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Literature summary for 5.6.1.6 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
Search for more literature for 5.6.1.6

Activating Compound

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

Cloned(Commentary)

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

Protein Variants

Protein Variants Comment Organism
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
R334C/E1126A this double mutant is insensitive to 0.05 mM ZnCl2 Homo sapiens
T1122C 0.05 mM ZnCl2 decreases the channel conductance of the mutant by about 55.2%. Internal curcumin reverses the Zn2+ inhibition Homo sapiens
T122H the mutant exhibits Cl--independent Zn2+ inhibition Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
5-[(4-carboxyphenyl)methylene]-2-thioxo-3-[(3-trifluoromethyl)phenyl]4-thiazolidinone
-
 Homo sapiens
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

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

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293T cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

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

Synonyms

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