Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 5.6.1.6 extracted from

  • Wang, G.
    Molecular basis for Fe(III)-independent curcumin potentiation of cystic fibrosis transmembrane conductance regulator activity (2015), Biochemistry, 54, 2828-2840.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
curcumin molecular basis for Fe(III)-independent curcumin potentiation of cystic fibrosis transmembrane conductance regulator activity, overview. Highly conserved aromatic and positively charged residues at the ICL1/ICL4 interface and phosphorylation site S813 are sensitive to curcumin regardless of whether Fe3+ and nucleotide-binding domain 2 are removed. Spontaneous disulfide cross-linking between curcumin-sensitive ICL1 and S795 is observed to be enough to promote channel opening as curcumin does. Curcumin may potentiate CFTR activity not only by removing inhibitory Fe3+ to release the R domain from ICL3 but also by stabilizing the stimulatory R-ICL1/ICL4 interactions Homo sapiens
additional information phosphorylation-dependent enzyme activity Homo sapiens

Cloned(Commentary)

Cloned (Comment) Organism
transient expression of the enzyme in HEK-293T cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Fe3+ binds at the interface of the regulatory (R) domain and intracellular loop (ICL) 3 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
membrane transmembrane protein Homo sapiens 16020
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P13569
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein stimulatory phosphorylation site S795 and S813 at the C-terminus of the R domain. The phosphorylated R domain, once released from ICL3, may function as a length- and gating-regulatory cross-linker between two transmembrane domains to promote the stimulatory interactions between the R domain and the ICL1/ICL4 interface Homo sapiens

Synonyms

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

General Information

General Information Comment Organism
additional information the phosphorylated R domain, once released from ICL3, may function as a length- and gating-regulatory cross-linker between two transmembrane domains to promote the stimulatory interactions between the R domain and the ICL1/ICL4 interface Homo sapiens