Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.21.119 extracted from

  • Gruba, N.; Bielecka, E.; Wysocka, M.; Wojtysiak, A.; Brzezinska-Bodal, M.; Sychowska, K.; Kalinska, M.; Magoch, M.; Pecak, A.; Falkowski, K.; Wisniewska, M.; Sasiadek, L.; Plaza, K.; Kroll, E.; Pejkovska, A.; Rehders, M.; Brix, K.; Dubin, G.; Kantyka, T.; Potempa, J.; Lesner, A.
    Development of chemical tools to monitor human kallikrein 13 (KLK13) activity (2019), Int. J. Mol. Sci., 20, 1557 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.21.119

Application

Application Comment Organism
analysis substrate substrate ABZ-Val-Arg-Phe-Arg-Ser-Thr-Gln-Tyr(3-NO2)-NH2 is suitable for determination of KLK13 activity and is successfully converted into an activity-based probe by the incorporation of a chloromethylketone warhead and biotin bait. The modified subvsrtae is applicable in complex biological samples Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
acetyl-VRFR-chloromethylketone
-
 Homo sapiens
butyl-VRFR-chloromethylketone
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.01
-
 ABZ-VRFRSTQ-Tyr(3-NO2)-NH2 pH 7.5, 37°C Homo sapiens
0.015
-
 ABZ-VRFRSTS-Tyr(3-NO2)-NH2 pH 7.5, 37°C Homo sapiens
0.018
-
 ABZ-Val-Arg-Phe-Arg-5-amino-2-nitrobenzoic acid pH 7.5, 37°C Homo sapiens
0.02
-
 ABZ-VRFRSTG-Tyr(3-NO2)-NH2 pH 7.5, 37°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9UKR3
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ABZ-Val-Arg-Phe-Arg-5-amino-2-nitrobenzoic acid + H2O kinetically preferred substrate Homo sapiens ABZ-Val-Arg-Phe-Arg + 5-amino-2-nitrobenzoic acid
-
 ?
ABZ-VRFRSTG-Tyr(3-NO2)-NH2 + H2O
-
 Homo sapiens ABZ-VRFR + STG-Tyr(3-NO2)-NH2
-
 ?
ABZ-VRFRSTQ-Tyr(3-NO2)-NH2 + H2O
-
 Homo sapiens ABZ-VRFR + STQ-Tyr(3-NO2)-NH2
-
 ?
ABZ-VRFRSTS-Tyr(3-NO2)-NH2 + H2O
-
 Homo sapiens ABZ-VRFR + STS-Tyr(3-NO2)-NH2
-
 ?

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
94.36
-
 ABZ-Val-Arg-Phe-Arg-5-amino-2-nitrobenzoic acid pH 7.5, 37°C Homo sapiens
96.4
-
 ABZ-VRFRSTQ-Tyr(3-NO2)-NH2 pH 7.5, 37°C Homo sapiens
113.1
-
 ABZ-VRFRSTS-Tyr(3-NO2)-NH2 pH 7.5, 37°C Homo sapiens
169.4
-
 ABZ-VRFRSTG-Tyr(3-NO2)-NH2 pH 7.5, 37°C Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0024
-
 pH 7.5, 37°C Homo sapiens acetyl-VRFR-chloromethylketone
0.005
-
 pH 7.5, 37°C Homo sapiens butyl-VRFR-chloromethylketone

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
5310
-
 ABZ-Val-Arg-Phe-Arg-5-amino-2-nitrobenzoic acid pH 7.5, 37°C Homo sapiens
7710
-
 ABZ-VRFRSTS-Tyr(3-NO2)-NH2 pH 7.5, 37°C Homo sapiens
9640
-
 ABZ-VRFRSTQ-Tyr(3-NO2)-NH2 pH 7.5, 37°C Homo sapiens
68620
-
 ABZ-VRFRSTG-Tyr(3-NO2)-NH2 pH 7.5, 37°C Homo sapiens