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Literature summary extracted from

  • Wang, G.; Linsley, R.; Norimatsu, Y.
    External Zn2+ binding to cysteine-substituted cystic fibrosis transmembrane conductance regulator constructs regulates channel gating and curcumin potentiation (2016), FEBS J., 283, 2458-2475 .
    View publication on PubMed

Activating Compound

EC Number Activating Compound Comment Organism Structure
5.6.1.6 3-isobutyl-methylxanthine
-
 Homo sapiens
5.6.1.6 isoproterenol
-
 Homo sapiens

Cloned(Commentary)

EC Number Cloned (Comment) Organism
5.6.1.6 expressed in Xenopus laevis oocytes Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
5.6.1.6 R334C the mutant enzyme is unaffected by external ZnCl2 even at 5 mM concentrations. At steady activation, 0.05 mM external ZnCl2 inhibits its channel conductance by 54.47%. Internal curcumin reverses the Zn2+ inhibition Homo sapiens
5.6.1.6 R334C/E1126A this double mutant is insensitive to 0.05 mM ZnCl2 Homo sapiens
5.6.1.6 T1122C 0.05 mM ZnCl2 decreases the channel conductance of the mutant by about 55.2%. Internal curcumin reverses the Zn2+ inhibition Homo sapiens
5.6.1.6 T122H the mutant exhibits Cl--independent Zn2+ inhibition Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.6.1.6 5-[(4-carboxyphenyl)methylene]-2-thioxo-3-[(3-trifluoromethyl)phenyl]4-thiazolidinone
-
 Homo sapiens
5.6.1.6 Zn2+ Zn2+ inhibits channel activity in a dose- and Cl--dependent manner. Cl--dependent Zn2+ inhibition is weakened at higher Zn2+ concentrations, Zn2+ affinity is stronger in the resting state than in the activated state, and activation current noises are decreased by external Zn2+ binding Homo sapiens

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
5.6.1.6 additional information external Zn2+ is without any effect on wild type enzyme activity Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
5.6.1.6 HEK-293T cell
-
 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
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.6.1.6 CFTR
-
 Homo sapiens
5.6.1.6 cystic fibrosis transmembrane conductance regulator
-
 Homo sapiens