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

BRENDA support

Literature summary extracted from

  • Tran, T.; Quan, C.; Edosada, C.Y.; Mayeda, M.; Wiesmann, C.; Sutherlin, D.; Wolf, B.B.
    Synthesis and structure-activity relationship of N-acyl-Gly-, N-acyl-Sar- and N-blocked-boroPro inhibitors of FAP, DPP4, and POP (2007), Bioorg. Med. Chem. Lett., 17, 1438-1442.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.21.B28
-
 Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.14.5 N-[2-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-2-oxoethyl]-N-methyl-5-oxoprolinamide
-
 Homo sapiens
3.4.14.5 [(2R)-1-(4-oxo-4-phenylbutanoyl)pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-(N-acetyl-N-methylglycyl)pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)acetyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[(2-oxopyridin-1(2H)-yl)acetyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[N-(2,2-dimethylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[N-(cyclohexylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[N-(cyclopentylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[N-methyl-N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[N-methyl-N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.14.5 [(2R)-1-[N-[(2,5-dichlorophenyl)carbonyl]glycyl]pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.21.B28 L-Val-aminoacyl-proline boronic acid PT-100 Homo sapiens
3.4.21.B28 N-[2-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-2-oxoethyl]-9-N-methyl-5-oxoprolinamide
-
 Homo sapiens
3.4.21.B28 [(2R)-1-(4-oxo-4-phenylbutanoyl)pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-(N-acetyl-L-alanyl)pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-(N-acetyl-N-methylglycyl)pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[(2-oxopyridin-1(2H)-yl)acetyl]pyrrolidin-2-yl]-9-boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[N-(2,2-dimethylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl-9]-boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[N-(cyclohexylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[N-(cyclopentylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[N-methyl-N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[N-methyl-N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]-9-boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[N-[(2,5-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid
-
 Homo sapiens
3.4.21.B28 [(2R)-1-[N-[(2,6-dichlorophenyl)carbonyl]glycyl]-9-pyrrolidin-2-yl]boronic acid
-
 Homo sapiens

Organism

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

Purification (Commentary)

EC Number Purification (Comment) Organism
3.4.21.B28
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.B28 Gly-Pro-7-amido-4-trifluoromethylcoumarin + H2O
-
 Homo sapiens Gly-Pro + 7-amino-4-trifluoromethylcoumarin + H2O
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.14.5 DPP4
-
 Homo sapiens
3.4.21.B28 FAP
-
 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 0.000023
-
 [(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid in 50 mM Tris-HCl, 100 mM NaCl, pH 7.4, at 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens
3.4.21.B28 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 23°C Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.14.5 0.000068
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.000377
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid
3.4.14.5 0.00143
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.0043
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.0046
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[N-methyl-N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.006871
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-(N-acetyl-N-methylglycyl)pyrrolidin-2-yl]boronic acid
3.4.14.5 0.007391
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[N-(cyclohexylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.00908
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[N-(cyclopentylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.0095
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[N-[(2,5-dichlorophenyl)carbonyl]glycyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.0113
-
 23°C, pH 7.4 Homo sapiens N-[2-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-2-oxoethyl]-N-methyl-5-oxoprolinamide
3.4.14.5 0.0195
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[N-methyl-N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.0227
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)acetyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.0384
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.182
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[(2-oxopyridin-1(2H)-yl)acetyl]pyrrolidin-2-yl]boronic acid
3.4.14.5 0.451
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-(4-oxo-4-phenylbutanoyl)pyrrolidin-2-yl]boronic acid
3.4.14.5 0.608
-
 23°C, pH 7.4 Homo sapiens [(2R)-1-[N-(2,2-dimethylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid