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Literature summary extracted from

  • Soares da Costa, T.P.; Tieu, W.; Yap, M.Y.; Pendini, N.R.; Polyak, S.W.; Sejer Pedersen, D.; Morona, R.; Turnidge, J.D.; Wallace, J.C.; Wilce, M.C.; Booker, G.W.; Abell, A.D.
    Selective inhibition of biotin protein ligase from Staphylococcus aureus (2012), J. Biol. Chem., 287, 17823-17832.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

EC Number Cloned (Comment) Organism
6.3.4.15
-
 Staphylococcus aureus

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
6.3.4.15 hanging drop vapor diffusion method, using 8-12% (w/v) PEG8000 in 0.1 M Tris pH 7.5 or 8.0 and 10% (v/v) glycerol Staphylococcus aureus

Protein Variants

EC Number Protein Variants Comment Organism
6.3.4.15 R125A the mutant shows severely reduced catalytic efficiency compared to the wild type enzyme Staphylococcus aureus
6.3.4.15 R125N the mutant shows severely reduced catalytic efficiency compared to the wild type enzyme Staphylococcus aureus

Inhibitors

EC Number Inhibitors Comment Organism Structure
6.3.4.15 (3aS,4S,6aR)-4-(5-[1-[3-(naphthalen-2-yloxy)propyl]-1H-1,2,3-triazol-4-yl]pentyl)tetrahydro-1H-thieno[3,4-d]imidazol-2(3H)-one
-
 Staphylococcus aureus
6.3.4.15 (3aS,4S,6aR)-4-(5-[1-[4-(naphthalen-1-yloxy)butyl]-1H-1,2,3-triazol-4-yl]pentyl)tetrahydro-1H-thieno[3,4-d]imidazol-2(3H)-one
-
 Staphylococcus aureus
6.3.4.15 (3aS,4S,6aR)-4-(5-[1-[4-(naphthalen-2-yloxy)butyl]-1H-1,2,3-triazol-4-yl]pentyl)tetrahydro-1H-thieno[3,4-d]imidazol-2(3H)-one
-
 Staphylococcus aureus
6.3.4.15 (3aS,4S,6aR)-4-[-[1-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl]methyl]triazol-4-yl]pentyl]-1,3,3a,4,6,6ahexahydrothieno[3,4-d]imidazol-2-one competitive inhibitor Staphylococcus aureus
6.3.4.15 (3aS,4S,6aR)-4-[4-[1-[[(3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)-2,2-dimethyl-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-6-yl]methyl]triazol-4-yl]butyl]-1,3,3a,4,6,6a-hexa hydrothieno[3,4-d]imidazol-2-one
-
 Staphylococcus aureus
6.3.4.15 (3aS,4S,6aR)-4-[5-[1-(4-phenoxybutyl)-1H-1,2,3-triazol-4-yl]pentyl]tetrahydro-1H-thieno[3,4-d]imidazol-2(3H)-one
-
 Staphylococcus aureus
6.3.4.15 (3aS,4S,6aR)-4-[5-[1-[[(3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)-2,2-dimethyl-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-6-yl]methyl]triazol-4-yl]pentyl]-1,3,3a,4,6,6a-hexa hydrothieno[3,4-d]imidazol-2-one
-
 Staphylococcus aureus
6.3.4.15 (3aS,4S,6aR)-4-[5-[3-[[(3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)-2,2-dimethyl-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-6-yl]methyl]triazol-4-yl]pentyl]-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-2-one
-
 Staphylococcus aureus
6.3.4.15 (3aS,4S,6aR)-4-[6-[1-[[(3aR,4R,6R,6aR)-4-(6-aminopurin-9-yl)-2,2-dimethyl-3a,4,6,6a-tetrahydrofuro[3,4-d][1,3]dioxol-6-yl]methyl]triazol-4-yl]hexyl]-1,3,3a,4,6,6a-hexahydrothieno[3,4-d]imidazol-2-one
-
 Staphylococcus aureus
6.3.4.15 2-(4-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentyl]-1H-1,2,3-triazol-1-yl)ethyl 2,2-dimethylpropanoate
-
 Staphylococcus aureus
6.3.4.15 5-methyl-3-[3-(4-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentyl]-1H-1,2,3-triazol-1-yl)propyl]-1,3-benzoxazol-2(3H)-one
-
 Staphylococcus aureus
6.3.4.15 5-methyl-3-[4-(4-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentyl]-1H-1,2,3-triazol-1-yl)butyl]-1,3-benzoxazol-2(3H)-one competitive inhibitor versus biotin Staphylococcus aureus
6.3.4.15 biotinol-5'-AMP
-
 Staphylococcus aureus
6.3.4.15 biotinyl-5'-AMP selective inhibitor Staphylococcus aureus

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
6.3.4.15 0.00101
-
 biotin wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.00108
-
 biotin mutant enzyme R125A, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.00108
-
 biotin mutant enzyme R125N, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.18
-
 ATP wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.35
-
 ATP mutant enzyme R125N, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.42
-
 ATP mutant enzyme R125A, at pH 7.5 and 37°C Staphylococcus aureus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
6.3.4.15 Mg2+ required Staphylococcus aureus

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
6.3.4.15 ATP + biotin + apo-[acetyl-CoA:carbon-dioxide ligase (ADP-forming)] Staphylococcus aureus
-
 AMP + diphosphate + [acetyl-CoA:carbon-dioxide ligase (ADP-forming)]
-
 ?
6.3.4.15 ATP + biotin + apo-[acetyl-CoA:carbon-dioxide ligase (ADP-forming)] Staphylococcus aureus ECT-2
-
 AMP + diphosphate + [acetyl-CoA:carbon-dioxide ligase (ADP-forming)]
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
6.3.4.15 Staphylococcus aureus
-
-
-
6.3.4.15 Staphylococcus aureus ECT-2
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
6.3.4.15
-
 Staphylococcus aureus

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
6.3.4.15 ATP + biotin + apo-[acetyl-CoA:carbon-dioxide ligase (ADP-forming)]
-
 Staphylococcus aureus AMP + diphosphate + [acetyl-CoA:carbon-dioxide ligase (ADP-forming)]
-
 ?
6.3.4.15 ATP + biotin + apo-[acetyl-CoA:carbon-dioxide ligase (ADP-forming)]
-
 Staphylococcus aureus ECT-2 AMP + diphosphate + [acetyl-CoA:carbon-dioxide ligase (ADP-forming)]
-
 ?

Synonyms

EC Number Synonyms Comment Organism
6.3.4.15 biotin protein ligase
-
 Staphylococcus aureus
6.3.4.15 BPL
-
 Staphylococcus aureus

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
6.3.4.15 440
-
 ATP mutant enzyme R125A, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 520
-
 ATP mutant enzyme R125N, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 810
-
 biotin mutant enzyme R125A, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 840
-
 biotin mutant enzyme R125N, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 360000
-
 ATP wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 450000
-
 biotin wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus

Cofactor

EC Number Cofactor Comment Organism Structure
6.3.4.15 ATP
-
 Staphylococcus aureus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
6.3.4.15 0.00009
-
 5-methyl-3-[4-(4-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentyl]-1H-1,2,3-triazol-1-yl)butyl]-1,3-benzoxazol-2(3H)-one wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.00117
-
 (3aS,4S,6aR)-4-[-[1-[[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl]methyl]triazol-4-yl]pentyl]-1,3,3a,4,6,6ahexahydrothieno[3,4-d]imidazol-2-one wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.0017
-
 (3aS,4S,6aR)-4-(5-[1-[4-(naphthalen-2-yloxy)butyl]-1H-1,2,3-triazol-4-yl]pentyl)tetrahydro-1H-thieno[3,4-d]imidazol-2(3H)-one wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.01
-
 2-(4-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentyl]-1H-1,2,3-triazol-1-yl)ethyl 2,2-dimethylpropanoate Ki above 0.01 mM, wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.01
-
 (3aS,4S,6aR)-4-[5-[1-(4-phenoxybutyl)-1H-1,2,3-triazol-4-yl]pentyl]tetrahydro-1H-thieno[3,4-d]imidazol-2(3H)-one Ki above 0.01 mM, wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.01
-
 (3aS,4S,6aR)-4-(5-[1-[4-(naphthalen-1-yloxy)butyl]-1H-1,2,3-triazol-4-yl]pentyl)tetrahydro-1H-thieno[3,4-d]imidazol-2(3H)-one Ki above 0.01 mM, wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.01
-
 (3aS,4S,6aR)-4-(5-[1-[3-(naphthalen-2-yloxy)propyl]-1H-1,2,3-triazol-4-yl]pentyl)tetrahydro-1H-thieno[3,4-d]imidazol-2(3H)-one Ki above 0.01 mM, wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus
6.3.4.15 0.01
-
 5-methyl-3-[3-(4-[5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentyl]-1H-1,2,3-triazol-1-yl)propyl]-1,3-benzoxazol-2(3H)-one Ki above 0.01 mM, wild type enzyme, at pH 7.5 and 37°C Staphylococcus aureus