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Literature summary extracted from

  • Ashok, Y.; Miettinen, M.; Oliveira, D.K.H.; Tamirat, M.Z.; Naereoja, K.; Tiwari, A.; Hottiger, M.O.; Johnson, M.S.; Lehtioe, L.; Pulliainen, A.T.
    Discovery of compounds inhibiting the ADP-ribosyltransferase activity of pertussis toxin (2020), ACS Infect. Dis., 6, 588-602 .
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
2.4.2.30 expressed in Escherichia coli BL21(DE3) cells Bordetella pertussis

Protein Variants

EC Number Protein Variants Comment Organism
2.4.2.30 Q127D/E129D the mutant shows drastically diminished activity compared to the wild type enzyme Bordetella pertussis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.30 (1E,4E)-1,5-di(pyridin-3-yl)penta-1,4-dien-3-one i.e. NSC149286 Bordetella pertussis
2.4.2.30 4,5,7,9-tetrahydro-2H-purine-2,8(3H)-dithione i.e. NSC29193 Bordetella pertussis
2.4.2.30 4-nitro-7-[(1-oxo-1lambda(5)-pyridin-2-yl)sulfanyl]-2,1,3-benzoxadiazole i.e. NSC228155 Bordetella pertussis

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.2.30 NAD+ + Galphai Bordetella pertussis
-
 nicotinamide + (ADP-D-ribosyl)-Galphai + H+
-
 ?
2.4.2.30 NAD+ + Galphai Bordetella pertussis Tohama I
-
 nicotinamide + (ADP-D-ribosyl)-Galphai + H+
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.30 Bordetella pertussis P04977
-
-
2.4.2.30 Bordetella pertussis Tohama I P04977
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
2.4.2.30 HisTrap column chromatography and Superdex 75 gel filtration Bordetella pertussis

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.30 NAD+ + Galphai
-
 Bordetella pertussis nicotinamide + (ADP-D-ribosyl)-Galphai + H+
-
 ?
2.4.2.30 NAD+ + Galphai
-
 Bordetella pertussis Tohama I nicotinamide + (ADP-D-ribosyl)-Galphai + H+
-
 ?

Subunits

EC Number Subunits Comment Organism
2.4.2.30 monomer 1 * 23400, recombinant C-terminally truncated enzyme, SDS-PAGE Bordetella pertussis
2.4.2.30 monomer 1 * 30000, native enzyme, SDS-PAGE Bordetella pertussis

Synonyms

EC Number Synonyms Comment Organism
2.4.2.30 ADP-ribosyltransferase
-
 Bordetella pertussis
2.4.2.30 ART
-
 Bordetella pertussis
2.4.2.30 pertussis toxin
-
 Bordetella pertussis
2.4.2.30 PtxS1
-
 Bordetella pertussis

Temperature Stability [°C]

EC Number Temperature Stability Minimum [°C] Temperature Stability Maximum [°C] Comment Organism
2.4.2.30 54.7
-
 melting temperature Bordetella pertussis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.30 0.003
-
 at pH 7.5 and 25°C Bordetella pertussis 4-nitro-7-[(1-oxo-1lambda(5)-pyridin-2-yl)sulfanyl]-2,1,3-benzoxadiazole
2.4.2.30 0.0068
-
 at pH 7.5 and 25°C Bordetella pertussis 4,5,7,9-tetrahydro-2H-purine-2,8(3H)-dithione
2.4.2.30 0.02
-
 at pH 7.5 and 25°C Bordetella pertussis (1E,4E)-1,5-di(pyridin-3-yl)penta-1,4-dien-3-one