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Literature summary for 3.4.21.B28 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
Search for more literature for 3.4.21.B28

Inhibitors

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

KM Value [mM]

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

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
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

Organism UniProt Comment Textmining
Homo sapiens Q12884
-
-

Reaction

Reaction Comment Organism Reaction ID
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

Source Tissue Comment Organism Textmining
blood plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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 ?
-
 ?
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 ?
-
 ?
benzyloxycarbonyl-Gly-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens benzyloxycarbonyl-Gly-Pro + 7-amino-4-methylcoumarin
-
 ?
Gly-Pro-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens Gly-Pro + 7-amino-4-methylcoumarin
-
 ?
MEPLGRQLTSGP-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens MEPLGRQLTSGP + 7-amino-4-methylcoumarin
-
 ?
MEPLGWQLTSGP-7-amido-4-methylcoumarin + H2O
-
 Homo sapiens MEPLGWQLTSGP + 7-amino-4-methylcoumarin
-
 ?
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

Synonyms Comment Organism
antiplasmin-cleaving enzyme
-
 Homo sapiens
APCE
-
 Homo sapiens
FAP
-
 Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
29.1
-
 Gly-Pro-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens
36.4
-
 benzyloxycarbonyl-Gly-Pro-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens
55.3
-
 MEPLGWQLTSGP-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens
70.2
-
 MEPLGRQLTSGP-7-amido-4-methylcoumarin pH 7.5, 22°C Homo sapiens

Ki Value [mM]

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

IC50 Value

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