Information on EC 3.4.21.B28 - fibroblast activation protein alpha subunit

Word Map on EC 3.4.21.B28
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The expected taxonomic range for this enzyme is: Tetrapoda

EC NUMBER
COMMENTARY hide
3.4.21.B28
preliminary BRENDA-supplied EC number
RECOMMENDED NAME
GeneOntology No.
fibroblast activation protein alpha subunit
-
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
fibroblast activation protein requires substrates with Pro at P1 and Gly or D-amino acids at P2. Met-alpha2-antiplasmin is cleaved N-terminally at Pro3-Leu4 and Pro12-Asn13 into Asn-alpha2-antiplasmin that is rapidly cross-linked to fibrin and protects it from digestion by plasmin
show the reaction diagram
fibroblast activation protein requires substrates with Pro at P1 and Gly or D-amino acids at P2. Met-alpha2-antiplasmin is cleaved N-terminally at Pro3-Leu4 and Pro12-Asn13 into Asn-alpha2-antiplasmin that is rapidly cross-linked to fibrin and protects it from digestion by plasmin.
show the reaction diagram
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REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
cleavage of C-N-linkage
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hydrolysis of peptide bond
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CAS REGISTRY NUMBER
COMMENTARY hide
352031-63-1
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GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
evolution
malfunction
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siRNA knockdown of FAP-alpha in a glioma cell line shows decreased invasion through brain extracellular matrix proteoglycan brevican and denatured collagen
metabolism
-
FAP-alpha is significantly increased in breast cancer patients with poor outcome and survival
physiological function
additional information
-
overexpression of FAP-alpha results in a reduction of phosphorylated focal adhesion kinase level in both MCF-7 cells and MDA-MB-231 cells cultured in normal media and serum-free media, while the growth of MDA-MB-231 cells and the adhesion and invasion ability of both MCF-7 cells and MDA-MB-231 cells are not dramatically influenced by FAP-alpha expression
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
7-methoxycoumarin-4-acetic acid-APGSKGDA-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-ASGPAGPA-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-DKGESGPA-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-DRGETGP-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-DRGETGPA-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-DSGETGP-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-DSGETGPA-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-EPGPPGPA-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-ERGETGPA-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-ERGETGPAG-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-ERGETGPAGG-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-ERGETGPSG-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
7-methoxycoumarin-4-acetic acid-VGPAGK-dinitrophenyl + H2O
?
show the reaction diagram
-
-
-
-
?
acetyl-D-Ala-Pro-7-amido-4-trifluoromethylcoumarin + H2O
acetyl-D-Ala-Pro + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
acetyl-Gly-Pro-7-amido-4-methylcoumarin + H2O
acetyl-Gly-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin + H2O
acetyl-Gly-Pro-7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
acetyl-Gly-Pro-9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate + H2O
acetyl-Gly-Pro + 9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate
show the reaction diagram
-
-
-
-
?
acetyl-Gly-Pro-Gly-Pro-9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate + H2O
acetyl-Gly-Pro-Gly-Pro + 9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate
show the reaction diagram
-
most efficient substrate, FAP shows a greater catalytic efficiency for acetyl-Gly-Pro-Gly-Pro-9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate than for acetyl-Gly-Pro-9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate and TSGP-9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate
-
-
?
Ala-Pro-4-trifluoromethylcoumarin-7-amide + H2O
Ala-Pro + 4-trifluoromethylcoumarin-7-amine
show the reaction diagram
Ala-Pro-4-trifluoromethylcoumarin-7-amide + H2O
Ala-Pro-4 + trifluoromethylcoumarin-7-amine
show the reaction diagram
-
-
-
?
Ala-Pro-7-amido-4-methylcoumarin + H2O
Ala-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Ala-Pro-7-amido-4-trifluoromethylcoumarin + H2O
Ala-Pro + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
Ala-Pro-7-amido-4-trifluoromethylcoumarin + H2O
Ala-Pro + 7-amino-4-trifluoromethylcoumarin + H2O
show the reaction diagram
-
-
-
-
?
Ala-Pro-Ala-Pro-9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate + H2O
Ala-Pro-Ala-Pro + 9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate
show the reaction diagram
-
-
-
-
?
Ala-Ser-Gly-Pro-Asn-Gln + H2O
Ala-Ser-Gly-Pro + Asn-Gln
show the reaction diagram
-
-
-
-
?
Ala-Ser-Gly-Pro-Ser-Ser + H2O
Ala-Ser-Gly-Pro + Ser-Ser
show the reaction diagram
-
-
-
-
?
alpha2-antiplasmin + H2O
?
show the reaction diagram
alpha2-antiplasmin + H2O
truncated alpha2-antiplasmin + Met
show the reaction diagram
-
-
cleaves Met from the N-terminus yielding Asn as the N-terminal amino acid
-
?
Arg-Lys(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-Gly-Pro-Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Arg + H2O
Arg-Lys(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-Gly-Pro + Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Arg
show the reaction diagram
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-
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-
?
Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-D-Ala-Pro-Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)-Arg + H2O
Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-D-Ala-Pro + Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)-Arg
show the reaction diagram
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-
-
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?
Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-D-Ser-Pro-Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)-Arg + H2O
Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-D-Ser-Pro + Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)-Arg
show the reaction diagram
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-
-
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?
Arg-Pro-7-amido-4-methylcoumarin + H2O
Arg-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
preferred substrate
-
-
?
B-type natriuretic peptide + H2O
?
show the reaction diagram
-
efficiently hydrolysed and mostly preferred substrate
-
-
?
benzyloxycarbonyl-Gly-L-Pro-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Gly-L-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
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-
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?
benzyloxycarbonyl-Gly-Pro-7-amido-4-methyl-3-carbamoylcoumarin + H2O
benzyloxycarbonyl-Gly-Pro + 7-amino-4-methyl-3-carbamoylcoumarin
show the reaction diagram
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-
-
-
?
benzyloxycarbonyl-Gly-Pro-7-amido-4-methylcoumarin + H2O
benzyloxycarbonyl-Gly-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
biotinyl-Gly-Pro-7-amido-4-methyl-3-carbamoylcoumarin + H2O
biotinyl-Gly-Pro + 7-amino-4-methyl-3-carbamoylcoumarin
show the reaction diagram
-
-
-
-
?
Boc-Ala-Gly-Pro-Arg-7-amido-4-methylcoumarin + H2O
Boc-Ala-Gly-Pro-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
D-Ala-Pro-7-amido-4-trifluoromethylcoumarin + H2O
D-Ala-Pro + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
denatured type I collagen + H2O
?
show the reaction diagram
-
-
-
-
?
GASGPAGPA + H2O
GASGP + AGPA
show the reaction diagram
-
-
-
-
?
Gelatin + H2O
?
show the reaction diagram
gelatine + H2O
?
show the reaction diagram
GEPGPPGPA + H2O
GEP + GPPGP + L-Ala
show the reaction diagram
-
-
-
-
?
GFSPFQRED + H2O
?
show the reaction diagram
-
low activity
-
-
?
Gln-Pro-7-amido-4-methylcoumarin + H2O
Gln-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Glu-Pro-7-amido-4-methylcoumarin + H2O
Glu-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
glucagon-like peptide-1 + H2O
?
show the reaction diagram
-
slow hydrolysis
-
-
?
glucose-dependent insulinotropic peptide + H2O
?
show the reaction diagram
-
slow hydrolysis
-
-
?
Gly-Pro-4-trifluoromethylcoumarin-7-amide + H2O
Gly-Pro + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
?
Gly-Pro-7-amido-4-methylcoumarin + H2O
Gly-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
Gly-Pro-7-amido-4-trifluoromethylcoumarin + H2O
Gly-Pro + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
Gly-Pro-7-amido-4-trifluoromethylcoumarin + H2O
Gly-Pro + 7-amino-4-trifluoromethylcoumarin + H2O
show the reaction diagram
-
-
-
-
?
GTAGPNQEQE + H2O
GTAGP + NQEQE
show the reaction diagram
-
-
-
-
?
GTSGPNQEQE + H2O
GTSGP + NQEQE
show the reaction diagram
-
-
-
-
?
Ile-Pro-7-amido-4-methylcoumarin + H2O
Ile-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
most preferred substrate
-
-
?
Ile-Pro-7-amido-4-trifluoromethylcoumarin + H2O
Ile-Pro + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
L-Ala-L-Pro-7-amido-4-methylcoumarin + H2O
L-Ala-L-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
L-Ala-Pro-7-amido-4-trifluoromethylcoumarin + H2O
L-Ala-Pro + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
L-Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-Gly-Pro-Asn-Gln-Gln-Gln-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Arg + H2O
?
show the reaction diagram
-
FRET-peptide
-
-
?
Leu-Pro-7-amido-4-methylcoumarin + H2O
Leu-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Lys-Ala-7-amido-4-trifluoromethylcoumarin + H2O
Lys-Ala + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
Lys-Pro-4-trifluoromethylcoumarin-7-amide + H2O
Lys-Pro + 4-trifluoromethylcoumarin-7-amine
show the reaction diagram
-
-
-
?
Lys-Pro-7-amido-4-methylcoumarin + H2O
Lys-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
MEPLGRQLTSGP-7-amido-4-methylcoumarin + H2O
MEPLGRQLTSGP + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
MEPLGWQLTSGP-7-amido-4-methylcoumarin + H2O
MEPLGWQLTSGP + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Met-alpha2-antiplasmin + H2O
?
show the reaction diagram
Met-Pro-7-amido-4-methylcoumarin + H2O
Met-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Leu-Phe-His + H2O
?
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-7-amido-4-methylcoumarin + H2O
N-benzyloxycarbonyl-Gly-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Ala + H2O
N-benzyloxycarbonyl-Gly-Pro + L-Ala
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Glu + H2O
N-benzyloxycarbonyl-Gly-Pro + L-Glu
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-His + H2O
N-benzyloxycarbonyl-Gly-Pro + L-His
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Leu + H2O
N-benzyloxycarbonyl-Gly-Pro + L-Leu
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Met + H2O
N-benzyloxycarbonyl-Gly-Pro + L-Met
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Met-His + H2O
N-benzyloxycarbonyl-Gly-Pro + Met-His
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Met-His-Arg-Ser + H2O
N-benzyloxycarbonyl-Gly-Pro + Met-His-Arg-Ser
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Phe + H2O
N-benzyloxycarbonyl-Gly-Pro + L-Phe
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Phe-His + H2O
N-benzyloxycarbonyl-Gly-Pro + L-Phe-L-His
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Phe-His-Arg + H2O
N-benzyloxycarbonyl-Gly-Pro + Phe-His-Arg
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Phe-His-Arg-Ser + H2O
N-benzyloxycarbonyl-Gly-Pro + Phe-His-Arg-Ser
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Ser + H2O
N-benzyloxycarbonyl-Gly-Pro + L-Ser
show the reaction diagram
-
-
-
-
?
N-benzyloxycarbonyl-Gly-Pro-Tyr + H2O
N-benzyloxycarbonyl-Gly-Pro + L-Tyr
show the reaction diagram
-
-
-
-
?
N-formyl-Gly-Pro-7-amido-4-methyl-3-carbamoylcoumarin + H2O
N-formyl-Gly-Pro + 7-amino-4-methyl-3-carbamoylcoumarin
show the reaction diagram
-
-
-
-
?
N-methyl-Gly-Pro-7-amido-4-methyl-3-carbamoylcoumarin + H2O
N-methyl-Gly-Pro + 7-amino-4-methyl-3-carbamoylcoumarin
show the reaction diagram
-
-
-
-
?
neuropeptide Y + H2O
?
show the reaction diagram
-
efficiently hydrolysed and mostly preferred substrate
-
-
?
peptide YY + H2O
?
show the reaction diagram
-
efficiently hydrolysed substrate
-
-
?
Phe-Pro-7-amido-4-methylcoumarin + H2O
Phe-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Phe-Pro-7-amido-4-trifluoromethylcoumarin + H2O
Phe-Pro + 7-amino-4-trifluoromethylcoumarin
show the reaction diagram
-
-
-
-
?
pre-digested collagen + H2O
?
show the reaction diagram
-
-
-
-
?
precursor Met-alpha2-antiplasmin + H2O
L-Asn-alpha2-antiplasmin + ?
show the reaction diagram
-
the enzyme cleaves between Pro12 and Asn13
-
-
?
Pro-Pro-7-amido-4-methylcoumarin + H2O
Pro-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
preferred substrate
-
-
?
RPKPQQFFGLM + H2O
RPKP + QQ + FFGLM
show the reaction diagram
-
the substance P-derived sequence is cleaved although it does not contain Gly-Pro
-
-
?
Ser-Pro-7-amido-4-methylcoumarin + H2O
Ser-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Substance P + H2O
?
show the reaction diagram
-
efficiently hydrolysed substrate
-
-
?
Thr-Ala-Gly-Pro-Asn-Gln + H2O
Thr-Ala-Gly-Pro + Asn-Gln
show the reaction diagram
-
-
-
-
?
Thr-Pro-7-amido-4-methylcoumarin + H2O
Thr-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Thr-Ser-Gly-Pro-Asn-Gln + H2O
Thr-Ser-Gly-Pro + Asn-Gln
show the reaction diagram
-
-
-
-
?
Thr-Ser-Gly-Pro-Asn-Ser + H2O
Thr-Ser-Gly-Pro + Asn-Ser
show the reaction diagram
-
-
-
-
?
Thr-Ser-Gly-Pro-Ser-Gln + H2O
Thr-Ser-Gly-Pro + Ser-Gln
show the reaction diagram
-
-
-
-
?
Tic-Pro-7-amido-4-trifluoromethylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
TSGP-9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate + H2O
TSGP + 9-di-3-sulfonylpropylaminobenzo[a]phenoxazonium perchlorate
show the reaction diagram
-
-
-
-
?
Type I collagen + H2O
?
show the reaction diagram
Tyr-Pro-7-amido-4-methylcoumarin + H2O
Tyr-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Val-Pro-7-amido-4-methylcoumarin + H2O
Val-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Z-Gly-L-Pro-7-amido-4-methylcoumarin + H2O
Z-Gly-L-Pro + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
alpha2-antiplasmin + H2O
?
show the reaction diagram
B-type natriuretic peptide + H2O
?
show the reaction diagram
-
efficiently hydrolysed and mostly preferred substrate
-
-
?
Gelatin + H2O
?
show the reaction diagram
gelatine + H2O
?
show the reaction diagram
glucagon-like peptide-1 + H2O
?
show the reaction diagram
-
slow hydrolysis
-
-
?
glucose-dependent insulinotropic peptide + H2O
?
show the reaction diagram
-
slow hydrolysis
-
-
?
Met-alpha2-antiplasmin + H2O
?
show the reaction diagram
-
APCE and rFAP cleave both Pro3-Leu4 and Pro12-Asn13 bonds of Met-alpha2-antiplasmin, but relative kcat /Km values for Pro12-Asn13 are about 16fold higher than for Pro3-Leu4. Conversion of Met-alpha2-antiplasmin by membrane or soluble FAP to the more easily fibrin-incorporable form, Asn-alpha2-antiplasmin, may increase plasmin inhibition within fibrin surrounding certain neoplasms and have an impact on growth and therapeutic susceptibility
-
-
?
neuropeptide Y + H2O
?
show the reaction diagram
-
efficiently hydrolysed and mostly preferred substrate
-
-
?
peptide YY + H2O
?
show the reaction diagram
-
efficiently hydrolysed substrate
-
-
?
pre-digested collagen + H2O
?
show the reaction diagram
-
-
-
-
?
Substance P + H2O
?
show the reaction diagram
-
efficiently hydrolysed substrate
-
-
?
Type I collagen + H2O
?
show the reaction diagram
-
-
-
?
additional information
?
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
1-benzyl-7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
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-
1-[(4-methoxyquinazolin-2-yl)methyl]-3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-7-(3-methylbut-2-en-1-yl)-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-7-(4-methylpent-3-en-1-yl)-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
2-mercaptoethanol
-
inhibition at 140 mM
3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
3-[[7-(but-2-yn-1-yl)-3-methyl-2,6-dioxo-8-(piperazin-1-yl)-2,3,6,7-tetrahydro-1H-purin-1-yl]methyl]benzonitrile
-
-
4'-[[7-(but-2-yn-1-yl)-3-methyl-2,6-dioxo-8-(piperazin-1-yl)-2,3,6,7-tetrahydro-1H-purin-1-yl]methyl]biphenyl-2-carbonitrile
-
-
4-(2-aminoethyl)-benzenesulfonyl fluoride hydrochloride
-
AEBSF, inhibition at 5 mM
4-(2-aminoethyl)-benzenesulfonylfluoride
4-amidino phenylsulfonyl fluoride
-
APSF, inhibition at 0.05 mM
4-amidino-phenylsulfonylfluoride
7-(but-2-yn-1-yl)-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-1-[[2-(hydroxymethyl)-1,3-thiazol-4-yl]methyl]-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-1-(naphthalen-2-ylmethyl)-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-8-(piperidin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-1-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-1-(pyridin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-1-(pyridin-3-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-1-(pyridin-4-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-(quinazolin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-(quinolin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-[4-(1H-1,2,4-triazol-1-yl)benzyl]-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-[4-(1H-pyrazol-1-yl)benzyl]-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-8-ethoxy-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-8-[(3S)-3-(hydroxymethyl)-5-oxopiperazin-1-yl]-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
-
7-(but-2-yn-1-yl)-8-[(8aS)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
-
7-benzyl-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
8-[(3R)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-methyl-1-(propan-2-yl)-3,7-dihydro-1H-purine-2,6-dione
-
-
acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-D-Ala-L-boroPro
-
selectively inhibits antiplasmin-cleaving enzyme vs. plasma dipeptidyl peptidase IV
acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-D-Asp-L-boroPro
-
-
acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-Gly-L-boroPro
-
-
acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-Ser-Gly-L-boroPro
-
-
acetyl-Arg-Gly-Gly-L-boroPro
-
-
acetyl-Arg-peg-D-Asp-L-boroPro
-
-
-
acetyl-Arg-peg-Gly-L-boroPro
-
-
-
acetyl-Arg-peg-Ser-Gly-L-boroPro
-
-
-
acetyl-Gly-boro-Pro
-
-
acetyl-Gly-L-boroPro
-
-
acetyl-Gly-Pro-boronic acid
-
-
acetyl-Gly-Pro-CN
-
-
Ala-ProP(OPh)2
-
-
alogliptin
-
-
chymostatin
-
50% inhibition at 0.16 mM
diisopropyl fluorophosphate
-
0.005 mM
diisopropylfluorophosphate
dimethyl sulfoxide
-
50% inhibition at 4%
dithiothreitol
-
inhibition at 10 mM
dutogliptin
-
-
FRQLTSG-pipecolinyl-NQEQV
-
-
Gly-ProP(OPh)2
-
-
HgCl2
Ile-boro-Pro
-
-
Ile-Pro-CN
-
-
L-Val-aminoacyl-proline boronic acid
-
PT-100
Leu-Pro-PO(OPh)2
-
-
linagliptin
-
-
N-ethylmaleimide
N-[(3R)-1-[7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]piperidin-3-yl]acetamide
-
-
N-[2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl]quinoline-4-carboxamide
-
-
N-[2-([7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]amino)ethyl]acetamide
-
-
N-[2-([7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]amino)ethyl]pyridine-4-carboxamide
-
-
N-[2-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-2-oxoethyl]-9-N-methyl-5-oxoprolinamide
-
-
N2-[7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]glycinamide
-
-
Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-(R)-fluoropyrrolidide
-
-
Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-(S)-fluoropyrrolidide
-
-
Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQEQV
-
-
Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-piperidide
-
-
Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-pyrrolidide
-
-
Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQEQV
-
-
Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQGQV
-
-
Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pyrrolidide
-
-
Phe-ProP(OPh)2
-
-
phenylmethylsulfonyl fluoride
Phenylmethylsulfonylfluoride
Pro-ProP(OPh)2
-
-
saxagliptin
-
-
Ser-ProP(OPh)2
-
-
sitagliptin
-
-
Talabostat
Tyr-ProP(OPh)2
-
-
Val-boro-Pro
-
-
Val-boroPro
-
-
Val-Pro-CN
-
-
Val-ProP(OPh)2
-
-
ValboroPro
-
complete inhibition at 0.05 mM
vildagliptin
-
-
[(2R)-1-(4-oxo-4-phenylbutanoyl)pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-(N-acetyl-L-alanyl)pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-(N-acetyl-N-methylglycyl)pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid
-
-
[(2R)-1-[(2-oxopyridin-1(2H)-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid
-
-
[(2R)-1-[N-(2,2-dimethylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
-
[(2R)-1-[N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl-9]-boronic acid
-
-
[(2R)-1-[N-(cyclohexylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
-
[(2R)-1-[N-(cyclopentylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
-
[(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
-
[(2R)-1-[N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
-
[(2R)-1-[N-methyl-N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
-
[(2R)-1-[N-methyl-N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
-
[(2R)-1-[N-[(2,5-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[N-[(2,6-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid
-
-
[(2S)-1-(D-valyl)pyrrolidin-2-yl]boronic acid
-
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
trans-epoxysuccinyl-L-leucylamido(4-guanidino)-butane
-
activation
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.051
7-methoxycoumarin-4-acetic acid-APGSKGDA-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.0361
7-methoxycoumarin-4-acetic acid-ASGPAGPA-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.046
7-methoxycoumarin-4-acetic acid-DKGESGPA-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.0238
7-methoxycoumarin-4-acetic acid-DRGETGP-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.021
7-methoxycoumarin-4-acetic acid-DRGETGPA-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.0396
7-methoxycoumarin-4-acetic acid-DSGETGP-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.0202
7-methoxycoumarin-4-acetic acid-DSGETGPA-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.0269
7-methoxycoumarin-4-acetic acid-EPGPPGPA-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.0567
7-methoxycoumarin-4-acetic acid-ERGETGPA-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.043
7-methoxycoumarin-4-acetic acid-ERGETGPAG-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.0371
7-methoxycoumarin-4-acetic acid-ERGETGPAGG-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.0513
7-methoxycoumarin-4-acetic acid-ERGETGPSG-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.052
7-methoxycoumarin-4-acetic acid-VGPAGK-dinitrophenyl
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.541
acetyl-D-Ala-Pro-7-amido-4-trifluoromethylcoumarin
-
23C
0.087 - 2.3
acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin
0.2 - 0.46
Ala-Pro-4-trifluoromethylcoumarin-7-amide
0.244 - 0.323
Ala-Pro-7-amido-4-trifluoromethylcoumarin
0.0022
Ala-Ser-Gly-Pro-Asn-Gln
-
23C
0.0043
Ala-Ser-Gly-Pro-Ser-Ser
-
23C
0.026 - 0.029
Arg-Lys(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-Gly-Pro-Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Arg
0.0008
Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-D-Ala-Pro-Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)-Arg
-
23C
0.0006
Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-D-Ser-Pro-Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)-Arg
-
23C
0.09 - 0.124
benzyloxycarbonyl-Gly-Pro-7-amido-4-methylcoumarin
0.213
D-Ala-Pro-7-amido-4-trifluoromethylcoumarin
-
23C
0.455 - 1
Gly-Pro-7-amido-4-methylcoumarin
0.062 - 1.8
Gly-Pro-7-amido-4-trifluoromethylcoumarin
0.106
Ile-Pro-7-amido-4-trifluoromethylcoumarin
-
at 23C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4
0.2 - 0.323
L-Ala-Pro-7-amido-4-trifluoromethylcoumarin
0.029
L-Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-Gly-Pro-Asn-Gln-Gln-Gln-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Arg
-
recombinant enzyme
0.189
Lys-Ala-7-amido-4-trifluoromethylcoumarin
-
at 23C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4
0.9
Lys-Pro-4-trifluoromethylcoumarin-7-amide
-
pH 7.8, 37C
0.021
MEPLGRQLTSGP-7-amido-4-methylcoumarin
-
pH 7.5, 22C
0.07
MEPLGWQLTSGP-7-amido-4-methylcoumarin
-
pH 7.5, 22C
0.245
Phe-Pro-7-amido-4-trifluoromethylcoumarin
-
at 23C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4
0.0007
Thr-Ala-Gly-Pro-Asn-Gln
-
23C
0.0013
Thr-Ser-Gly-Pro-Asn-Gln
-
23C
0.0022
Thr-Ser-Gly-Pro-Asn-Ser
-
23C
0.0019
Thr-Ser-Gly-Pro-Ser-Gln
-
23C
0.053
Tic-Pro-7-amido-4-trifluoromethylcoumarin
-
in 25 mM sodium phosphate buffer, pH 7.5, containing 1.0 mM EDTA and 2% (v/v) methanol, at 22C
0.27
Z-Gly-Pro-4-methylcoumarin-7-amide
-
-
TURNOVER NUMBER [1/s]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.015
7-methoxycoumarin-4-acetic acid-APGSKGDA-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.196
7-methoxycoumarin-4-acetic acid-ASGPAGPA-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.067
7-methoxycoumarin-4-acetic acid-DKGESGPA-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.003
7-methoxycoumarin-4-acetic acid-DRGETGP-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.081
7-methoxycoumarin-4-acetic acid-DRGETGPA-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.003
7-methoxycoumarin-4-acetic acid-DSGETGP-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.059
7-methoxycoumarin-4-acetic acid-DSGETGPA-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.115
7-methoxycoumarin-4-acetic acid-EPGPPGPA-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.141
7-methoxycoumarin-4-acetic acid-ERGETGPA-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.121
7-methoxycoumarin-4-acetic acid-ERGETGPAG-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.079
7-methoxycoumarin-4-acetic acid-ERGETGPAGG-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.268
7-methoxycoumarin-4-acetic acid-ERGETGPSG-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.095
7-methoxycoumarin-4-acetic acid-VGPAGK-dinitrophenyl
Homo sapiens
-
in 100 mM NaCl, 100 mM Tris, pH 7.8, at 37C
0.3
acetyl-D-Ala-Pro-7-amido-4-trifluoromethylcoumarin
Homo sapiens
-
23C
0.05 - 14
acetyl-Gly-Pro-7-amido-4-trifluoromethylcoumarin
2
Ala-Pro-4-trifluoromethylcoumarin-7-amide
Homo sapiens
-
pH 8.5
0.995 - 14.2
Ala-Pro-7-amido-4-trifluoromethylcoumarin
2.7
Ala-Ser-Gly-Pro-Asn-Gln
Homo sapiens
-
23C
5.5
Ala-Ser-Gly-Pro-Ser-Ser
Homo sapiens
-
23C
1.06 - 1.2
Arg-Lys(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-Gly-Pro-Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Arg
0.19
Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-D-Ala-Pro-Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)-Arg
Homo sapiens
-
23C
0.22
Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-D-Ser-Pro-Asn-Gln-Glu-Gln-Glu(5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid)-Arg
Homo sapiens
-
23C
0.51 - 36.4
benzyloxycarbonyl-Gly-Pro-7-amido-4-methylcoumarin
1.5
D-Ala-Pro-7-amido-4-trifluoromethylcoumarin
Homo sapiens
-
23C
29.1
Gly-Pro-7-amido-4-methylcoumarin
Homo sapiens
-
pH 7.5, 22C
0.03 - 5.6
Gly-Pro-7-amido-4-trifluoromethylcoumarin
6.9
Ile-Pro-7-amido-4-trifluoromethylcoumarin
Homo sapiens
-
at 23C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4
1.08
L-Ala-Pro-7-amido-4-trifluoromethylcoumarin
Homo sapiens
-
recombinant enzyme
1.2
L-Arg-Lys-(4-(4-dimethylaminophenylazo)benzoyl)-Thr-Ser-Gly-Pro-Asn-Gln-Gln-Gln-Glu(5-[(2-aminoethyl)amino]-naphthalene-1-sulfonic acid)-Arg
Homo sapiens
-
recombinant enzyme
0.01
Lys-Ala-7-amido-4-trifluoromethylcoumarin
Homo sapiens
-
at 23C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4
70.2
MEPLGRQLTSGP-7-amido-4-methylcoumarin
Homo sapiens
-
pH 7.5, 22C
55.3
MEPLGWQLTSGP-7-amido-4-methylcoumarin
Homo sapiens
-
pH 7.5, 22C
1.1
Phe-Pro-7-amido-4-trifluoromethylcoumarin
Homo sapiens
-
at 23C in 50 mM Tris-HCl, 100 mM NaCl, 1 mM EDTA, pH 7.4
1.5
Thr-Ala-Gly-Pro-Asn-Gln
Homo sapiens
-
23C
1.6
Thr-Ser-Gly-Pro-Asn-Gln
Homo sapiens
-
23C
3.1
Thr-Ser-Gly-Pro-Asn-Ser
Homo sapiens
-
23C
2
Thr-Ser-Gly-Pro-Ser-Gln
Homo sapiens
-
23C
1.19
Tic-Pro-7-amido-4-trifluoromethylcoumarin
Homo sapiens
-
in 25 mM sodium phosphate buffer, pH 7.5, containing 1.0 mM EDTA and 2% (v/v) methanol, at 22C
kcat/KM VALUE [1/mMs-1]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
22
Tic-Pro-7-amido-4-trifluoromethylcoumarin
Homo sapiens
-
in 25 mM sodium phosphate buffer, pH 7.5, containing 1.0 mM EDTA and 2% (v/v) methanol, at 22C
41938
Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0000057
acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-D-Ala-L-boroPro
-
in 25 mM sodium phosphate buffer, pH 7.5, containing 1.0 mM EDTA and 2% (v/v) methanol, at 22C
0.001377
acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-D-Asp-L-boroPro
-
in 25 mM sodium phosphate buffer, pH 7.5, containing 1.0 mM EDTA and 2% (v/v) methanol, at 22C
0.0000018
acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-Gly-L-boroPro
-
in 25 mM sodium phosphate buffer, pH 7.5, containing 1.0 mM EDTA and 2% (v/v) methanol, at 22C
0.0000027
acetyl-Arg-(8-amino-3,6-dioxaoctanoic acid)-Ser-Gly-L-boroPro
-
in 25 mM sodium phosphate buffer, pH 7.5, containing 1.0 mM EDTA and 2% (v/v) methanol, at 22C
0.0000172
acetyl-Arg-Gly-Gly-L-boroPro
-
in 25 mM sodium phosphate buffer, pH 7.5, containing 1.0 mM EDTA and 2% (v/v) methanol, at 22C
0.023
acetyl-Gly-boro-Pro
-
mutant enzyme A657D, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA; wild type enzyme, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA
0.0000207
acetyl-Gly-L-boroPro
-
in 25 mM sodium phosphate buffer, pH 7.5, containing 1.0 mM EDTA and 2% (v/v) methanol, at 22C
0.000023
acetyl-Gly-Pro-boronic acid
-
-
6.8
acetyl-Gly-Pro-CN
-
mutant enzyme A657D, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA; wild type enzyme, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA
0.014
FRQLTSG-pipecolinyl-NQEQV
-
pH 7.5, 22C
0.00327
Gly-ProP(OPh)2
-
in 25 mM Tris, containing 140 mM NaCl and 10 mM KCl, pH 7.9
0.014
Ile-boro-Pro
-
mutant enzyme A657D, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA; wild type enzyme, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA
0.84
Ile-Pro-CN
-
mutant enzyme A657D, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA; wild type enzyme, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA
0.006
Leu-Pro-PO(OPh)2
-
in 25 mM Tris, containing 140 mM NaCl and 10 mM KCl, pH 7.9
0.000146
N-[2-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-2-oxoethyl]-9-N-methyl-5-oxoprolinamide
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.0553
Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-(R)-fluoropyrrolidide
-
pH 7.5, 22C
0.0538
Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-(S)-fluoropyrrolidide
-
pH 7.5, 22C
0.015
Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQEQV
-
pH 7.5, 22C
0.264
Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-piperidide
-
pH 7.5, 22C
0.068
Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-pyrrolidide
-
pH 7.5, 22C
0.057
Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQEQV
-
pH 7.5, 22C
0.0145
Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQGQV
-
pH 7.5, 22C
0.703
Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pyrrolidide
-
pH 7.5, 22C
0.0046
Pro-ProP(OPh)2
-
in 25 mM Tris, containing 140 mM NaCl and 10 mM KCl, pH 7.9
0.00216
Ser-ProP(OPh)2
-
in 25 mM Tris, containing 140 mM NaCl and 10 mM KCl, pH 7.9
0.00259
Tyr-ProP(OPh)2
-
in 25 mM Tris, containing 140 mM NaCl and 10 mM KCl, pH 7.9
0.0062
Val-boro-Pro
-
mutant enzyme A657D, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA; wild type enzyme, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA
0.034
Val-Pro-CN
-
mutant enzyme A657D, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA; wild type enzyme, at 23C in 50 mM Tris (pH 7.4), 100 mM NaCl, and 1 mM EDTA
0.00363
Val-ProP(OPh)2
-
in 25 mM Tris, containing 140 mM NaCl and 10 mM KCl, pH 7.9
0.000094
[(2R)-1-(4-oxo-4-phenylbutanoyl)pyrrolidin-2-yl]boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.00035
[(2R)-1-(N-acetyl-L-alanyl)pyrrolidin-2-yl]boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000161
[(2R)-1-(N-acetyl-N-methylglycyl)pyrrolidin-2-yl]boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000023
[(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.0000075
[(2R)-1-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.0029
[(2R)-1-[(2-oxopyridin-1(2H)-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000751
[(2R)-1-[N-(2,2-dimethylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000051
[(2R)-1-[N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000014
[(2R)-1-[N-(cyclohexylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.00002
[(2R)-1-[N-(cyclopentylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000246
[(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000142
[(2R)-1-[N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000265
[(2R)-1-[N-methyl-N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000191
[(2R)-1-[N-methyl-N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000029
[(2R)-1-[N-[(2,5-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
0.000012
[(2R)-1-[N-[(2,6-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid
-
in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23C
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.1
1-benzyl-7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.1
1-[(4-methoxyquinazolin-2-yl)methyl]-3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.05
1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-7-(4-methylpent-3-en-1-yl)-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.1
3,7-dimethyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.1
3-[[7-(but-2-yn-1-yl)-3-methyl-2,6-dioxo-8-(piperazin-1-yl)-2,3,6,7-tetrahydro-1H-purin-1-yl]methyl]benzonitrile
Homo sapiens
-
above, pH and temperature not specified in the publication
0.1
4'-[[7-(but-2-yn-1-yl)-3-methyl-2,6-dioxo-8-(piperazin-1-yl)-2,3,6,7-tetrahydro-1H-purin-1-yl]methyl]biphenyl-2-carbonitrile
Homo sapiens
-
above, pH and temperature not specified in the publication
0.0058
7-(but-2-yn-1-yl)-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.0012
7-(but-2-yn-1-yl)-1-[(4-methoxyquinazolin-2-yl)methyl]-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.1
7-(but-2-yn-1-yl)-1-[[2-(hydroxymethyl)-1,3-thiazol-4-yl]methyl]-3-methyl-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.041
7-(but-2-yn-1-yl)-3-methyl-1-(naphthalen-2-ylmethyl)-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.0019
7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.00074
7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.01
7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-8-(piperidin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.1
7-(but-2-yn-1-yl)-3-methyl-1-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]-8-(piperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.0125
7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-1-(pyridin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.1
7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-1-(pyridin-3-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.1
7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-1-(pyridin-4-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.1
7-(but-2-yn-1-yl)-3-methyl-8-(3-oxopiperazin-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.0018
7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-(quinazolin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.0103
7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-(quinolin-2-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.1
7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-[4-(1H-1,2,4-triazol-1-yl)benzyl]-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.05
7-(but-2-yn-1-yl)-3-methyl-8-(piperazin-1-yl)-1-[4-(1H-pyrazol-1-yl)benzyl]-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.1
7-(but-2-yn-1-yl)-8-ethoxy-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.0033
7-(but-2-yn-1-yl)-8-[(3S)-3-(hydroxymethyl)-5-oxopiperazin-1-yl]-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.011
7-(but-2-yn-1-yl)-8-[(8aS)-hexahydropyrrolo[1,2-a]pyrazin-2(1H)-yl]-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
pH and temperature not specified in the publication
0.1
8-[(3R)-3-aminopiperidin-1-yl]-7-(but-2-yn-1-yl)-3-methyl-1-(propan-2-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
above, pH and temperature not specified in the publication
0.1
alogliptin
Homo sapiens
-
above, pH and temperature not specified in the publication
0.00752
dutogliptin
Homo sapiens
-
pH and temperature not specified in the publication
0.000089 - 0.00037
linagliptin
Homo sapiens
-
pH and temperature not specified in the publication
0.01
N-[(3R)-1-[7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]piperidin-3-yl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000033
N-[2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl]quinoline-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01
N-[2-([7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]amino)ethyl]acetamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01
N-[2-([7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]amino)ethyl]pyridine-4-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.1
N2-[7-(but-2-yn-1-yl)-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl]glycinamide
Homo sapiens
-
above, pH and temperature not specified in the publication
0.091
Phe-Arg-(8-amino-3,6-dioxaoctanoic acid)-Gly-[R]-fluoropyrrolidide
Homo sapiens
-
cleavage of Met-alpha2-antiplasmin
-
0.0026
saxagliptin
Homo sapiens
-
pH and temperature not specified in the publication
0.1
sitagliptin
Homo sapiens
-
above, pH and temperature not specified in the publication
0.00004
Talabostat
Homo sapiens
-
-
0.073
vildagliptin
Homo sapiens
-
pH and temperature not specified in the publication
0.00007
[(2S)-1-(D-valyl)pyrrolidin-2-yl]boronic acid
Homo sapiens
-
pH and temperature not specified in the publication
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7
-
wild type enzyme
8.5 - 9
-
-
8.5
-
recombinant enzyme
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
pI VALUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
5
-
isoelectric focusing
5.68
-
isoelectric focusing
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
-
-
Manually annotated by BRENDA team
-
malignant mesenchymal cells
Manually annotated by BRENDA team
-
lowenzyme activity
Manually annotated by BRENDA team
-
cancer stroma cells
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
higher levels in cancer tissue than normal tissue
Manually annotated by BRENDA team
-
mainly located, seprase-expressing carcinoma tissue more often found in the scirrhous type than in other types of gastric carcinoma
Manually annotated by BRENDA team
-
; glioma stem-like cell, isolated from a solid glioblastoma in a long term culture, low expression
Manually annotated by BRENDA team
-
lowenzyme activity
Manually annotated by BRENDA team
-
expression in idiopathic pulmonary fibrosis, not expressed in normal lung tissue or tissue with evidence of centriacinar emphysema
Manually annotated by BRENDA team
-
transiently expressed in certain normal fetal mesenchymal tissues
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
high enzyme activity
Manually annotated by BRENDA team
-
lowenzyme activity
Manually annotated by BRENDA team
-
the induced seprase expression of ovarian tumor cells influences their collagen contraction and invasion capability. Tumor cells with reduced seprase expression, due to manipulation by RNA interference, show a reduction of type I collagen gel contraction
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
expressed in both premalignant and malignant forms of squamous cell carcinoma, but are lacking in normal esophageal epithelia, suggesting that the enzyme is involved in squamous cell carcinoma neoplastic progression
Manually annotated by BRENDA team
-
high enzyme activity
Manually annotated by BRENDA team
-
lowenzyme activity
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
-
high enzyme activity
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
87720
-
subunit, calculated from amino acid sequence
90000
-
theoretical value of FAPalpha-His6tag
93000
-
2 * 93000, recombinant FAP, SDS-PAGE
96000
-
-
100000
-
2 * 100000, multiangle light scattering in combination with gel filtration chromatography and interferometric refractometry
105000
-
1 * 95000 + 1 * 105000, SDS-PAGE
153000
-
recombinant FAP, gel filtration
160000 - 170000
-
-
160000
-
-
170000
175000
-
native APCE, gel filtration
200000
-
multiangle light scattering in combination with gel filtration chromatography and interferometric refractometry
215000
-
SDS-PAGE under nonreducing conditions
400000
SUBUNITS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
homodimer
monomer
-
Western immunoblotting
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
glycoprotein
Crystallization/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
at 4C, by Syrrxs automated Nanovolume crystallization technology, Ala657 reduces the acidity in this pocket, which may explain the lower affinity for N-terminal amines
-
Purification/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
ammonium sulfate precipitation, hydrophobic interaction column chromatography, and immunoaffinity column chromatography
-
anti-FLAG affinity chromatography
-
by column chromatographies, 30197fold to homogeneity
-
glycosylated form, near homogeneity
-
M2-anti-FLAG resin column chromatography
-
Ni-NTA resin column chromatography
-
partial purification by Sephacryl S-200 gel filtration
-
S-200 gel filtration, hydroxylapatite column chromatography, Cibacron blue chromatography, and WGA-agarose column chromatography
standard protocol
-
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
97000 Da subunit
-
expressed in 293 cells
-
expressed in HEK-293 cells
expressed in Schneider S2 cells
-
expressed in WI38 cells
-
FAP is expressed in Pichia pastoris
-
into a modified pFastBacHTb vector
-
quantitative real-time PCR enzyme expression analysis
-
recombinant expression in Escherichia coli TOP10 cells and transfection of SKOV-3 and HO-8910 cells, two poorly differentiated ovarian serous adenocarcinoma cell lines, using a lentivirus expression vector, quantitative real-time PCR enyzme expression analzsis
-
subcloned into tetracyline-inducible vectors
-
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
FAP-alpha is considerably induced upon differentiation with 10% fetal calf serum, FAP-alpha is elevated in glioblastomas and increases upon tumor stem cell differentiation
-
ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
A657F
-
decreased activity
A657G
-
decreased activity
A657N
-
increased activity
A657Q
-
decreased activity
A657S
-
decreased activity
A657T
-
decreased activity
A657V
-
decreased activity
E203A
-
diminished activity
E203A/E204A
-
diminished activity
E203D
-
diminished activity
E203D/E204D
-
diminished activity
E203Q
-
diminished activity
E203Q/E204Q
-
diminished activity
E204A
-
diminished activity
E204D
-
diminished activity
E204Q
-
diminished activity
N704A
-
diminished activity
R123A
-
diminished activity
R123K
-
diminished activity
R123M
-
diminished activity
S624A
-
inactive mutant
Y656F
-
diminished activity
additional information
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
medicine