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

BRENDA support

Literature summary extracted from

  • Edosada, C.Y.; Quan, C.; Wiesmann, C.; Tran, T.; Sutherlin, D.; Reynolds, M.; Elliott, J.M.; Raab, H.; Fairbrother, W.; Wolf, B.B.
    Selective inhibition of fibroblast activation protein protease based on dipeptide substrate specificity (2006), J. Biol. Chem., 281, 7437-7444.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.19.1 plasmid containing full-length acylpeptide hydrolase used as template to generate pFLAG-CMV1 expression construct. This construct encodes amino acids 2-732 of acylpeptide hydrolase. For protein production, transfection into 293 cells synthetic construct
3.4.21.B28 expressed in 293 cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.19.1 Ac-Gly-prolineboronic acid
-
synthetic construct
3.4.19.1 acetyl-Gly-prolineboronic acid selectivity for APH 25fold higher than for fibroblast activation protein synthetic construct
3.4.21.B28 acetyl-Gly-Pro-boronic acid
-
Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.B28 0.106
-
Ile-Pro-7-amido-4-trifluoromethylcoumarin at 23°C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4 Homo sapiens
3.4.21.B28 0.189
-
Lys-Ala-7-amido-4-trifluoromethylcoumarin at 23°C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4 Homo sapiens
3.4.21.B28 0.244
-
Ala-Pro-7-amido-4-trifluoromethylcoumarin at 23°C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4 Homo sapiens
3.4.21.B28 0.245
-
Phe-Pro-7-amido-4-trifluoromethylcoumarin at 23°C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4 Homo sapiens
3.4.21.B28 0.248
-
Gly-Pro-7-amido-4-trifluoromethylcoumarin at 23°C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4 Homo sapiens

Molecular Weight [Da]

EC Number Molecular Weight [Da] Molecular Weight Maximum [Da] Comment Organism
3.4.21.B28 97000
-
SDS-PAGE Homo sapiens
3.4.21.B28 100000
-
2 * 100000, multiangle light scattering in combination with gel filtration chromatography and interferometric refractometry Homo sapiens
3.4.21.B28 200000
-
multiangle light scattering in combination with gel filtration chromatography and interferometric refractometry Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.19.1 synthetic construct
-
-
-
3.4.21.B28 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.19.1 by affinity chromatography, more than 95% pure synthetic construct
3.4.21.B28 M2-anti-FLAG resin column chromatography Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.19.1 acetyl-Ala-7-amido-4-methylcoumarin + H2O
-
synthetic construct acetyl-Ala + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 acetyl-Gly-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens acetyl-Gly-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Ala-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Ala-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Ala-Pro-7-amido-4-trifluoromethylcoumarin + H2O
-
Homo sapiens Ala-Pro + 7-amino-4-trifluoromethylcoumarin
-
?
3.4.21.B28 Arg-Pro-7-amido-4-methylcoumarin + H2O preferred substrate Homo sapiens Arg-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 benzyloxycarbonyl-Gly-Pro-7-amido-4-methyl-3-carbamoylcoumarin + H2O
-
Homo sapiens benzyloxycarbonyl-Gly-Pro + 7-amino-4-methyl-3-carbamoylcoumarin
-
?
3.4.21.B28 biotinyl-Gly-Pro-7-amido-4-methyl-3-carbamoylcoumarin + H2O
-
Homo sapiens biotinyl-Gly-Pro + 7-amino-4-methyl-3-carbamoylcoumarin
-
?
3.4.21.B28 Gln-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Gln-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Glu-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Glu-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Gly-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Gly-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Gly-Pro-7-amido-4-trifluoromethylcoumarin + H2O
-
Homo sapiens Gly-Pro + 7-amino-4-trifluoromethylcoumarin
-
?
3.4.21.B28 Ile-Pro-7-amido-4-methylcoumarin + H2O most preferred substrate Homo sapiens Ile-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Ile-Pro-7-amido-4-trifluoromethylcoumarin + H2O
-
Homo sapiens Ile-Pro + 7-amino-4-trifluoromethylcoumarin
-
?
3.4.21.B28 Leu-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Leu-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Lys-Ala-7-amido-4-trifluoromethylcoumarin + H2O
-
Homo sapiens Lys-Ala + 7-amino-4-trifluoromethylcoumarin
-
?
3.4.21.B28 Lys-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Lys-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Met-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Met-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 additional information shows very weak activity against acetyl-Ser-Pro-7-amido-4-methylcoumarin, Asp-Pro-7-amido-4-methylcoumarin, His-Pro-7-amido-4-methylcoumarin and Asn-Pro-7-amido-4-methylcoumarin, does not cleave succinyl-Gly-Pro-7-amido-4-methyl-3-carbamoylcoumarin, Gly-Ala-7-amido-4-methylcoumarin, acetyl-Ala-Pro-7-amido-4-methylcoumarin, acetyl-Asp-Pro-7-amido-4-methylcoumarin, acetyl-Glu-Pro-7-amido-4-methylcoumarin, acetyl-Phe-Pro-7-amido-4-methylcoumarin, acetyl-His-Pro-7-amido-4-methylcoumarin, acetyl-Ile-Pro-7-amido-4-methylcoumarin, acetyl-Lys-Pro-7-amido-4-methylcoumarin, acetyl-Leu-Pro-7-amido-4-methylcoumarin, acetyl-Met-Pro-7-amido-4-methylcoumarin, acetyl-Asn-Pro-7-amido-4-methylcoumarin, acetyl-Pro-Pro-7-amido-4-methylcoumarin, acetyl-Gln-Pro-7-amido-4-methylcoumarin, acetyl-Arg-Pro-7-amido-4-methylcoumarin, acetyl-Thr-Pro-7-amido-4-methylcoumarin, acetyl-Val-Pro-7-amido-4-methylcoumarin, and acetyl-Tyr-Pro-7-amido-4-methylcoumarin Homo sapiens ?
-
?
3.4.21.B28 N-formyl-Gly-Pro-7-amido-4-methyl-3-carbamoylcoumarin + H2O
-
Homo sapiens N-formyl-Gly-Pro + 7-amino-4-methyl-3-carbamoylcoumarin
-
?
3.4.21.B28 N-methyl-Gly-Pro-7-amido-4-methyl-3-carbamoylcoumarin + H2O
-
Homo sapiens N-methyl-Gly-Pro + 7-amino-4-methyl-3-carbamoylcoumarin
-
?
3.4.21.B28 Phe-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Phe-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Phe-Pro-7-amido-4-trifluoromethylcoumarin + H2O
-
Homo sapiens Phe-Pro + 7-amino-4-trifluoromethylcoumarin
-
?
3.4.21.B28 Pro-Pro-7-amido-4-methylcoumarin + H2O preferred substrate Homo sapiens Pro-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Ser-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Ser-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Thr-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Thr-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Tyr-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Tyr-Pro + 7-amino-4-methylcoumarin
-
?
3.4.21.B28 Val-Pro-7-amido-4-methylcoumarin + H2O
-
Homo sapiens Val-Pro + 7-amino-4-methylcoumarin
-
?

Subunits

EC Number Subunits Comment Organism
3.4.21.B28 homodimer 2 * 100000, multiangle light scattering in combination with gel filtration chromatography and interferometric refractometry Homo sapiens

Synonyms

EC Number Synonyms Comment Organism
3.4.19.1 acylpeptide hydrolase
-
synthetic construct
3.4.19.1 APH
-
synthetic construct
3.4.21.B28 FAP
-
Homo sapiens
3.4.21.B28 fibroblast activation protein protease
-
Homo sapiens

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.21.B28 0.01
-
Lys-Ala-7-amido-4-trifluoromethylcoumarin at 23°C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4 Homo sapiens
3.4.21.B28 1.1
-
Phe-Pro-7-amido-4-trifluoromethylcoumarin at 23°C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4 Homo sapiens
3.4.21.B28 5.6
-
Gly-Pro-7-amido-4-trifluoromethylcoumarin at 23°C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4 Homo sapiens
3.4.21.B28 6.9
-
Ile-Pro-7-amido-4-trifluoromethylcoumarin at 23°C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4 Homo sapiens
3.4.21.B28 14.2
-
Ala-Pro-7-amido-4-trifluoromethylcoumarin at 23°C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.19.1 0.000575
-
Ac-Gly-prolineboronic acid
-
synthetic construct
3.4.21.B28 0.000023
-
acetyl-Gly-Pro-boronic acid
-
Homo sapiens