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Literature summary for 3.4.16.4 extracted from

  • Inglis, S.R.; Zervosen, A.; Woon, E.C.; Gerards, T.; Teller, N.; Fischer, D.S.; Luxen, A.; Schofield, C.J.
    Synthesis and evaluation of 3-(dihydroxyboryl)benzoic acids as D,D-carboxypeptidase R39 inhibitors (2009), J. Med. Chem., 52, 6097-6106.
    View publication on PubMed
Search for more literature for 3.4.16.4

Inhibitors

Inhibitors Comment Organism Structure
(2-phenylethyl)boronic acid 91% residual activity at 1 mM Actinomadura sp. R39
(3-aminophenyl)boronic acid 20% residual activity at 1 mM Actinomadura sp. R39
(3-nitrophenyl)boronic acid 82% residual activity at 1 mM Actinomadura sp. R39
(4-phenoxyphenyl)boronic acid 98% residual activity at 1 mM Actinomadura sp. R39
(5-acetylthiophen-2-yl)boronic acid 88% residual activity at 1 mM Actinomadura sp. R39
(5-chlorothiophen-2-yl)boronic acid 91% residual activity at 1 mM Actinomadura sp. R39
(5-cyanothiophen-2-yl)boronic acid 95% residual activity at 1 mM Actinomadura sp. R39
(5-formylthiophen-2-yl)boronic acid 99% residual activity at 1 mM Actinomadura sp. R39
1-benzothiophen-2-ylboronic acid 86% residual activity at 1 mM Actinomadura sp. R39
2,1-benzoxaborol-1(3H)-ol 45% residual activity at 1 mM Actinomadura sp. R39
3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid 38% residual activity at 0.5 mM Actinomadura sp. R39
3-(acetylamino)-5-(dihydroxyboranyl)benzoic acid 50% residual activity at 1 mM Actinomadura sp. R39
3-(benzoylamino)-5-(dihydroxyboranyl)benzoic acid 9% residual activity at 1 mM Actinomadura sp. R39
3-(dihydroxyboranyl)-4-[(phenylacetyl)amino]benzoic acid 80% residual activity at 1 mM Actinomadura sp. R39
3-(dihydroxyboranyl)-5-[(2,6-dimethoxybenzoyl)amino]benzoic acid 84% residual activity at 1 mM Actinomadura sp. R39
3-(dihydroxyboranyl)-5-[(phenoxyacetyl)amino]benzoic acid 2% residual activity at 1 mM Actinomadura sp. R39
3-(dihydroxyboranyl)-5-[(thiophen-2-ylacetyl)amino]benzoic acid 5% residual activity at 1 mM Actinomadura sp. R39
3-(dihydroxyboranyl)-5-[(thiophen-2-ylcarbonyl)amino]benzoic acid 18% residual activity at 1 mM Actinomadura sp. R39
3-(dihydroxyboryl)-5-(2-methoxybenzamido)benzoic acid 10% residual acvtivity at 1 mM Actinomadura sp. R39
3-(dihydroxyboryl)-5-(2-phenylacetamido)benzoic acid 3% residual acvtivity at 1 mM Actinomadura sp. R39
3-(dihydroxyboryl)benzoic acid 20% residual acvtivity at 1 mM Actinomadura sp. R39
3-(trifluoroacetyl)benzoic acid 60% residual activity at 1 mM Actinomadura sp. R39
3-formylbenzoic acid 77% residual activity at 1 mM Actinomadura sp. R39
4-(dihydroxyboranyl)benzoic acid 85% residual activity at 1 mM Actinomadura sp. R39
4-[(phenylacetyl)amino]-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoic acid 81% residual activity at 1 mM Actinomadura sp. R39
5-(dihydroxyboranyl)thiophene-2-carboxylic acid 57% residual activity at 1 mM Actinomadura sp. R39
biphenyl-4,4'-diyldiboronic acid 97% residual activity at 0.1 mM Actinomadura sp. R39
additional information not inhibited by methyl 3-(dihydroxyboryl)-5-(2-phenylacetamido)benzoate Actinomadura sp. R39
phenylboronic acid 50% residual activity at 0.5 mM Actinomadura sp. R39
thiophen-2-ylboronic acid 88% residual activity at 1 mM Actinomadura sp. R39
[3-([[5-(dimethylamino)naphthalen-1-yl]sulfonyl]amino)phenyl]boronic acid 60% residual activity at 0.5 mM Actinomadura sp. R39
[3-[(2,6-dimethoxybenzoyl)amino]-5-(methoxycarbonyl)thiophen-2-yl]boronic acid 98% residual activity at 1 mM Actinomadura sp. R39

Organism

Organism UniProt Comment Textmining
Actinomadura sp. R39 P39045
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Actinomadura sp. R39

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
(R)-[2-(benzoylamino)propionylsulfanyl]acetic acid + H2O
-
 Actinomadura sp. R39 ?
-
 ?

Synonyms

Synonyms Comment Organism
D,D-carboxypeptidase R39
-
 Actinomadura sp. R39
PBP
-
 Actinomadura sp. R39
penicillin binding proteins
-
 Actinomadura sp. R39
R39 PBP
-
 Actinomadura sp. R39

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.023
-
 in 10 mM sodium phosphate buffer (pH 7.2) with 100 mM NaCl, 100 mM D-alanine, and 0.01 mg/ml bovine serum albumin for 60 min at 25°C Actinomadura sp. R39 3-(dihydroxyboryl)-5-(2-methoxybenzamido)benzoic acid
0.028
-
 in 10 mM sodium phosphate buffer (pH 7.2) with 100 mM NaCl, 100 mM D-alanine, and 0.01 mg/ml bovine serum albumin for 60 min at 25°C Actinomadura sp. R39 3-(dihydroxyboranyl)-5-[(phenoxyacetyl)amino]benzoic acid
0.032
-
 in 10 mM sodium phosphate buffer (pH 7.2) with 100 mM NaCl, 100 mM D-alanine, and 0.01 mg/ml bovine serum albumin for 60 min at 25°C Actinomadura sp. R39 3-(dihydroxyboranyl)-5-[(thiophen-2-ylcarbonyl)amino]benzoic acid
0.034
-
 in 10 mM sodium phosphate buffer (pH 7.2) with 100 mM NaCl, 100 mM D-alanine, and 0.01 mg/ml bovine serum albumin for 60 min at 25°C Actinomadura sp. R39 3-(benzoylamino)-5-(dihydroxyboranyl)benzoic acid
0.078
-
 in 10 mM sodium phosphate buffer (pH 7.2) with 100 mM NaCl, 100 mM D-alanine, and 0.01 mg/ml bovine serum albumin for 60 min at 25°C Actinomadura sp. R39 3-(dihydroxyboranyl)-5-[(thiophen-2-ylacetyl)amino]benzoic acid
0.088
-
 in 10 mM sodium phosphate buffer (pH 7.2) with 100 mM NaCl, 100 mM D-alanine, and 0.01 mg/ml bovine serum albumin for 60 min at 25°C Actinomadura sp. R39 3-(dihydroxyboryl)-5-(2-phenylacetamido)benzoic acid
0.4
-
 in 10 mM sodium phosphate buffer (pH 7.2) with 100 mM NaCl, 100 mM D-alanine, and 0.01 mg/ml bovine serum albumin for 60 min at 25°C Actinomadura sp. R39 3-(dihydroxyboryl)benzoic acid
0.5
-
 in 10 mM sodium phosphate buffer (pH 7.2) with 100 mM NaCl, 100 mM D-alanine, and 0.01 mg/ml bovine serum albumin for 60 min at 25°C Actinomadura sp. R39 phenylboronic acid
1
-
 in 10 mM sodium phosphate buffer (pH 7.2) with 100 mM NaCl, 100 mM D-alanine, and 0.01 mg/ml bovine serum albumin for 60 min at 25°C Actinomadura sp. R39 3-(acetylamino)-5-(dihydroxyboranyl)benzoic acid