprotein in Escherichia coli Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-(2-fluoro-phenyl)-5,6,7,8-tertrahydro-benzol[4,5]thieno[2,3-d][1,3]oxazin-4-one
-
 Homo sapiens
DMSO catalytic activity of the protease decreases with increasing DMSO concentration Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0059
-
 Ac-ED(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)KPILFRLGK(4-(4-dimethylaminophenylazo)benzoic acid)E-NH2 kcat/KM: 170000/Msec Homo sapiens
0.048
-
 Ac-EFKPILWRLGC-(6-(9-oxo-9H-acridin-10-yl)-hexanoate)E-NH2 Vmax: 12 nM/sec Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P49862
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Ac-ED(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)KPILFRLGK(4-(4-dimethylaminophenylazo)benzoic acid)E-NH2 + H2O
-
 Homo sapiens ?
-
 ?
Ac-EFKPILWRLGC-(6-(9-oxo-9H-acridin-10-yl)-hexanoate)E-NH2 + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
kallikrein 7
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.48
-
 Ac-EFKPILWRLGC-(6-(9-oxo-9H-acridin-10-yl)-hexanoate)E-NH2
-
 Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5.6
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00007
-
-
 Homo sapiens 2-(2-fluoro-phenyl)-5,6,7,8-tertrahydro-benzol[4,5]thieno[2,3-d][1,3]oxazin-4-one