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

BRENDA support

Literature summary extracted from

  • Lee, K.N.; Jackson, K.W.; Terzyan, S.; Christiansen, V.J.; McKee,P.A.
    Using substrate specificity of antiplasmin-cleaving enzyme for fibroblast activation protein inhibitor design (2009), Biochemistry, 48, 5149-5158.
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.B28 FRQLTSG-pipecolinyl-NQEQV
-
 Homo sapiens
3.4.21.B28 Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-(R)-fluoropyrrolidide
-
 Homo sapiens
3.4.21.B28 Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-(S)-fluoropyrrolidide
-
 Homo sapiens
3.4.21.B28 Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQEQV
-
 Homo sapiens
3.4.21.B28 Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-piperidide
-
 Homo sapiens
3.4.21.B28 Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-pyrrolidide
-
 Homo sapiens
3.4.21.B28 Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQEQV
-
 Homo sapiens
3.4.21.B28 Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQGQV
-
 Homo sapiens
3.4.21.B28 Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pyrrolidide
-
 Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.B28 0.021
-
 MEPLGRQLTSGP-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.07
-
 MEPLGWQLTSGP-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.09
-
 benzyloxycarbonyl-Gly-Pro-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.455
-
 Gly-Pro-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.4.21.B28 alpha2-antiplasmin + H2O Homo sapiens alpha2-antiplasmin is cleaved N-terminally to Asn-alpha2-antiplasmin that is rapidly cross-linked to fibrin and protects it from digestion by plasmin ?
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.B28 Homo sapiens Q12884
-
-

Reaction

EC Number Reaction Comment Organism Reaction ID
3.4.21.B28 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 Arg is optimal at position P7. Peptide cleavage rate increases with Arg in position P6 Homo sapiens
a

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.B28 blood plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.B28 alpha2-antiplasmin + H2O alpha2-antiplasmin is cleaved N-terminally to Asn-alpha2-antiplasmin that is rapidly cross-linked to fibrin and protects it from digestion by plasmin Homo sapiens ?
-
 ?
3.4.21.B28 alpha2-antiplasmin + H2O alpha2-antiplasmin is cleaved N-terminally at Pro12-Asn13 to Asn-alpha2-antiplasmin that is rapidly cross-linked to fibrin and protects it from digestion by plasmin Homo sapiens ?
-
 ?
3.4.21.B28 benzyloxycarbonyl-Gly-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-Gly-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 MEPLGRQLTSGP-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens MEPLGRQLTSGP + 7-amino-4-methylcoumarin
-
 ?
3.4.21.B28 MEPLGWQLTSGP-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens MEPLGWQLTSGP + 7-amino-4-methylcoumarin
-
 ?
3.4.21.B28 additional information FAP cleavage of peptide libraries of short amino acid sequences surrounding the scissile bond (-Pro12-Asn13-) indicates that Gly is required at position P2 and Pro is required at position P1. Arg is optimal at position P7. Peptide cleavage rate increases with Arg in position P6. Placing Arg in P4 or P8 reduces cleavage rates dramatically Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.B28 antiplasmin-cleaving enzyme
-
 Homo sapiens
3.4.21.B28 APCE
-
 Homo sapiens
3.4.21.B28 FAP
-
 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 29.1
-
 Gly-Pro-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens
3.4.21.B28 36.4
-
 benzyloxycarbonyl-Gly-Pro-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens
3.4.21.B28 55.3
-
 MEPLGWQLTSGP-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens
3.4.21.B28 70.2
-
 MEPLGRQLTSGP-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.B28 0.014
-
 FRQLTSG-pipecolinyl-NQEQV pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.0145
-
 Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQGQV pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.015
-
 Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQEQV pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.0538
-
 Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-(S)-fluoropyrrolidide pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.0553
-
 Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-(R)-fluoropyrrolidide pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.057
-
 Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pipecolinyl-NQEQV pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.068
-
 Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-pyrrolidide pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.264
-
 Phe-Arg-8-amino-3,6-dioxaoctanoyl-Gly-piperidide pH 7.5, 22°C Homo sapiens
3.4.21.B28 0.703
-
 Phe-Gly-8-amino-3,6-dioxaoctanoyl-Gly-pyrrolidide pH 7.5, 22°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.B28 0.091
-
 cleavage of Met-alpha2-antiplasmin Homo sapiens Phe-Arg-(8-amino-3,6-dioxaoctanoic acid)-Gly-[R]-fluoropyrrolidide