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Literature summary for 3.4.21.B28 extracted from

  • Meadows, S.A.; Edosada, C.Y.; Mayeda, M.; Tran, T.; Quan, C.; Raab, H.; Wiesmann, C.; Wolf, B.B.
    Ala657 and conserved active site residues promote fibroblast activation protein endopeptidase activity via distinct mechanisms of transition state stabilization (2007), Biochemistry, 46, 4598-4605.
    View publication on PubMed
Search for more literature for 3.4.21.B28

Cloned(Commentary)

Cloned (Comment) Organism
expressed in HEK-293 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
A657D increased activity Homo sapiens
A657F decreased activity Homo sapiens
A657G decreased activity Homo sapiens
A657N increased activity Homo sapiens
A657Q decreased activity Homo sapiens
A657S decreased activity Homo sapiens
A657T decreased activity Homo sapiens
A657V decreased activity Homo sapiens
E203A diminished activity Homo sapiens
E203A/E204A diminished activity Homo sapiens
E203D diminished activity Homo sapiens
E203D/E204D diminished activity Homo sapiens
E203Q diminished activity Homo sapiens
E203Q/E204Q diminished activity Homo sapiens
E204A diminished activity Homo sapiens
E204D diminished activity Homo sapiens
E204Q diminished activity Homo sapiens
N704A diminished activity Homo sapiens
R123A diminished activity Homo sapiens
R123K diminished activity Homo sapiens
R123M diminished activity Homo sapiens
Y656F diminished activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
acetyl-Gly-boro-Pro
-
 Homo sapiens
acetyl-Gly-Pro-CN
-
 Homo sapiens
Ile-boro-Pro
-
 Homo sapiens
Ile-Pro-CN
-
 Homo sapiens
Val-boro-Pro
-
 Homo sapiens
Val-Pro-CN
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.062
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.087
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657N, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.091
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.1
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.135
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657S, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.14
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203D/E204D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.25
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin wild type enzyme, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.33
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin wild type enzyme, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.37
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme N704A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.38
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.41
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657F, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.42
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657T, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.42
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657T, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.43
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657V, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.44
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.45
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.48
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123K, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.49
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657V, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.51
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.52
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657S, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.55
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203D/E204D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.57
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203A/E204A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.65
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123M, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.67
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.67
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123M, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.69
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.73
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.74
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.75
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.78
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.81
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.84
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme Y656F, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.92
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.1
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123K, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.1
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme Y656F, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.3
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657F, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.3
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657G, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.3
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme N704A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.4
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203Q/E204Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.5
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203Q/E204Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.8
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
2
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657G, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
2.3
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q12884
-
-

Purification (Commentary)

Purification (Comment) Organism
anti-FLAG affinity chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin + H2O
-
 Homo sapiens acetyl-Gly-Pro-7-amino-4-trifluoromethylcoumarin
-
 ?
Gly-Pro-7-amido-4-trifluoromethylcoumarin + H2O
-
 Homo sapiens Gly-Pro + 7-amino-4-trifluoromethylcoumarin
-
 ?
Type I collagen + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
FAP
-
 Homo sapiens
fibroblast activation protein
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.03
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.05
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203A/E204A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.09
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.09
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657V, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.12
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme N704A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.13
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.15
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme Y656F, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.19
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.19
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.2
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657F, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.26
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.28
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.29
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657T, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.33
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.36
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.37
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.37
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme Y656F, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.4
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123K, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.45
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.46
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657S, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.47
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.48
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123M, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.6
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E204Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.71
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203D/E204D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.94
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657V, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.2
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123K, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.4
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme E203D/E204D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.7
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123A, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
1.8
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657G, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
2
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657Q, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
2.1
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme R123M, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
4.5
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657T, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
4.7
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657S, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
5.6
-
 Gly-Pro-7-amido-4-trifluoromethylcoumarin wild type enzyme, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
7.7
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin wild type enzyme, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
8.9
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657N, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
14
-
 acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin mutant enzyme A657D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0062
-
 Val-boro-Pro mutant enzyme A657D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.0062
-
 Val-boro-Pro wild type enzyme, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.014
-
 Ile-boro-Pro mutant enzyme A657D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.014
-
 Ile-boro-Pro wild type enzyme, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.023
-
 acetyl-Gly-boro-Pro mutant enzyme A657D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.023
-
 acetyl-Gly-boro-Pro wild type enzyme, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.034
-
 Val-Pro-CN mutant enzyme A657D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.034
-
 Val-Pro-CN wild type enzyme, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.84
-
 Ile-Pro-CN mutant enzyme A657D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
0.84
-
 Ile-Pro-CN wild type enzyme, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
6.8
-
 acetyl-Gly-Pro-CN mutant enzyme A657D, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens
6.8
-
 acetyl-Gly-Pro-CN wild type enzyme, at 23°C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA Homo sapiens