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Literature summary extracted from

  • Galfre, E.; Galeno, L.; Moran, O.
    A potentiator induces conformational changes on the recombinant CFTR nucleotide binding domains in solution (2012), Cell. Mol. Life Sci., 69, 3701-3713.
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
5.6.1.6 2-pyrimidin-7,8-benzoflavone induces significant conformational changes of the isolated NBD1/NBD2 dimer in solution. 2-pyrimidin-7,8-benzoflavone does not modify the ATP binding constant, but reduces the ATP hydrolysis activity of the NBD1/NBD2 mixture. In absence of ATP, the NBD1/NBD2 dimer is disrupted by the compound, but in the presence of 2 mM ATP, the two NBDs keep dimerised, and a major change in the size and the shape of the structure is observed Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.6.1.6 expression of recombinant NBD1, from residue 394 to residue 672, and NBD2, from residue 1191 to residue 1480, polypeptides in Escherichia coli Homo sapiens

General Stability

EC Number General Stability Organism
5.6.1.6 in the absence of ATP, the Gd-HCl concentration to denature half of the proteins is about 2.2 M. A smaller Gd-HCl concentration,1.4 M, is needed to produce the same effect upon the application of 25 nM of 2-pyrimidin-7,8-benzoflavone Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
5.6.1.6 0.00331
-
 ATP isolated NBD1/NBD2 mixture, pH 8.0, 25°C Homo sapiens
5.6.1.6 0.0071
-
 ATP isolated NBD1/NBD2 mixture, presence of 12 nM 2-pyrimidin-7,8-benzoflavone, pH 8.0, 25°C Homo sapiens
5.6.1.6 0.00964
-
 ATP isolated NBD1/NBD2 mixture, presence of 25 nM 2-pyrimidin-7,8-benzoflavone, pH 8.0, 25°C Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
5.6.1.6 Homo sapiens
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.6.1.6 ATP + H2O + closed Cl- channel
-
 Homo sapiens ADP + phosphate + open Cl- channel
-
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